AURKA-IN-4 (compound 13), a capsaicin-derived prohibitin ligand, is an AURKA inhibitor. AURKA-IN-4 acts as a molecular glue within the AURKA/PHB2/LC3 complex. AURKA-IN-4 is specific to the mitochondrial pool of AURKA, and inhibits AURKA-dependent mitophagy. AURKA-IN-4 can be used for cancer research.

ATR-IN-31 is a selective ATR kinase inhibitor with an IC50 of 7 nM. ATR-IN-31 does not significantly inhibit ATM kinase activity. ATR-IN-31 functionally inhibits ATR kinase activity. ATR-IN-31 inhibits viability of prostate cancer cells.ATR-IN-31 can be used for the research of prostate cancer.

ATR ligand 2 (Compound 26) is a ATR PROTAC ligand. ATR ligand 2 can be conjugated with E3 ligase Ligand and linker to synthesize PROTAC ATR degrader-3.

ATP-ArN3 is a UV-activatable ATP-crosslinker analog. ATP-ArN3 relys on UV irradiation to activate the aryl azide (ArN3) crosslinking group and conjugate substrate to kinases and associated proteins.

ATOX1-IN-1 is an inhibitor of ATOX1 (a copper chaperone protein) with a Kd value of 12.5 μM. ATOX1-IN-1 induces intracellular copper accumulation, increases the level of DNA methylation in the NOTCH1 promoter region, and inhibits the NOTCH1/HES1 signaling pathway. ATOX1-IN-1 enhances the sensitivity of hepatocellular carcinoma cells to Cisplatin. ATOX1-IN-1 can be used in hepatocellular carcinoma-related research.

Atiprosine (AY-28228) is an orally effective selective α1-adrenergic receptor antagonist with a pA2 value of 8.11. Atiprosine exhibits antagonistic activity against α2-adrenergic receptors (α1-adrenergic receptor), 5-HT₂ receptors (5-HT₂ receptor), and H₁ receptors (H₁ receptor). The pA2 values for these receptors are 6.04, 6.87, and 7.32 respectively. Atiprosine has antihypertensive and hypotensive effects in rats, dogs, and monkeys. It can be used for research on cardiovascular and mental disorders.

Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a Kd of 0.2199 μM. Atg4B activator-1 binds to the allosteric pocket of ATG4B and induces conformational changes. Atg4B activator-1 induces Autophagy. Atg4B activator-1 inhibits the proliferation and migration of triple-negative breast cancer cells. Atg4B activator-1 can be used in studies related to triple-negative breast cancer.

AT-9 is an anthraquinone-triazene derivative. AT-9 exhibits strong DNA intercalation ability. AT-9 can also interact with Topo IIA. AT-9 exhibits anticancer activity against non-small cell lung cancer and cervical cancer.

AT1R antagonist 4 (Example 26) is an AT1R antagonist. AT1R antagonist 4 shows excellent antagonistic activity against calcium influx in cells stably expressing AT1 receptors and ETA receptors. AT1R antagonist 4 can be used in kidney disease research.

AT-051/43421517 is a cytoprotective agent and apoptosis inhibitor that binds to human phosphoglycerate kinase 1 (hPgk1). AT-051/43421517 protects cells from rotenone-induced cell death without inducing cell proliferation. AT-051/43421517 can be used for the research of parkinson’s disease.

ASS1 activator 1 (Compound 10f) is a ASS1 activator with an EC50 of 1.90 μM. ASS1 activator 1 enhances the activity of ASS1 and promotes AMPK phosphorylation. ASS1 activator 1 induces cell Apoptosis. ASS1 activator 1 exhibits anticancer activity against triple-negative breast cancer, colorectal cancer and liver cancer.

Aspirin Trelamine is a salicylic acid prodrug. Aspirin Trelamine has been used in research related to ischemic stroke, as well as COVID-19-associated acute respiratory distress syndrome (ARDS) and pneumonia.

Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system.

Asocainol hydrochloride (Goe 4704 hydrochloride) is an antiarrhythmic agent. Asocainol hydrochloride reduces the maximum rate of action potential rise and action potential amplitude. Asocainol hydrochloride is applicable for the research of arrhythmias.

ASK1-IN-12 is an ASK1 inhibitor with an IC50 of 6.3 nM. ASK1-IN-12 inhibits TNF-α-induced activation of the ASK1-p38/JNK pathway. ASK1-IN-12 can reduce free fatty acid-induced cholesterol increase, lipid droplet accumulation and improves hepatocellular steatosis. ASK1-IN-12 can be used for the research of non-alcoholic steatohepatitis (NASH).

Asciminib-NH2 is a BCR-ABL ligand and can be used for the synthesis of PROTACs, such as P19As.

Arucadiol is a rosane-type diterpenoid anti-inflammatory agent. 5 μM Arucadiol significantly inhibits LPS-induced TNF-α, IL-1β, and IL-8 production (inhibition rates of 39.8%, 44.4%, and 34.5%, respectively). Arucadiol exerts its anti-inflammatory activity by inhibiting the mRNA and protein expression of inflammatory cytokines and can be used in research on inflammation-related cardiovascular diseases such as atherosclerosis. Arucadiol can be naturally extracted from the roots of Salvia miltiorrhiza var. alba.

Artecanin is a SARS-CoV-2 main protease (Mpro) inhibitor with predicted high gastrointestinal absorption and oral bioavailability, and no predicted hepatotoxicity, carcinogenicity, mutagenicity or cytotoxicity. Artecanin interacts with His41 and Cys145, the key amino acid residues in the active site of Mpro, blocks the cleavage and maturation of viral precursor proteins, and forms a stable complex with Mpro. Artecanin blocks the invasion of SARS-CoV-2. Artecanin is applicable to the research of COVID-19.

Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research.

Aromatase-IN-1 is a competitive aromatase (P450arom) inhibitor with a human IC50 of 40 nM and a Ki of 1.05 nM. Aromatase-IN-1 binds via coordination of imidazole nitrogen to the heme iron of aromatase. Aromatase-IN-1 can be used for the research of breast cancer.

Aristoforin, a hypericin derivative, inhibits the activities of SIRT1 and SIRT2. Aristoforin induces G1 phase cell cycle arrest, scavenges hydroxyl free radicals, and exhibits protective activity against Fe2+-induced DNA breakage. Aristoforin can be used in studies related to breast cancer and colon adenocarcinoma.

ARI-809 (CP-744809) is a highly selective, orally active aldose reductase inhibitor with an IC50 of 1 nM. ARI-809 blocks excessive glucose flux through the polyol pathway. ARI-809 normalizes elevated sorbitol and fructose levels in sciatic nerve tissues of diabetic rat models, inhibits sorbitol accumulation in lens tissues, and brings elevated urinary albumin excretion close to normal. ARI-809 can be used in diabetes research.

Argimesna ethanesulfonate is a uroprotective agent. Argimesna ethanesulfonate is promising for research of hemorrhagic cystitis in cancer chemotherapy.

ARCA (Anti-Reverse cap analog) is a 5′- cap analogue. ARCA caps mRNA. ARCA can be used in protein expression studies.

AR-102 free acid, an active metabolite of AR-102, is a prostaglandin F (PGF) derivative.

AR ligand-48 is an AR (Androgen Receptor) inhibitor and a ligand for the target protein for PROTAC (AR). AR ligand-48 can be used to synthesize PROTAC AR Degrader-12.

AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC).

AQ-13 (Compound 7) is a Chloroquine analogue with anti-breast cancer property. AQ-13 shows antiproliferative activities against MDA-MB231 and MCF7 with GI50 of 27.81 and 17.85 μM. AQ-13 shows low cytotoxicity against non-cancerous breast epithelial cells MCF10A (GI50 = 65.26 μM). AQ-13 can be used for the research of breast cancer.

Apoptosis inducer 60 (Compound 4a) is an Apoptosis inducer. Apoptosis inducer 60 induces concentration-dependent apoptosis in cells. Apoptosis inducer 60 exhibits moderate cytotoxicity against breast cancer cell lines.

Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and Bax/Bcl-2 ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer.