DSPG-Na is the component of liposomes for drug delivery.

Vanin-1-IN-2 is a potent vanin-1 inhibitor with an IC50 of 162 nM. Vanin-1 is a cell-surface-associated, glycosylphosphatidyl inositol (GPI)-anchored protein which is expressed at high levels in the kidney, liver, and small intestine.

Nur77 modulator 2, a Nur77 modulator (Kd of 0.35 μM), is a potent and orally active inflammation inhibitor. Nur77 modulator 2 modulates the colocalization of Nur77 at mitochondria.

ZA3-Ep10 is a zwitterionic lipid used in lipid nanoparticles formulation for in vivo RNA delivery and non-viral CRISPR/Cas gene editing.

FEN1-IN-SC13 is a potent DNA fragmentation endonuclease 1 (FEN1) inhibitor (CN106692155A, SC13).

W3601 is the impurity of Lidocaine. W3601 exhibits nerve blocking activity with the pKa of 7.4.

BTC tetrapotassium is a low affinity calcium indicator (Kd approximately 7-26 µM) featuring many desirable properties for cellular calcium imaging, including long excitation wavelengths (400/485 nm), low sensitivity to Mg2+, and accuracy of ratiometric measurement.

Dihydrorhodamine 6G (DHR 6G) is the reduced form of Rhodamine 6G, which is used as fluorescent mitochondrial dye. It is nonfluorescent, but it readily enters most of the cells and is oxidized by oxidative species or by cellular redox systems to the fluorescent rhodamine 6G that accumulates in mitochondrial membranes. Dihydrorhodamine 6G is useful for detecting reactive oxygen species (ROS) including superoxide.

B10-S is a potent anti-allergic agent. B10-S can inhibit the degranulation of LAD2 induced by substance P.

DiAzK is a bifunctional amino acid. DiAzK can be inserted into almost any protein interface with minimal structural perturbation using genetic code expansion.

Allyl (2-aminoethyl)carbamate is a cleavable linker.

LY3372689 is an orally active O-GlcNAcase (OGA) enzyme inhibitor. LY3372689 can be used for tauopathies research, including Alzheimer’s disease.

O-GlcNAcase-IN-4 is a O-GlcNAcase inhibitor extracted from patent WO2018140299A1 Formulaic Ic. O-GlcNAcase-IN-4 can be used for the research of neurodegenerative diseases and disorders, such as Alzheimer's disease.

4-PQBH is a potent Nur77 binder (KD=1.17 μM). 4-PQBH extensively induces caspase-independent cytoplasmic vacuolization and paraptosis through Nur77-mediated ER stress and autophagy. 4-PQBH can be used for cancer research.

Ethylene glycol diacrylate (Ethylene diacrylate) is a cross-linking homobifunctional reagent. Ethylene glycol diacrylate can be polymerized to form poly(ethylene glycol) diacrylate for drug delivery.

(R)-BDP9066 is a potent inhibitor of myotonic dystrophy kinase-related Cdc42-binding kinase (MRCK). (R)-BDP9066 blocks cancer cell invasion. (R)-BDP9066 has the potential for the research of proliferative diseases, such as cancer.

NVP-DKY709 is a potent IKZF2 inhibitor for the treatment of cancers.

FTT5 is a lipid-like compound for efficient delivery of long mRNAs in vivo.

GFP150 TFA is a green fluorescent protein used for labeling proteins.

3CPLro-IN-1 (compound A17) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 of 5.65 μM. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive drug target for fighting COVID-19.

THR-β agonist 2 is a potent agonist of THR-β. THR-β agonist 2 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021121210A1, compound 3).

Glucobrassicanapin (4-Pentenylglucosinolate) potassium is an aliphatic glucosinolate in vegetable crops of Brassica rapa.

BAY-888 exhibits IC50 value of 1.5 nM and 5.5 nM towards CSNK1A1 and CSNK1D, respectively.

BAY-204 is an inhibitor of Casein kinase 1 alpha and delta (CSNK1α and δ) useful for the treatment of proliferative disorders.

MIF-IN-4 hydrochloride is potent macrophage migration inhibitory factor (MIF) inhibitor (pIC50=5.01-6). MIF is a cytokine originally found to play a role in inhibiting macrophage migration.

LC kinetic stabilizer-1 (compound 21) is a potent and selective amyloidogenic immunoglobulin light chain kinetic stabilizer with EC50s of 140 and 74.1 nM for WIL-FL* and WIL-FL* T46L/F49Y, respectively. WIL-FL is an amyloidogenic FL LC dimer.

(R)-CFT7455 is a IKZF1/3 degrader extracted from patent WO2020210630A1. (R)-CFT7455 can be used for the research of defective proteasomal degradation.

BDP-4 is an amino acid-modified near-infrared Aza-BODIPY photosensitizer, acts as an immune initiator for potent photodynamic therapy in melanoma.

Spermine Prodrug-1 (Compound 1) is a redox-sensitive spermine prodrug for the potential treatment of snyder robinson syndrome. Spermine Prodrug-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively.

XT2 is a potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 of 9.1 nM. XT2 suppresses CCl4-induced upregulation of ALT, a key biomarker of acute liver injury. XT2 also decreases immune cell infiltration into the injured liver tissue. XT2 has the potential for the research of liver inflammatory diseases.

RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer.

CD38 inhibitor 2 is a potent CD38 inhibitor (IC50 = 0.01 ~ 0.1 μΜ).

Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.

Remdesivir de(ethylbutyl 2-aminopropanoate) is an impurity of Remdesivir. Remdesivir, a nucleoside analogue with effective antiviral activity, has EC50s of 74 nM for SARS-CoV and MERS-CoV in HAE cells, and 30 nM for murine hepatitis virus in delayed brain tumor cells. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.

TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe. TEPC466 shows a high degree of selectivity and sensitivity for the detection of PKM2 protein via the AIE effect. EPC466 can be used for the detection of PKM2. TEPC466 is successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. TEPC466 is a useful tool for cancer diagnosis and research.

Glutathione synthesis-IN-1 (DC-1) is a glutathione synthesis inhibitor.

(±)9,10-DiHOME is the racemate of 9,10-DiHOME. 9,10-DiHOME is a leukotoxin derivative of linoleic acid diol that has been reported to be toxic in human's tissue preparations, and is produced by inflammatory leukocytes such as neutrophils and macrophages.

246C10 is a synthesized ionizable lipid. 246C10 can be formulated into lipid nanoparticles (LNPs) with dioleoylphosphatidylethanolamine (DOPE), cholesterol, and C16-PEG2000 ceramide (PEG-lipid) as well as mRNA. The lipid nanoparticle formulations can be used for mRNA delivery. To obtain iLNPs that could specifically target liver sinusoidal endothelial cells (LSECs), six different ionizable lipids (241C10 to 246C10) were synthesized by an epoxide ring-opening reaction with piperazine- or piperidine-containing amines. Biodistribution and gene regulation of various iLNPs were assessed in vivo, and the results showed that the 246C10 iLNPs (containing piperazine amine) had the highest luciferase expression in the liver. When further analyzing the 246C10 iLNPs transfection efficiency in different types of liver cells, it was found that tdTomato fluorescence was mainly concentrated in hepatocytes, not in LSECs. Figure 6f shows that 80% of hepatocytes are fluorescent, 40% of LSECs are fluorescent, and 20% of Kupffer cells are fluorescent. Due to the mannose receptor on LSECs, mannose-PEG lipid was introduced into 246C10 iLNPs to alter the distribution of iLNPs in different liver cells. As shown in Figure 6g, tdTomato fluorescence distribution was 15% of hepatocytes, 70% of LSECs, and 15% of Kupffer cells, significantly improved the ability of iLNPs to actively target LSECs. In contrast, this work indirectly shows that the iLNPs with piperazine head lipid are more able to deliver mRNA to the liver and translate the target protein than the iLNPs with piperidine head lipid. It is worth mentioning that the preparation buffer of 246C10 iLNPs could influence the encapsulation efficiency of mRNA. With the addition of sodium chloride in the citrate buffer, the encapsulation efficiency of CRISPR-Cas9 mRNA and sgRNA was increased. These iLNPs were able to treat hemophilia safely, without causing hepatotoxicity, the immune response induced by Cas9 and off-target editing.

OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.

SSAO/VAP-1 inhibitor 1 is a potent inhibitor of SSAO/VAP-1. SSAO/VAP-1 promotes the transfer of Glucose transport 4 (GLUT 4) from adipocytes to the cell membrane, thereby regulating glucose transport. In endothelial cells, SSAO/VAP-1 can mediate the adhesion and exudation of leukocytes and endothelial cells, and participate in inflammatory responses. SSAO/VAP-1 inhibitor 1 has the potential for the research of inflammation and/or inflammation-related disease or diabetes and/or diabetes-related disease (extracted from patent WO2021102774A1, compound E3).

THRβ Agonist 1 is a potent and selective agonist of THRβ. Thyroid hormone receptor mediates the physiological activity of thyroid hormones which plays a key role in normal growth and development of the body and in maintaining metabolic balance. THRβ Agonist 1 has the potential for the research of thyroid hormone receptor-related diseases (extracted from patent WO2021104288A1, compound 2).

THR-β agonist 3 is a potent agonist of THR-β. THR-β agonist 3 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021129827A1, compound 6).

BuChE-IN-1 (Compound 23) is a potent inhibitor of butyrylcholinesterase (BuChE). Butyrylcholinesterase (BuChE) is recently regarded as a biomarker in progressed Alzheimer’s disease (AD).

THR-β agonist 4 is a potent agonist of THR-β. THR-β agonist 4 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021143706A1, compound 72).

GRK6-IN-2 (compound 10a) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for the research of multiple myeloma.

1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol) sodium salt is a lipid molecule having one negative charge, which can interact with the positive charges of peptides.

ADAMTS-5-IN-3 (Example 37-2) is a potent inhibitor of ADAMTS-5 and ADAMTS-4 with IC50s of 8 and 12 nM, respectively. ADAMTS-5-IN-3 can be used for the research of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis.

Antimalarial agent 8 (Compound 7e) is a novel orally active class of antimalarials. Antimalarial agent 8 is potent in vitro against P. falciparum and is orally efficacious (40 mg/kg) in an in vivo mouse model of malaria.

CSF1R-IN-6 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-6 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-6 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 5).

CHD1Li 6.11 is a potent oncogenic CHD1L inhibitor (IC50=3.3 µM for cat-CHD1L recombinant protein). CHD1Li 6.11 is an orally bioavailable antitumor agent, significantly reducing the tumor volume of CRC xenografts generated from isolated quasi mesenchymal cells (M-phenotype), which possess enhanced tumorigenic properties.

RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM). RECQL5-IN-1 inhibits RECQL5-WT cells and RECQL5-KO2 cells with IC50s of 4.8 μM and 19.6 μM, respectively. RECQL5-IN-1 can be used for the research of breast cancer.

Myt1-IN-4 (compound 181) is a potent Myt1 inhibitor with an IC50 of <10 nM. Myt1-IN-4 has anticancer effects.

5-heptyl-DNJ is a potent GAA agonist with a Ki of 0.0047 μM. 5-C-heptyl-DNJ increases GAA activities by chaperrone effects.

Fludarabine-Cl (ZYS-1) has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases[1].

SGC agonist 2 is a potent agonist of soluble guanylate cyclase (SGC). Soluble guanylate cyclase is a key signal transduction enzyme in the NO-sGC-cGMP signaling pathway. SGC agonist 2 has the potential for the research of cardiovascular disease (heart failure, pulmonary hypertension, angina, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis) (extracted from patent WO2021219088A1, compound 031).

SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14).

SSTR4 agonist 4 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14).

Chalcones A-N-5 is a trihydroxy chalcone derivative compound. Chalcones A-N-5 doesn’t show cytotoxicity at the concentration lower than 100 µM (with IC50 > 1 mM), but has a significant effect on promoting cell proliferation. Chalcones A-N-5 potentially promotes neuronal cell growth in the damaged brain tissue. Chalcones A-N-5 also inhibits ferroptosis induced by RSL or erastin and reduces the lipid peroxidation levels induced by Aβ1-42 protein aggregation. Chalcones A-N-5 is a promising molecular skeleton candidate for further development of lead compound for in vivo test to research AD.

ABAI-30 is a potent and orally active anti-inflammatory agent. ABAI-30 effectively inhibits NO production in lipopolysaccharide (LPS) induced RAW264.7 cells.

3CPLro-IN-2 (compound C1) is a potent and orally active inhibitor of SARS-CoV-2 3CLpro with an IC50 and Ki of 1.55 and 6.09 μM, respectively. 3-Chymotrypsin-like cysteine protease (3CLpro) is an indispensable protein in viral replication and represents an attractive drug target for fighting COVID-19.

SC-435 is an apical sodium-dependent Bile acid (BA) transporter inhibitor. SC-435 can alter hepatic cholesterol metabolism and lower plasma low-density lipoprotein-cholesterol concentrations.

Tidiacic is a hepatoprotective agent that acts as an antioxidant and a sulfur donor.

2-Nitro-5-thiocyanatobenzoic acid (NTCB) is a highly reactive reagent that transfers its cyano group rapidly to a nucleophilic thiolate. 2-Nitro-5-thiocyanatobenzoic acid has been proposed as a reagent for converting thiol groups in proteins into their S-cyano derivatives.

APF is a fluorescence probe that can selectively, and dose dependently detect certain species among ROS and that are highly resistant to autoxidation. APF can be used in enzymatic and cellular systems.

BMPO (BocMPO) is a cyclic nitrone spin trap. BMPO offers several advantages over the existing spin traps in the detection and characterization of thiyl radicals, hydroxyl radicals, and superoxide anions in biological systems.

Isaxonine acts as a modifier of the surface pH of the bilayer. Isaxonine accelerates the rate of peripheral nerve regeneration, stimulate axonal sprouting and promote motor and sensory function recovery. Isaxonine is a neurotrophic agent.

NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17).

KDdiA-PC is a kind of oxidized LDL (oxLDL), and is a ligand for the macrophage scavenger receptor CD36.

Buramate exhibits neuroprotective and anticonvulsant activities.

Salacetamide (N-Acetylsalicylamide) is the stable isomer of O-Acetylsalicylamide, is a product for proteomics research.

5β-Cholanic acid can be used for 5β-Cholanic acid derivatives synthesis.

BMS-566419 is an acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase (IMPDH). Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme in the de novo synthesis of guanosine nucleotides. BMS-566419 has clinical utility for the research of transplant rejection.

DCVJ (9-(2,2-Dicyanovinyl)julolidine), a molecular rotor and unique fluorescent dye, binds to tubulin and actin, and increases its fluorescence intensity drastically upon polymerization. DCVJ also binds to phospholipid bilayers and increases its fluorescence intensity. DCVJ can detect the kinetic process of degranulation of mast cells.

Tilomisole (Wy 18251) is a benzimidazothiazole experimental drug with anti-inflammatory activity. Tilomisole causes less agranulocytosis than levamisole, but retains immunomodulating capabilities. Tilomisole is orally active. Tilomisole has the potential for the research of cancer and inflammation.

1,2-Dilauroyl-sn-glycerol is a saturated diacylglycerol and may play a role in second messenger signal transduction.

Dioctanoylglycol (Ethylene glycol dicaprylate), a diacylglycerol analog, is a diacylglycerol kinase (DGK) inhibitor (Ki of 58 μM).

Chrysamine G, a carboxylic acid analogue of Congo Red, can be used as a probe of amyloid deposition in Alzheimer's disease. Chrysamine G also can inhibit Aβ-induced toxicity in PC12 cells.

Anticancer agent 38 (compound 19), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 38 inhibits A431 cell growth with an IC50 of 5.2 µg/mL.

Pyruvate Carboxylase-IN-1 (compound 37) is a potent inhibitor of pyruvate carboxylase (PC) with IC50s of 0.204 and 0.104 μM in cell lysate-based and cell-based PC activity, respectively. Pyruvate Carboxylase-IN-1 is a natural analog of erianin. Pyruvate Carboxylase-IN-1 inhibites the enzymatic activity of PC, mediating the anticancer effect in human hepatocellular carcinoma (HCC).

Coelenteramine 400a (Bisdeoxycoelenterazine), a derivative of Coelenterazine, is a Renilla luciferase (RLuc) substrate. In the presence of Coelenteramine 400a, RLuc can emit blue light at 395 nm.

GYKI-13380 is an appetite suppressant. GYKI-13380 has the potential for the research of neurology diseases.

Quin C1 is a highly specific and potent agonist for formyl peptide receptor 2 (FPR2/ALX). Quin-C1 significantly reduces the neutrophil and lymphocyte counts in BALF, diminishes expression of TNF-α, IL-1β, KC, and TGF-β1, and decreases collagen deposition in lung tissue. Quin C1 has the potential for the research of lung injury.

TASIN-1 is a selective inhibitor of truncated APC gene (adenomatous polyposis coli gene) and exerts cytotoxic effects through inhibition of cholesterol biosynthesis. TASIN-1 represents a potential therapeutic strategy for prevention and intervention in CRC with mutant APC.

m7GpppApG is a trinucleotide mRNA 5' cap analog that can be used for RNA synthesis in vitro.

MIF-IN-1 (compound 14) is a potent macrophage migration inhibitory factor (MIF) inhibitor (pIC50=6.87).

Anisole-piperazine-methanone-benzothiazole-p-methylpiperidine is an active compound.

S(-)-Bisoprolol is a S(-)-enantiomer of Bisoprolol. Bisoprolol is a potent, selective and orally active β1-adrenergic receptor blocker. Bisoprolol has little activity on β2-receptor and has the potential for hypertension, coronary artery disease and stable ventricular dysfunction research.

2-Hydroxyestradiol-13C6 is the 13C-labeled 2-Hydroxyestradiol. 2-Hydroxyestradiol, a metabolite of 17β-estradiol with minimal estrogenic activity, possesses antioxidant effects and reacts with DNA to form stable adducts and exerts genotoxicity.

WH-10417-099 is a degrader that could collectively induce degradation of the largest number of unique kinases (>125 unique kinases).

SK-3-91 is a multi-kinase degrader. SK-3-91 could collectively induce degradation of the largest number of unique kinases (>125 unique kinases).

Mitochondria-Targeted Photoactivatable Prodrug accumulates in the mitochondria and shows light-triggered temporally controlled cell death. Mitochondria-Targeted Photoactivatable Prodrug can be used in a novel drug delivery platform that provides on-demand, real-time, organelle-specific drug release and monitoring upon photoactivation.

AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis.

NCGC00538431 is a potent modulator of SIRPα-CD47.

Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively.

Antimalarial agent 9 (Compound 11) is a potent antimalarial agent. Antimalarial agent 9 is a quinoline-imidazole derivative compound. Antimalarial agent 9 exhibits significant antimalarial efficacy in-vitro against both CQ-sensitive (IC50-0.14 μM) and MDR strain (IC50-0.41 μM) with minimal cytotoxicity and high selectivity.

Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM.

Anticancer agent 35 (compound 10), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 35 inhibits A549, A431, PACA2 cell growth with IC50s of 18.1 µg/mL, 4.0 µg/mL, 18.9 µg/mL, respectively.

Anti-inflammatory agent 13 (Compound 3) is a pentacyclic triterpene compound. Anti-inflammatory agent 13 exhibits a considerable inhibitory effect on inflammation models. Anti-inflammatory agent 13 has the potential for the research of either DAMPs or PAMPs triggered inflammation.

Glucosylceramide synthase-IN-3 (compound BZ1) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 16 nM for human GCS.Glucosylceramide synthase-IN-3 can be used for Gaucher's disease research.

Agistatin B, isolated from fungus, is a mycotoxin. Agistatin B inhibits cholesterol synthesis.

Agistatin E is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.

Edotreotide is a somatostatin analogue. Edotreotide bound to various radionuclides, has the potential for the research and diagnosis of certain types of cancer.

Deoxybrevianamide E, an indole alkaloid, is a biosynthetic precursor for advanced metabolites isolated from the marine-derived Aspergillus sp..

BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease.

CD73-IN-6 is a CD73 inhibitor extracted from patent WO2022007677A1 compound 2. CD73-IN-6 can be used for the research of cancer.

GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells.

Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively).

Citalopram is marketed as a racemate mixture of the S(+)-enantiomer and R(-)-enantiomer and the active S(+)-enantiomer (Escitalopram) that possess inhibitory effects. Citalopram is an antidepressant and enhances serotoninergic neurotransmission through potent and selective inhibition of serotonin reuptake (selective serotonin reuptake inhibitor).

(-)-(E)-α-Atlantone is a volatile constituent of Artemisia vestita oil.

Methyl jasmonate is a phytohormone involved in plant defenses under stress conditions. Methyl jasmonate can improve antioxidant properties of blueberry leaf extracts (mainly anthocyanins), and decrease the viability and migration capacity of AGS cells. Anticarcinogenic activity.

4-epi-Withaferin A (compound 28) is the analogue of Withaferin A. 4-epi-Withaferin A enhances cytotoxicity and cytoprotective heat-shock-inducing activity (HSA). 4-epi-Withaferin A has the potential for the research of protein aggregation-associated diseases by stimulating cellular defense mechanisms.

MC 304 is a β-resorcylate isolated from cultures of Phanerochaete chrysosporium. MC 304 has antibacterial activity. MC 304 shows a stimulatory effect on root elongation of Lepidium satiuum.

Agistatin D is a pyranacetal originally isolated from a Fusarium sp. that inhibits the cholesterol biosynthesis.

Roridin A is an inhibitor of pollen development in Arabidopsis thaliana. Roridin A is isolated from the fungus Cylindrocarpon sp. Roridin A inhibits the pollen development at concentrations of 2 μM.

Aquastatin A is an inhibitor of mammalian adenosine triphosphatases. Aquastatin A is isolated from a fungus identified as Fusarium aquaeductuum. Aquastatin A inhibits Na+/K(+)-ATPase with an IC50 value of 7.1 μM, and H+/K(+)-ATPase with an apparent IC50 value of 6.2 μM.

Carbolactone is a biologically active metabolite from fungi.

Pixinol, a natural glycoside, shows cytotoxicity against the human lung carcinoma GLC4 and adenocarcinoma COLO 320 cell lines (IC50=71 µM and 43 µM, respectively).

4-Methyl withaferin A is a withaferin A-analogue with anti-tumor activity.

4,27-Dimethyl withaferin A is a synthetic analog of withanolide natural products. 4,27-Dimethyl withaferin A has the potential for the research of neurodegenerative diseases (extracted from patent WO2015077780A1).

Terrelumamide A is a lumazine-containing peptide. Terrelumamide A is isolated from the culture broth of the marine-derived fungus Aspergillus terreus. Terrelumamide A exhibits pharmacological activity by improving insulin sensitivity. Terrelumamide A has the potential in the application of DNA sequence recognition.

Trypacidin is the conidia-bound metabolite with antiprotozoal activity. Trypacidin has a protective function against phagocytes both in the environment and during the infection process.

epi-Progoitrin is the major thioglucoside of Crambe abyssinica seed.

Stachybotrysin B is a phenylspirodrimane derivative. Stachybotrysin B is isolated from Stachybotrys chartarum CGMCC 3.5365.

Diallyl disulfide inhibits human squalene monooxygenase with an IC50 of 400 μM for squalene epoxidation.

2,3-Dihydro-3-methoxywithaferin A is an analogue of 2,3-dihydrowithaferin-A. 2,3-Dihydro-3-methoxywithaferin A inhibits proiiferation of P388 cells.

Methyl tetracosanoate is used as an analytical standard in chromatographic assays.

Gluconapin potassium is the precursor of sulforaphane. Sulforaphane is a potent anti-cancer isothiocyanate.

OB3, a derivative of Leptin, show more effective than leptin in reducing obesity and diabetes in mouse models. OB3 can reduce Leptin-related inflammation and proliferation in hepatocellular carcinoma cells.

Hortein is a natural product from the fungus Hortaea werneckii associated with the sponge Aplysina aerophoba.

Tajixanthone is the fungus metabolite from Aspergillus variecolor.

Mycestericin C is a compound isolated from the culture broth of Mycelia sterilia ATCC 20349. Mycestericin C suppresses the proliferation of lymphocytes in the mouse allogeneic mixed lymphocyte reaction.

Muristerone A is a phytoecdysteroid analog of ecdysone and a potent agonist of ecdysteroid receptor with a Kd of 1 nM.

(-)-(E)-Guggulsterone is the metabolite of Z-guggulsterone. Guggulsterone is an active constituent of guggulipid, an ayurvedic drug derived from Commiphora mukul. Guggulsterone has hypolipidaemic activity.

Agonodepside B is a compound isolated from a nonsporulating filamentous fungus, F7524.

Anhydroophiobolin A is a potent inhibitor of photosynthesis with IC50s of 77 and 14 mM in the photosynthesis of chlorella and spinach, respectively. Anhydroophiobolin A is an analog of Ophiobolin A.

Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity.

Choline oxidase catalyzes the oxidation of choline to glycine betaine via betaine aldehyde in glycine betaine biosynthesis and betaine acts as an osmolyte. Choline oxidase has potential in enzymatic betaine production.

Aspulvinone O is a natural inhibitor of aspartate transaminase 1 (GOT1). GOT1 plays an important role in energy metabolism and Reactive Oxygen Species (ROS) balance. GOT1 may serve as an important target in PDAC. Aspulvinone O suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism.

11-O-Methylpseurotin A is a compound of mixed polyketide synthase–nonribosomal peptide synthetase (PKS/NRPS) origin. 11-O-Methylpseurotin A selectively inhibits a Hof1 deletion strain.

γ-AA peptide P6 (Cyclic γ-AA P6) is a potent activator of E6 associated protein (E6AP). γ-AA peptide P6 can stimulate the self-ubiquitination of E6AP and E6AP-catalyzed substrate ubiquitination in reconstituted reactions in vitro. γ-AA peptide P6 can also enhance the ubiquitination of E6AP substrates in the cell and accelerate their degradation by the proteasome.

3-(2-Hydroxyethyl) thio withaferin A is a Withaferin A derivative. Withaferin A, a steroidal lactone, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.

Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer. IC50 value: Target: In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].

>98%,Standard References

Colchicine is a potent therapeutic tool against COVID-19. Colchicine is a tricyclic alkaloid that is extracted from the plant Colchicum autumnale. Colchicine acts as a potent inhibitor of tubulin polymerization.

Diquat dibromide is a comprehensive herbicide commonly used in the cultivation of cotton, soybeans, and other crops to combat unwanted weeds. Diquat dibromide has an IC50 of 60 mg/L in the Allium root growth inhibition test.

SLEC-11 acts as a potential synthetic lethal lead for the treatment of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1-/-.

Custirsen is a highly specific antisense oligonucleotide that inhibits the production of clusterin , an antiapoptotic protein that is upregulated in response to chemotherapy and that confers treatment resistance.

Triton X-100 is a non-denaturing detergent that solubilizes lipid membranes. Triton X-100 is commonly used in laboratories and is applied to vaccines at different stages of the manufacturing process. Triton X-100 is listed as an excipient in certain vaccines including split virus influenza vaccines. Triton X-100 is a nonionic surfactant.

Anticancer agent 37 (compound 18), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 37 inhibits HePG2 cell growth with an IC50 of 17.2 µg/mL.

Benzyl-piperazine-CO-benzothiazole-4-methylpiperidine alters the lifespan of a eukaryotic organism.

CLinDMA, a cationic lipid, can cause inflammatory response. CLinDMA can be used for the synthesis LNP201. LNP201 is a liposome assembly for systemic delivery of siRNA.

Volanesorsen is an antisense oligonucleotide targeting Apolipoprotein C-III (APOC3) mRNA to treat patients with the familial chylomicronemia syndrome.

98N12-5 is an ionizable cationic lipid. It has been used in combination with other lipids in the generation of lipid nanoparticles (LNPs). LNPs containing 98N12-5 and encapsulating proprotein convertase subtilisin kexin type 9 (PCSK9) siRNA selectively accumulate in the liver and reduce total serum cholesterol levels in mice and rats and serum LDL levels in cynomolgus monkeys.

PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM).

BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer.

17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC50s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC).

ChemR23-IN-3 is a potent thiazole-based ChemR23 inhibitor with an IC80 value of 12 nM.

TS010 is a potent inhibitor of GLO-I with IC50 of 0.57 μM. TS010 has the potential for the research of cancer disease.

Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC50 of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro.

Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively.

BOD-NH-NP is an activatable fluorescent probe for imaging endogenous nitric oxide via the eNOS enzymatic pathway.

AGL-0182-30 is a proprietary microtubule disrupting agent.

Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM.

ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells.

Anti-inflammatory agent 12 (Compound 2) is a pentacyclic triterpene compound. Anti-inflammatory agent 12 shows a significant bias in the LPS-induced inflammatory response with an IIC50 value of 2.22 μM. Anti-inflammatory agent 12 has the potential for the research of inflammation disease.

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.

GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.

PHGDH-IN-2 is a potent and NAD+ competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells.

A cathepsin cleavable ADC peptide linker.

13PCSK9i is a highly potent PCSK9-LDLR disruptor peptide with EC50 of 2 nM, SPR Kd of 6.1 nM and 21 nM for hPCSK9 and mPCSK9.13PCSK9i reduces plasma cholesterol levels and increases hepatic LDLR density in a dose-dependent manner.13PCSK9i functions by a unique, allosteric mechanism and is the smallest molecule identified to date with in vivo PCSK9-LDLR disruptor function.

A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB.

A small-molecule enhancer of autophagy through an mTOR-independent pathway; significantly reduces the number of eGFP-HDQ74-positive cells, and increases the transcript level of p62 in Atg5+/+ MEFs; significantly reduces levels of endogenous p62 and cell death in NPC1 hiPSC-derived neurons; enhances bacterial clearance and suppresses IL-1β Secretion in an autophagy-dependent manner; a valuable tool for studying the role of autophagy in the context of cellular homeostasis and disease.

anle145c is a small molecule inhibitor of amyloid aggregation and formation, inhibits human islet amyloid polypeptide (hIAPP)-induced death of INS-1E cells.anle145c has a special mode of action in which anle145c-stabilized oligomers act as a thermodynamic sink for the preferred aggregation state of hIAPP and anle145c.anle145c prevents hIAPP fibril formation in solution, and converts preformed hIAPP fibrils into non-toxic oligomers.anle145c is a promising candidate to inhibit protein aggregation in case of T2DM.

AS105 (AS-105) is a highly potent, ATP-competitive CaMKII inhibitor, inhibits CaMKIIδ with IC50 of 8 nM, Ki of 3 nM. AS105 is also effective against autophosphorylated CaMKII (in contrast to the commonly used allosteric CaMKII-inhibitor KN-93). In isolated atrial cardiomyocytes from human donors and ventricular myocytes from CaMKIIδC-overexpressing mice with heart failure, AS105 effectively reduced diastolic SR Ca2+ leak by 38% to 65% as measured by Ca2+-sparks or tetracaine-sensitive shift in [Ca2+]i. AS105 effectively reduced SR Ca2+-leak, thus improving SR Ca2+-accumulation and reducing cellular arrhythmogenic correlates, without negatively influencing excitation-contraction coupling.

Autophagy inducer D61 is a small molecule autophagy inducer with antibacterial activity, induces LC3II and promotes aggregation of LC3II near Salmonella.D61 (25 uM) reduced the bacterial load (GFP signal in RAW 264.7 macrophages) by 20-fold, with IC50 of 1.3 μM in the SAFIRE assay.D61 antibacterial activity depends on the VPS34 complex and on ATG5.D61 also reduced Salmonella load in the spleens and livers of infected mice.D61 antibacterial activity in macrophages is synergistic with the antibiotic chloramphenicol but that this synergy is largely independent of the known autophagy-stimulating activity of chloramphenicol.Salmonella enterica is a natural bacterial pathogen of humans and animals that causes systemic infection or gastroenteritis.

Autophazole is a novel autophagy inhibitor, promotes cancer cell death via caspase activation.Autophazole was internalized into lysosomes of cells where it induced lysosomal membrane permeabilization (LMP), promoted LMP-mediated apoptosis.LMP induced by Autophazole caused release of cathepsins from lysosomes into the cytosol. Cathepsins in the cytosol cleaved Bid to generate tBid, which subsequently activated Bax to induce mitochondrial outer membrane permeabilization (MOMP).Autophazole is a new chemical probe in efforts aimed at gaining a better understanding of the autophagic process.

Autoquin is a novel autophagy inhibitor (IC50=0.56 uM) by indirect modulation of the activity of the lysosomal enzymes acid sphingomyelinase and acid ceramidase; Autoquin showed a dose‐dependent inhibition of EGFP‐LC3 puncta after 3 hours upon autophagy induction by amino acid starvation in the primary screening assay. Autoquin is a lysosomotropic compound that acts as a functional inhibitor of acid sphingomyelinase, increases lysosomal mass and sequesters Fe2+ to the lysosomes in MCF7 cells, causing an increase in lysosomal reactive oxygen species.

BI-4916 (BI-4916) is the prodrug of BI-4924, which is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.

BI-4924 (BI 4924) is a potent, selective NADH/NAD+-competitive PHGDH inhibitor with IC50 of 2 nM.BI-4924 splays high selectivity against the majority of other dehydrogenase targets.

BTX306 (BTX-306) is a novel protein homeostatic modulator, potently reduces levels of GSPT1, eRF1, CK1α, MCL-1, and c-MYC in myeloma cells, overcomes bortezomib and lenalidomide resistance.BTX306 is much more potently reduced human-derived myeloma cell line viability, with median inhibitory concentrations in the single nanomolar range versus micromolar values for lenalidomide or pomalidomide, and more potently activated caspases 3/8/9.BTX306 did not impact viability of murine hematopoietic cells in an in vivo model, demonstrating its specificity for human cereblon.BTX306 did show some reduced activity in lenalidomide-resistant cell line models but nonetheless retained its nanomolar potency in vitro, overcame bortezomib resistance, and was equipotent against otherwise isogenic cell line models with either wild-type or knockout TP53.BTX306 demonstrated strong activity against primary CD138-positive plasma cells, showed enhanced anti-proliferative activity in combination with bortezomib and dexamethasone.BTX306 was effective in an in vivo systemic model of multiple myeloma.

CaMK1D-IN-18 is a potent, selective CaMK1D inhibitor with IC50 of 31 nM, >150-fold greater activity against CaMK1D than all non-CaMK1 kinases.CaMK1D-IN-18 improves insulin sensitivity and glucose control in the diet-induced obesity mouse model after both acute and chronic administration.

CBK288679 (CBK79) is a novel compound that impairs both protein degradation by the ubiquitin-proteasome system (UPS) and autophagy.CBK79 inhibits cell viability of MelJuSo Ub-YFP cells with 72h IC50 of 0.22 uM, CBK79-inflicted cell death was caspase-independent.CBK79 causes accumulation of ubiquitin-dependent and -independent proteasome substrates.CBK79 induces non-canonical lipidation of MAP1LC3B/LC3B (microtubule-associated protein 1 light chain 3 beta) that requires ATG16L1 but is independent of the ULK1 and class III phosphatidylinositol 3-kinase (PtdIns3K) complexes.CBK79 (10 uM) induces proteotoxic stress and the heat shock response in HOS GFP-LC3B cells.CBK79 has unique features as it inhibits both ubiquitin-dependent and -independent degradation of short-lived proteins by the UPS, as well as the degradation of long-lived proteins by autophagy.

CFT-14441 is a potent and selective BRD9 BiDAC degrader with DC50 of 39 nM (2h), high selectivity over BRD4 abd BRD7.CFT-14441 efficiently degrades endogenous BRD9 in the Yamato-SS synovial sarcoma cell line, results in growth inhibition of BAF-perturbed HSSYII synovial sarcoma cells but not BAF-wild type SW982 soft tissue sarcoma cells.CFT-14441 demonstrates efficacy in both cell-derived and patient-derived models of synovial sarcoma (IV or IP dosing).

CFT-8634 (CFT8634) is a potent, selective, orally bioavailable BRD9 BiDAC degrader with DC50 of 3 nM, high selectivity over BRD4 abd BRD7.Unlike BRD9 inhibition, BRD9 degradation is efficacious in preclinical models of synovial sarcoma and CFT8634 is ongoing for the treatment of SMARCB1-perturbed cancers.

CG428 (CG-428) is a first-in-class potent and selective TRK degrader (PROTAC) with DC50 of 0.36 nM.CG428 (CG-428) showed selectivity for the degradation of endogenous TPM3-TRKA over ectopically expressed ATP/GTP binding protein-like 4 (AGBL4)-TRKB or ETS variant transcription factor 6 (ETV6)-TRKC fusion proteins in KM12 cells.CG428 exhibited higher potency for inhibiting growth of KM12 cells with IC50 of 2.9 nM, compared with the parental TRK kinase inhibitor.CG428 (CG-428) is a valuable chemical tool compound for investigating the in vivo function of TRK fusion during tumorigenesis

CS640 (CS-640) is a potent, selective CaMK1D inhibitor with nanomolar range at both the enzymatic and cellular levels.CS640 prevent Aβ induced tau hyperphosphorylation in culture, but were not able to protect cells from Aβ induced toxicity.CS640 was able to ablate Aβ induced increased tau phosphorylation at Thr181 in mouse primary neurons.

CU7218 is a small-molecule inhibitor of 14-3-3 protein, inhibits the interaction between 9J10 and 14-3-3, displaces FOXO3a and other substrate proteins from 14-3-3 and reproduces the cellular phenotypes induced by 9J10 expression.

dBRD9 dihydrochloride is a potent and selective degrader (PROTAC) of BRD9 with IC50 of 56.6 nM in MOLM-13 cells.dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide.dBRD9 does not degrade BRD4 or BRD7 at concentrations up to 5 uM.dBRD9 exhibits antiproliferative effects in human AML cell lines.

dBRD9‐A is a chemical degrader (PROTAC) of BRD9, a highly specific binder of the BRD9 bromodomain and elicits near complete BRD9 degradation at low nanomolar concentrations.dBRD9‐A blocks synovial sarcoma tumour progression and oncogenic transcription.dBRD9‐A limited IFN‐induced expression of certain ISGs in multiple cell types, significantly reduced induction of 29 ISGs, including many ISGs known to harbor antiviral activity against the viruses, such as MX1, MX2, IFITM1, IFITM3, IDO1, and BST2.

DDC-01-163 is an allosteric EGFR degrader that selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected; DDC-01-163 exhibited an acceptable biochemical potency with an IC50 value of 45 nM against EGFR L858R/T790M. DDC-01-163 is also effective against osimertinib-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations. The anti-proliferative activity of DDC-01-163 against L858R/T790M EGFR-Ba/F3 cells is enhanced when combined with an ATP-site EGFR inhibitor, Osimertinib.

DGY-09-192 is a bivalent degrader (PROTAC) that couples the pan-FGFR inhibitor BGJ398 to a CRL2VHL E3 ligase recruiting ligand,preferentially induces FGFR1/2 degradation while largely sparing FGFR3/4.DGY-09-192 exhibited two-digit nanomolar DC50s for both wildtype FGFR2 and several FGFR2-fusions, resulting in degradation-dependent antiproliferative activity in representative gastric cancer and cholangiocarcinoma cells (IC50=1 nM).DGY-09-192 induced degradation of a clinically relevant FGFR2 fusion protein in xenograft model.

Endosidin 9 (ES9) is a novel mitochondrial uncoupler, and a potent inhibitor of clathrin-mediated endocytosis (CME) in different systems, strongly reduces FM4-64 uptake in Arabidopsis root cells with IC50 of 5 uM.Endosidin 9 (ES9) inhibits CME dynamics and organelle movement in the cytoplasm.Endosidin9 (ES9) inhibits clathrin-mediated endocytosis largely through cytoplasmic acidification.

FGIN-1-27 is an anxiolytic compound that acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO).FGIN-1-27 inhibited Th17 cell differentiation, significantly downregulated the expression of RORγt target genes, notably Il17a, Il17f, Il23r, Ltb4r1,Ccr6.FGIN-1-27 protected mice against EAE, induced amino acid starvation response (AAR), FGIN-1-27 produced anti-anxiety and anti-panic effects in non-mammalian models.

GRK6 inhibitor 18 is a potent, and selective GRK6 inhibitor with IC50 of 8 nM.GRK6 inhibitor 18 displays >1,000-fold selectivity over Aurora A, as well as high selectivity against a panel of 85 kinases.GRK6 inhibitor 18 has potent cellular target engagement and antiproliferative activity against MM cells (IC50=0.4-0.46 uM) and is synergistic with bortezomib.

GS-680 (GS680) is a novel selective and ATP-competitive CaMKII inhibitor with biochemical IC50 of 2.3 and 15.9 nM against CaMKIIδ and CaMKIIα, respectively.GS-680 inhibited phospholamban phosphorylation in NRVM with an EC50 of 98.9 nM.GS-680 inhibits premature atrial contractions.GS-680 significantly reduced CaMKII autophosphorylation.GS-680 inhibits pro-arrhythmic activity in human atrium and improves contractility in failing human ventricle.

HDAC6 Degrader 13f (YZ268) is a selective HDAC6 degrader (PROTAC) with high potency, specific chemical probe to knock-down HDAC6.

HDAC8 PROTAC 1 is a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8).HDAC8 PROTAC 1 induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.

HTT-D3 is a potent, CNS-penetrant, orally bioavailable huntingtin (HTT) splicing modulator, affects HTT pre-mRNA splicing and reduces HTT expression with IC50 of 8 nM.Oral administration of HTT-D3 resulted in dose-dependent and approximately equivalent mHTT protein lowering in both brain and peripheral tissues in mouse models carrying human mHTT transgene, BACHD and Hu97/18.HTT-D3 (10 mg/kg) reduced mHTT mRNA and protein levels in BACHD brain in BACHD mice.

HuR inhibitor KH-3 is a small molecule, selective inhibitior of HuR function with Ki of 0.83 and 0.72 uM in FP and AlphaLISA assays, respectively.KH-3 potently inhibits breast cancer cell growth in vitro and in vivo.KH-3 inhibits breast cancer cell invasion in vitro as well as delays initiation of lung colonies and improves mouse survival in an experimental metastasis model in vivo.KH-3 suppresses breast cancer cell invasion by disrupting HuR-FOXQ1 mRNA interaction.Inhibition of HuR with KH-3 yielded a significant reduced in the progression of pathological cardiac hypertrophy in a transverse aortic constriction model.

K-312 is a novel cholesteryl ester transfer protein (CETP) inhibitor with IC50 of 60 nM, also suppresses hepatocyte expression of PCSK9, raises HDL and lowers LDL cholesterol levels in vivo; raises HDL cholesterol, decreases LDL cholesterol, and attenuates aortic atherosclerosis in cholesterol-fed rabbits; decreases PCSK9 expression in human primary hepatocytes and in the human hepatoma cell line HepG2, decreases the occupancy of SREBP-1 and SREBP-2 on the sterol regulatory element of the PCSK9 promoter.