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.

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.

AP22161 is a potent and selective Src SH2 domain inhibitor with an IC50 of 0.24 µM. AP22161 exhibits >120-fold selectivity over Yes SH2 (IC50 = 29.38 µM) and ZAP SH2 (IC50 = 421.86 µM). AP22161 inhibits Src-dependent cellular activity and diminishes osteoclast resorptive activity. AP22161 can be used for osteoporosis research.

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.

Anti-Trypanosoma cruzi agent-9 is a topoisomerase II inhibitor. Anti-Trypanosoma cruzi agent-9 inhibits the growth of Trypanosoma cruzi and Leishmania donovani.

anti-TNBC agent-13, a NO donor-Aurovertin B conjugate, is a ferroptosis inducer. anti-TNBC agent-13 inhibits GPX4 activity and leads to triple-negative breast cancer (TNBC) cell death. anti-TNBC agent-13 can be used for the research of triple-negative breast cancer.

Antiproliferative agent-76 (Compound II-2) is an 8-sulfonamidoquinoline derivative and a selective anticancer agent. Antiproliferative agent-76 blocks the NF-κB and WNT signaling pathways. Antiproliferative agent-76 promotes cancer cell Apoptosis. Antiproliferative agent-76 exhibits anticancer activity against colorectal cancer and leukemia.

Antiproliferative agent-75, Pyrrole derivative, is an antiproliferative agent with an IC50 value of 0.06 μM against Myc-driven human B-cells. Antiproliferative agent-75 can be used for the development of pyrrole-based Myc inhibitor.

Antiproliferative agent-74 (Compound 19a) is an anti-proliferative agent. Antiproliferative agent-74 suppresses Twist1 expression, induces weak Apoptosis. Antiproliferative agent-74 displays anti-proliferative activity against non-small cell lung cancer cells.