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.

BP Lipid 222 BP Lipid 222 is an butanolamine ionizable lipid with both ester bonds located adjacent to C8 relative to the amine head. The introduction of ester linkages can improve the clearance of the lipid in the liver. This compound is analgous to ALC-0315 (BP-25498). The lipid can be used for mRNA-based therapies which depends on the availability of a safe and efficient delivery vehicle. Reagent grade, for research purpose. Please contact us for GMP-grade inquiries.

BP Lipid 211 is an ethanolamine ionizable lipid with 9 carbon of primary-ester lipid tail. The ethanolamine head helps with mRNA encapsulation. Both ester bonds are located at C10 position relative to the amine nitrogen. The introduction of ester linkages can improve the clearance of the lipid in the liver. Reagent grade, for research purpose.

1LNP Lipid-7 (Compound 7013) is a lipid. LNP Lipid-6 can be used to prepare lipid nanoparticles (LNP) and for drug delivery.

BP Lipid 309 is an ionizable lipid analogue of ALC-0315 featuring a tertiary amine head, a central tertiary amine, and two identical esters linking to nonpolar tails. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 307 is a multi-ionizable amino-lipid featuring a dimethylamine headgroup, a central tertiary amine, and two identical ester branches linking to saturated C17 tails. This compound may be employed in the development of lipid nanoparticles for drug delivery.

BP Lipid 318 is a lipid analog comprised of three unsaturated fatty acid tails and an ionizable dimethylamino butanoate head group. This lipid may be used in the generation of lipid nanoparticles (LNPs) for mRNA delivery.

BP Lipid 316 is an ionizable lipid analogue of DLin-MC3-DMA featuring a 4-(dimethylamino)butanoate head, two linoleic acid tails, and one primary alcohol. The alcohol may be used to further derivatize this compound. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 317 is an amino lipid featuring a dimethylamine headgroup connected to two oleic esters and a hydroxy group which may be used for further derivatization. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 320 is an ionizable amino lipid comprised of three oleic fatty acid tails and a novel pyrrolidine head group four carbon atoms in length. This lipid may be used in the generation of lipid nanoparticles (LNPs) for mRNA delivery.

BP Lipid 315 is a cationic ionizable lipid ALC-0315 analogue featuring a Boc-protected primary amine, a central tertiary amine, and two ester tails located at the C8 position relative to the amine. One of these esters features a symmetrical branched C17 tail, while the other is an asymmetric C11 tail. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 319 is a multi-ionizable amino lipid analogue of ALC-0315 featuring a propylamino headgroup and two acyl tails, one being a branched symmetrical C17 and the other being an asymmnetrical C11 chain. Ionizable lipids such as this may be applied in the development of lipid nanoparticles.

BP Lipid 312 is a cationic ionizable lipid analogue of LP01, with the substitution of a polyunsaturated tail for a monounsaturated equivalent. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 311 is a branched amino lipid featuring a dimethylamino headgroup, esters of a palmitoleic acid group and an aliphatic acetal. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 308 has a terminal tertiary amine group, a linoleic group, and a 4,4-bis(octyloxy)butanoic acid sodium salt tail. This compound can be useful for the building or modification of lipid nanoparticles. Reagent grade, for research use only.

BP Lipid 314 is an ionizable amino lipid featuring a dimethylamino head group, a carbamate linking to a central tertiary carbon with two other branches, a linoleate ester, and an aliphatic acetal ester. A compound like this may be employed in the development of lipid nanoparticles for drug delivery.

BP Lipid 310 is an ionizable aminolipid analog of CL1. The structure features an ethanolamine head and an ester linking to a polyunsaturated hydrophobic tail. This lipid may be used to encapsulate nucleic acids or small-molecule drugs to form lipid nanoparticles for drug discovery.

BP Lipid 323 is an ionizable aminolipid analog of CL1 which features a unique azetidine head and an ester linking to a polyunsaturated hydrophobic tail. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 321 is an ionizable aminolipid analog of CL1 which features a unique 3-hydroxyazetidine head and an ester linking to a polyunsaturated hydrophobic tail. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

BP Lipid 322 is a multichargeable lipid analog of CL1 which features a novel 2-hydroxyethyl piperazine ionizable head and an ester linking to a polyunsaturated hydrophobic tail. Ionizable lipids such as this may be applied in the development of lipid nanoparticles for drug discovery.

Al-28 is a multi-ionizable aminolipid featuring a central amine and three identical disulfide-linked saturated side chains. The hydrophobic side chains are linked to the central structure by ester as well as disulfide bonds. Disulfide bonds are readily cleaved in the reducing environment of the cell cytoplasm. Ionizable lipids are typically used in the design of nucleic acid lipid nanoparticles, as their pH-dependent positive charge stabilizes the anionic nucleic acids they encapsulate.

9A1P9 is a multi-tail ionizable cationic phospholipid. 9A1P9 induces membrane destabilization. 9A1P9 can be used for CRISPR-Cas9 gene editing in mice.

ALC-0315 analogue-1 (compound P-10) is a cationic lipid. ALC-0315 analogue-1 is the raw material for synthesis of cationic liposome.

BLU-451, also known as LNG-451, orally bioavailable, central nervous system (CNS) penetrating, mutant-selective covalent inhibitor of epidermal growth factor receptor (EGFR) exon 20 insertion (Ex20ins) activating mutations, with potential antineoplastic activity. Upon oral administration, EGFR Ex20ins inhibitor BLU-451 selectively targets, irreversibly binds to and inhibits the activity of EGFR Ex20ins and some other oncogenic point mutations. This prevents EGFR Ex20ins-mediated signaling. This may induce cell death and inhibit tumor growth in EGFR Ex20ins-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumors, plays a key role in tumor cell proliferation and tumor vascularization. BLU-451 is able to penetrate the blood-brain-barrier (BBB) and may therefore exert its activity against EGFR Ex20ins-driven CNS primary tumors and CNS metastases. BLU-451 does not inhibit the activity of wild-type (WT) EGFR. EGFR Ex20ins are oncogenic driver mutations that constitutively upregulate kinase activity.

VK-2019 is a selective EBNA1 inhibitor. VK-2019 was developed as a highly specific inhibitor of EBNA1 DNA binding activity and is currently in phase 1 development as a treatment for EBV-associated carcinomas. EBNA1 is an Epstein Barr virus (EBV) protein expressed in all EBV-associated cancers. EBNA1 plays a critical role in the replication and maintenance of EBV episomes in latently infected cells.

PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 µM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.

PRMT5 inhibitors; PRMT5 inhibitors;

NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research.

UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2.

AK59-51TB (AK59) is a STING degrader leveraging HERC4, a HECT-domain E3 ligase.

IDE397 is a potent inhibitor of MAT2A, which is developed to selectively exploit this synthetic lethal vulnerability in MTAP−/− tumors.

Compound 32 (HER2) is a potent and selective covalent inhibitor of HER2/WT and HER2/YVMA with IC50 of 49 nM and 42 nM, respectively.

IDOR-1117-2520 is a selective and insurmountable antagonist of CCR6 with IC50 of 20 nM.

Pidobenzone is a dermatologic agent.

Pseudouridine-5’-triphosphate (Pseudo-UTP) is one of the most commonly used modified nucleoside for the polymerase-mediated synthesis of RNA molecules. Compared with uridine-containing unmodified mRNAs, the application of pseudouridine-containing modified mRNAs exhibits better nuclease stability, immunogenicity, and translational properties.

LSN3441732 is a dimeric compound and inhibits the formation of Lipoprotein(a) (Lp(a)) particles in vitro with IC50 of 0.18 nM.

R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.

BIO-8169 is a highly potent, selective, and brain-penetrant IRAK4 inhibitor with IC50 of 0.2 nM. BIO-8169 has an excellent PK profile, reduces the in vivo production of pro-inflammatory cytokines, and is tolerated in toxicity studies in rodents and dogs.

Nelutroctiv (CK-136) is a novel cardiac troponin activator devoid of PDE-3 activity that demonstrates a wider pharmacodynamic window in vivo relative to a representative myosin activator, CK-138.

TAC is a TERT activator compound that upregulates TERT transcription via the MEK/ERK/AP-1 cascade. TAC alleviates neuroinflammation, increases neurotrophic factors, stimulates adult neurogenesis, and preserves cognitive function without evident toxicity, including cancer risk.

GalNAc-L96-tert-butyl ester is a cleavable PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-Tri-(t-butoxycarbonylethoxymethyl)-methane is also a PEG/Alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.