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.

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).

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.

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.

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.

APD-209 is a sialic acid conjugate with a PEG4 polar linker and a PDA non-polar tail. APD-209 aggregates adenovirus type 37 particles, blocks the binding of viral particles to human corneal epithelial cells, and inhibits cellular entry of adenovirus type 37. APD-209 can be used for the research of epidemic keratoconjunctivitis.

AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma.

AP21998 is a Fv (mutant FKBP) domain-selective ligand that binds to a single FKBPv. AP21998 disrupts FKBP-mediated oligomerization, blocks the proliferation of transformed myeloid progenitors and facilitates their terminal myeloid differentiation. AP21998 disrupts aggregates of CAD-hM1 receptor fusion protein, allowing receptors to exit the ER and enter the plasma membrane. AP21998 can be used for cancer research.

Antrafenine (Stakane) dihydrochloride is a non-narcotic analgesic. Antrafenine dihydrochloride demonstrates central analgesic effects in acetic acid writhing test and mouse hot plate test experiments. Antrafenine dihydrochloride significantly alleviates osteoarthritis pain. Antrafenine dihydrochloride exhibits mild anti-inflammatory activity in a rat toe edema model. Antrafenine dihydrochloride can be used for pain and anti-inflammatory research.

Antiviral agent 80 is a conjugate of Zanamivir and Amantadine, acting as a dual inhibitor of influenza virus M2 ion channel/neuraminidase (NA). Antiviral agent 80 exhibits potent inhibitory activity against both wild-type and drug-resistant influenza neuraminidase mutants, with an IC50 value range of 1.50 nM to 120.4 nM. Antiviral agent 80 can be used in influenza-related research.

Antiviral agent 75 (example D26) is a Ebolavirus (EBOV) and Bundibugyo ebolavirus (BDBV) inhibitor with IC50s of 0.11 μM and 0.75 μM, respectively. Antiviral agent 75 can be used for the study of filovirus infection.

Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer.

Antitumor agent-212 is a α-exo-methylene-selenolactone derivative with prominent selective antitumor activity. Antitumor agent-212 exhibits an MIC value of 128 μg/mL against Gram-positive bacteria. Antitumor agent-212 exhibits significant antitumor effects in the U87 human glioma xenograft model. Antitumor agent-212 can be used for the study of glioma, breast cancer and non-small cell lung cancer, and antibacterial study.

Antitumor agent-210 (Compound 1778) is an NK cell activator. Antitumor agent-210 has a weak proliferative effect on NK92 cells, promoting the activation and degranulation of NK cells, and significantly enhancing the cytotoxicity of NK92 cells against tumor cells. Antitumor agent-210 promotes the release of cytokine granzyme B, perforin, and IFN-γ. Antitumor agent-210 reduces the number of lung metastatic lesions in mice and can be used for the study of melanoma lung metastasis.

Antitrypanosomal agent 30 (compound 6b) is a trypanocidal agent with extremely low cytotoxicity against mouse macrophages. Antitrypanosomal agent 30 can be used for the research of Chagas disease.