cytotoxity (targeted to DNA topoisomerase II); anti-cancer activity; fungicides;

useful for the treatment of cystic fibrosis; modulating CFTR activity; altering the lifespan of a eukaryotic organism;

activate TLR8-dependent NF-kB signaling

IGF-1R/SRC inhibitor

GSK-3b inhibitors; GSK-3b inhibitors;

CB2R PAM is an orally active cannabinoid type-2 receptors (CB2Rs) positive allosteric modulator. CB2R PAM displays antinociceptive activity in vivo in an experimental mouse model of neuropathic pain.

Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.

Antibacterial agent 125 is an antibacterial agent. Antibacterial agent 125 has a potent antimicrobial activity against clinically relevant Gram-positive pathogens with MIC50 values range from 0.25 - 8 μM. Antibacterial agent 125 can be used for the research of antimicrobial resistance.

OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells. OTS514 hydrochloride induces cell cycle arrest and apoptosis.

Martinostat (hydrochloride) is a inhibitor of HDAC that can be labeled with radionuclides for diagnostic applications.

Martinostat is a histone deacetylase imaging agent.

STM2120 is a METTL3-METTL14 inhibitor with an IC50 of 64.5 μM.

ML 315 hydrochloride is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. ML 315 is used in cancer and neurological disease research.

KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects.

ANO61 is a dibenzyl formamide derivative, which exhibits an antiplatelet efficacy through modulation of thrombin-induced Ca2+ response with an IC50 of 47.7 μM.

BD1063 is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine. In other animal studies, BD1063 blocks the effects of MDMA, and reduces alcohol intake in rodent models of alcoholism.

GW549390X is a dual inhibitor of Fluc and VEGFR2 with IC50 of 0.26 μM and 1.2 μM, respectively. GW549390X can bind to the ATP pocket of FLuc through the aniline side chain and is an ATP-competitive inhibitor of Fluc. GW549390X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases, with potential implications for Fluc reporter assays.

N-Desmethyl-U-47700 is the primary metabolite of U-47700 (an opioid agonist).

CZL80, a brain-penetrable caspase-1 inhibitor with an IC50 of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility.

P2X4 antagonist-1 (Compound 24) is an antagonist for P2X4 with IC50 of 15 nM.

N-Benzyl-6-chloropyrimidin-4-amine is a pyrimidine derivative.

Antiviral agent 52 (Compound 30) is a Chlorcyclizine (HY-112067) derivative that exhibits antiviral activity against hepatitic C virus (HCV) with an EC50 of 17 nM. Antiviral agent 52 reveals cytotoxicity in cell Huh7.5.1 with CC50 of 21.3 μM.

(E/Z)-MCB-613 is a pan-Steroid Receptor Coactivator (SRC) stimulator. (E/Z)-MCB-613 overstimulates SRC activity in cancer cells resulting in excessive generation of reactive oxygen species (ROS), leading to cell stress and death by a process called paraptosis. (E/Z)-MCB-613 is a cytotoxic molecule that plays an important role in cancer.

CAY10464 (AHR antagonist 7; compound 4j) is a selective and high-affinity aryl hydrocarbon receptor (AhR) antagonist with a Ki of 1.4 nM.

11β-HSD2-IN-2 (compound 3) is a selective inhibitor for 17β-hydroxysteroid dehydrogenase type 2 (17β-HSD2) with an IC50 of 300 nM.

HDL-16 is a potent P2Y14R antagonist with an IC50 of 0.3095 nM. HDL-16 ameliorates DSS (HY-116282C)-induced colitis through suppressing necroptosis of intestinal epithelium cells (IECs) and protecting mucosal barrier function.

Scarlet 808 (Bronze Red; Shanghai Bronze Red) is a naphthol red pigment. Scarlet 808 can be used for coloring coatings, leather, and latex paints. It has the advantages of high tinting power, good hiding power, alkali resistance, and acid resistance.

Epstein-Barr virus (EBV) lytic cycle inducer-1 Dp44mT (compound C7) is an iron-chelatoe-like compound. Dp44mT cooperates with HDAC inhibitor Romidespin (HY-15149) and SAHA to induce EBV lytic cycle. Dp44mT reactivates EBV lytic cycle by activating the ERK1/2-autophagy axis in epithelial cancers.

LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells.

NorA-IN-1 (Compound 16) is a NorA inhibitor. NorA-IN-1 inhibits NorA efflux pump in everted membrane vesicles. NorA-IN-1 can be used for research of multidrug resistance.

Methyl 3,4-dimethoxycinnamate is an inhibitor of uredospore germination. Methyl 3,4-dimethoxycinnamate also inhibits global DNA methylation in in Hep3B cells.

Methyl 3,4,5-trimethoxycinnamate (Compound III) is a natural compound with hydroxyl radical-scavenging effects.

RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression.

hRIO2 kinase ligand-1 (com 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM.

(E)-Benzyl ferulate is a phenolic ester that can be isolated from Thai propolis.

H1L1A1B3 is an ionizable lipid which demonstrates a fourfold increase in circRNA transfection efficiency in lung cancer cells over ALC-0315. H1L1A1B31 is capable of proactively stimulating innate immune activation upon injection.

Sirtuin-1 inhibitor 1 (Compound 8) is an inhibitor of Sirtuin-1 that plays important roles in obesity-induced diabetes and aging-related diseases.

Acid Red 4 is an azo dye. The wavelength of maximum absorbance for Acid Red 4 is 508 nm.

UCCF-853 is a CFTR modulator.

CCR-11 is an antibacterial agent. CCR-11 can inhibit the proliferation of B. subtilis cells with an IC50 value of 1.2 μM. CCR-11 inhibits HeLa cell proliferation with an IC50 value of 18.1 μM. CCR-11 inhibits bacterial cytokinesis by inhibiting FtsZ assembly. CCR-11 can be used for the research of FtsZ-targeted antibacterial agents.

mAChR antagonist 1 (compound 4a) is a mAChR antagonist with Ki values of 255 nM, 121 nM, 158 nM, and 255 nM for M1, M3, M4, and M5 subtype, respectively.

A3373, a novel chemical inhibitor of Phospholipase D1 (PLD1) and PLD2, with IC50 of 325 nM and 15.15?μM, respectively, inhibits LPS-induced immune response and plays important roles in autoimmune arthritis, bone demineralization and osteoclastogenesis.

MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease.

STING-IN-7 (compound 21) is a potent STING inhibitor with an IC50 of 11.5 nM. STING-IN-7 inhibits the phosphorylation of STING and interferon regulatory factor 3 (IRF3).

PP5-IN-1 (Compound P053) is a competitive inhibitor of Serine/threonine protein phosphatase-5 (PP5) that binds to its catalytic domain and causes apoptosis in renal cancer.

TNKS-2-IN-2 is a potent and selective inhibitor of TNKS2 with an IC50 of 22 nM.

RORγ inverse agonist 1 is the inverse agonist of RORγ.

sulfo-SPDB-DM4 is a agent-linker conjugate for ADC by using the maytansinebased payload (DM4, an antitubulin agent) via the sulfo-SPDB linker.

WAY-232897 is an active molecule for the study of amyloid diseases and synucleinopathies.

WAY-639418 is an active molecule for the study of amyloid diseases and synucleinopathies.

WAY-312858 is an active molecule for the study of amyloid diseases and synucleinopathies.

N-(2-Hydroxyphenyl)picolinamide is an active molecule.

WAY-658674 is an active molecule for the study of amyloid diseases and synucleinopathies.

WAY-323756 is an active molecule for research into amyloid diseases and synucleinopathies.

WAY-309236 is an active molecule for the study of amyloid diseases and synucleinopathies.

N-Cyclopropyl-4-iodobenzamide is an active molecule.

WAY-620147 (compound 6) is an N-(2-morpholinoethyl)nicotinamide derivative that inhibits monoamine oxidase (Monoamine Oxidase). WAY-620147 inhibits MAO-A and MAO-B with IC50s of 26 μM and 55 μM, respectively.

WAY-637940 is an active molecule.

WAY-604603 is an active molecule.

WAY-621924 is an active molecule.

WAY-354574 is an active molecule targeting deacetylase (Sirtuin) for the study of Huntington's disease (HD).

WAY-608106 is an active molecule.

Topoisomerase I inhibitor 9 (compound 3d) is a leishmanial topoisomerase IB inhibitor. Topoisomerase I inhibitor 9 has antileishmanial activity against L. donovani promastigotes, with the IC50 of 34.81μM.

WAY-658675 is an active molecule.

WAY-659873 is an active molecule.

WAY-660222 is an active molecule.

WAY-324572 is an active molecule.

WAY-639228-A is an active molecule.

WAY-620521 is an active molecule.

WAY-607695 is an active molecule.

Nurr1 agonist 7 (compound 110) is a Nurr1 agonist with an EC50 value of 0.12 μM.

Nurr1 agonist 8 (compound 111) is a Nurr1 agonist with an EC50 value of 0.09 μM.

WAY-221060-A is an active molecule.

Anti-inflammatory agent 63 is an anti-inflammatory agent that shows optimal inhibitory activity (EC50 = 5.33±0.57 μM) against the production of nitric oxide (NO) induced by lipopolysaccharide (LPS) in RAW264.7 cells.

WAY-639872 is an active molecule.

WAY-215718 is an active molecule.

WAY-328127 is an active molecule.

WAY-616296 is an active molecule.

WAY-325811 is an active molecule.

WAY-649123 is an active molecule.

Tyrosinase-IN-17 (Compound 5b) is a lipophilic, skin-permeable, and non-cytotoxic Tyrosinase inhibitor (pIC50=4.99). Tyrosinase-IN-17 can be used for research on melanin-related diseases, such as melanoma, melanogenesis, etc.

Aβ42 agonist-1 (compound 7a) is a small molecule compound that can promote Aβ42 aggregation. Aβ42 agonist-1 can interact with Aβ42 oligomers and pentamers to promote nontoxic aggregate self-assembly and rapid fibril formation. Aβ42 agonist-1 prevents Aβ42-induced cytotoxicity in HT22 hippocampal neuronal cells.

Aurora kinase inhibitor-11 (compound 25) is an inhibitor of Aurora Kinase with an IC50 of 0.14 μM. Aurora kinase inhibitor-11 has anticancer activity.

Aβ42 agonist-2 (compound 7b) is a small molecule compound that can promote Aβ42 aggregation. Aβ42 agonist-2 can interact with Aβ42 oligomers and pentamers to promote nontoxic aggregate self-assembly and rapid fibril formation. Aβ42 agonist-2 prevents Aβ42-induced cytotoxicity in HT22 hippocampal neuronal cells.

ATG12-ATG3 inhibitor 1 (compound 189) is a potent inhibitor of autophage.

hCAI/II-IN-7 (compound 1F) is a potent carbonic anhydrase (CA) inhibitor with Ki values of 23 nM, 44 nM and 20.57 µM for hCA-I, hCA-II and bovine CA, respectively.

HDAC6-IN-27 (compound 8C) is a HDAC inhibitor with IC50 vales of 15.9 nM 136.5 nM and 6180.2 nM for HDAC6, HDAC8 and HDAC1, respectively. HDAC6-IN-27 shows potent antiparasitic effects.

AN-12-H5 intermediate-3 is an intermediate of the viral inhibitor AN-12-H5 (HY-120900) and can be used to synthesize Antibody-Drug Conjugates (ADCs).

Anti-osteoporosis agent-6 (compound 174) is an anti-osteoporosis agent. Anti-osteoporosis agent-6 has 14.11% inhibition rate against osteoclast formation at 10 μM.

Anti-osteoporosis agent-5 (compound 189) is a potent inhibitor of the formation of osteoclasts.

4,2′,4′,6′-Tetramethoxychalcone is a flavonoids that can be isolated from Gnaphalium affine.

Senexin A hydrochloride is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A hydrochloride inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.

TEAD-IN-8 is a novel TEAD inhibitor, which potently and specifically inhibits TEAD-YAP transcriptional activities. TM2, alone or in combination with MEK inhibitors, exhibits potent antiproliferative effects in YAP-dependent cancer cells.

Antioxidant/anticancer agent 1 (compound 5) is a pyrimidine-derivatized Schiff base based on pyrimidine hydroxy-1-naphthaldehyde and has antibacterial, antioxidant, antifungal, and anticancer properties. Antioxidant/anticancer agent 1.

HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection.

ATPase-IN-3 (compound 6) is a ATPase inhibitor. ATPase-IN-3 has Gastroprotective effect in ethanol-induced gastric ulcers by contribution of anti-apoptotic (BCL-2) and tumor suppressor (P53) proteins.

CAY10512 is an inhibitor of NF-κB. CAY10512 can suppress the upregulation of NF-κB-sensitive proinflammatory miRNAs (miRNA-9, miRNA-125b, miRNA-146a, miRNA-155) in cerebrospinal fluid and extracellular fluid, and can be used for research on Alzheimer's disease.

ZINC000028464438 is a selective HDAC11 inhibitor with an IC50 of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes.

AChE/Aβ-IN-5 (compound AV-2) is a bifunctional inhibitor that targets AChE and auto-induced Aβ (Amyloid-β) aggregation. AChE/Aβ-IN-5 can significantly improve scopolamine- and Aβ-induced cognitive impairment in mice.

BFC1108 is a small molecule Bcl-2 functional converter. BFC1108 induces a conformational change in Bcl-2, resulting in the exposure of its BH3 domain both in vitro and in vivo. BFC1108 effectively induces apoptosis in Bcl-2 expressing cancers.

p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor.

Avenanthramide-C methyl ester is an anti-inflammatory agent and NF-κB inhibitor that inhibits the secretion of pro-inflammatory factors. Avenanthramide-C methyl ester inhibits NF-κB activation by inhibiting IKK and IκB phosphorylation and inhibiting proteasome activity.

GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo.

CSF1R-IN-20 (compound 7a) is a CSF-1R Inhibitor with an IC50 value of 467 nM. CSF1R-IN-20 inhibits CSF-1R auto-phosphorylation.

Nav1.8-IN-8 (Compound A11) is a Nav1.8 channel inhibitor. Nav1.8-IN-8 may prevent associated diseases mediated by sodium ion channels (NaV).

PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.

URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare 11C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH.

Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research.

4-Methyl-4-(pyridin-2-yldisulfanyl)pentanoic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Moclobemide N-Oxide (Ro 12-5637) is N-oxide metabolite of Moclobemide. Moclobemide N-Oxide retains certain MAO-A (monoamine oxidase) inhibitory activity, but is generally present in low concentrations. Moclobemide N-Oxide can be detected by UV absorption at 240 nm.

EGFR-IN-80 (compound 30) is an EGFR inhibitor with a pIC50 of 10.6.

c-Kit-IN-3 (Compound 18) is a potent and selective c-KIT kinase inhibitor with an IC50s of 4 nM, 8 nM for c-KIT wt and c-KIT T670I, respectively. c-Kit-IN-3 displays great potencies against most of the gain-offunction mutations in the juxtamembrane domain, drugresistant mutations in the ATP binding pocket, and activation loops.

NS1652 is a reversible anion conductance inhibitor, blocks chloride channel, with an IC50 of 1.6 μM in human and mouse red blood cells.

CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011).

Firefly luciferase-IN-1 (compound 48) is a highly potent and reversible inhibitor of firefly luciferase with an IC50 value of 0.25 nM.

Antituberculosis agent-5 (compound 52) is a nitrofuranylamide derivative, inhibits M. tuberculosis UDP-Gal mutase. Antituberculosis agent-5 inhibits Glf activity with an IC50 value of 99 μM/mL and resists tuberculosis (TB) with a MIC value of 1.6 μg/mL.

Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.

TASK-1-IN-1 is a potent and selective TASK-1 (Potassium Channel) inhibitor with an IC50 of 148 nM. TASK-1-IN-1 shows a reduced inhibition of TASK-3 channels (IC50 of 1750 nM) and not a significant effect on other K+ channels. TASK-1-IN-1 has anticancer effects.

NDH-1 inhibitor-1 (compound 27) is a potent NDH-1 inhibitor with pI50 values of <4, 5.40, 6.15 µM for Bovine SMP (submitochondrial particles), Potato SMP and E. coli, respectively.

Antimalarial agent 17 is an antimalarial agent, also acts as a herbicide. Antimalarial agent 17 is photosystem II inhibitor, shows post-emergence herbicidal activity equal to commercial herbicides.

Antimicrobial agent-14, a benzyl thiophene sulfonamide derivative is an antimicrobial agent, with a MIC of 200 μM against Campylobacter coli ATCC33559. Antimicrobial agent-14 can be used for the research of bacterial foodborne gastroenteritis.

Anti-Influenza agent 4 is a potent and selective influenza virus inhibitor with EC50s of 150 nM and 62 nM for strains A/Roma and A/Parma, respectively.

Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitory activity against T. b. brucei, with an IC50 of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research.

Neuropeptide Y5 receptor ligand-1 (compound 54), a carbazole derivative, is a potent neuropeptide Y5 (NPY-5) receptor antagonist.

Anti-Trypanosoma cruzi agent-4 (compound 5c) is an inhibitor of Trypanosoma cruzi. Anti-Trypanosoma cruzi agent-4 can be used for the research of infection.

SPD-473 citrate is a serotonin/dopamine/norepinephrine reuptake inhibitior.

AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.

Teriparatide Free Base can treat osteoporosis in men and in women who have gone through menopause.

Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake.

FOXO4-DRI is a cell-permeable peptide antagonist that blocks the interaction of FOXO4 and p53. FOXO4-DRI is a senolytic peptide that induces apoptosis of senescent cells.

Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research.

G-5758 is a potent, selective, and orally available IRE1α inhibitor with IC50 of 38 nM in XBP1s reporter assay. G-5758 demonstrates a robust PD response in the KMS-11 tumor xenograft model.

PFI-7 is a potent, selective and cell-active chemical probe that antagonizes Pro/N-degron binding to human GID4 with Kd of 79 nM. PFI-7 will be a valuable research tool for investigating CTLH complex biology and facilitating development of targeted protein degradation strategies that highjack CTLH E3 ligase activity.

GLP-1-MK-801 is a GLP-1-directed NMDA receptor antagonist for targeting to achieve cell-specifc ionotropic receptor modulation and highlights the therapeutic potential of unimolecular mixed GLP-1 receptor agonism and NMDA receptor antagonism.

Jun12682 is a SARS-CoV-2 papain-like protease (PLpro) inhibitor with Ki of 37.7 nM and displays EC50 of 1.1 μM in the FlipGFP PLpro assay, more than 20-fold improved from GRL0617 (EC50=22.4 μM).

O12-D3-I3 is an imidazole-based lipid for siRNA delivery. O12-D3-I3-LNPs encapsulating FVII siRNA (FVII@O-LNP) elicites greater gene silencing than those with the DLin-MC3-DMA (MC3) due to its stronger endosomal escape.

CDD-2807 is a potent serine/threonine kinase 33 (STK33) inhibitor with Kd of 0.02 nM and IC50 of 9.2 nM, respectively. CDD-2807 shows >9-fold selectivity versus other kinases and demonstrates excellent metabolic stability with T1/2 >60 min in MLM and HLM.

Lipid 119-23 is an ionizable lipid for mRNA delivery. 119-23 LNP exhibits an enhanced capability to express functional mCre in several categories of immune cells, spanning the liver, spleen and lung.

KL-50 is a selective toxin toward tumors that lack the DNA repair protein O6-methylguanine-DNA-methyltransferase (MGMT), which reverses the formation of O6-alkylguanine lesions. KL-50 is the first reported compound to overcome acquired temozolomide resistance while maintaining high selectivity for MGMT-cells.

SL-25.1188 is a monoamine oxidase B (MAO-B) inhibitor potentially for treatment of Alzheimer's dementia and smoking cessation. SL-25.1188 is characterized in vivo by reversible binding, high brain uptake, and very slow plasma metabolism.

TLR7/8 agonist 1 is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.

FAP-IN-2 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor, that can be used for tumor imaging.

SL25.1188 precursor is the precursor of SL25.1188.

NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality.

FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios.

HYINC-FAPI-4 is a derivative of 99mTc-labeled isonitrile-containing fibroblast activation protein (FAPI) inhibitor, that can be used for tumor imaging.

3BP-3940 is a highly potent fibroblast activation protein (FAP)-targeting peptide for theranostics. 3BP-3940 is often coupled with radionuclides for tumor diagnosis and treatment.

Pentanedioate is a starting material for the synthesis of specific PSMAM inhibitors.

NOTA-octreotide is a ligand for making [18F]AlF-NOTA-octreotide, which is a PET/CT imaging agent for somatostatin receptor imaging in neuroendocrine tumor patients

DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging.

KN-93 phosphate is a novel membrane-permeant synthetic inhibitor of purified neuronal CaMK-II, with Ki of 370 nM.

altering the lifespan of a eukaryotic organism

Androgen Receptor modulator

XL413 is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.

CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies.

MCLA hydrochloride is a chemiluminescent reagent which can be used to quantify aqueous concentrations of superoxide.

GSK-3β inhibitor 12 (compound 15) is an inhibitor of GSK-3β. GSK-3β inhibitor 12 inhibits 49.11% and 37.11% activity of 25 μM and 50 μM GSK-3β, respectively. GSK-3β inhibitor 12 can be used for the research of neurodegenerative diseases.

CLK1-IN-4 (Compound 79) is an inhibitor for CDC like kinase 1 (CLK-1) with IC50 of 1.5-2 μM.

CB1 agonist 1 (compound 22) is an agonist of CB1. CB1 agonist 1 shows affinity to CB1 receptor with an pIC50 value of 5.7. CB1 agonist 1 can be used for the research of brain disorders.

CK2-IN-4 (compound 5) is a protein kinase (CK2) inhibitor (IC50=8.6 µM). CK2-IN-4 has good potential for research in the areas of cancer, viral infections and glomerulonephritis.

Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively.

JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity.

Casein kinase 1δ-IN-14 (compound 481) is a casein kinase inhibitor that can be used to study neurodegenerative diseases such as Alzheimer's disease.

ROS kinases-IN-2 is a ROS kinase inhibitor with 21.53% inhibition at 10 μM.

HIF-PHD-IN-3 (compound 4) is a potent hiPSC-CM cardioprotective scaffold. HIF-PHD-IN-3 can induce upregulation of heme oxygenase-1.

OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .

N-Acetylcysteine amide is a cell membranes and blood brain barrier permeant thiol antioxidant and neuroprotective agent, reduces ROS production.

Cevidoplenib (SKI-O-703) is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. Cevidoplenib is also the mesylate form of SKI-O-592. Cevidoplenib and SKI-O-592 inhibits BCR-mediated survival, proliferation, and differentiation of B cells. And SKI-O-592 potently inhibits multiple kinases with IC50s of 6.2 nM (Syk), 1.859 μM (Jak2), 5.807 μM (Jak3), 0.412 μM (RET), 0.687 μM (KOR), 1.783 μM (FLT3), 16.96 μM (FGFR1), 5.662 μM (FGFR3), and 0.709 μM (Pyk2), respectively.