FK-518 is a potent AmpC β-lactamase inhibitor. FK-518 demonstrates strong antimicrobial activity against P. aeruginosa strains overexpressing AmpC β-lactamase. FK-518 is promising for research of P. aeruginosa infections.

FGFR3-IN-10 is a FGFR3 inhibitor with superior selectivity for FGFR3 over FGFR1.FGFR3-IN-10 can be used for the research of cancer, systemic sclerosis, fibrosis, pulmonary fibrosis, achondroplasia, thanatophoric dysplasia, severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), Muenke syndrome.

Fasobegron is a β3-adrenergic receptor agonist with a human EC50 of 4.8 nM. Fasobegron shows an EC50 of 250 nM for human β1-adrenergic receptors. Fasobegron can be used for the research of overactive bladder.

Exatecan analog 13 is a analog of Exatecan. Exatecan (DX-8951) is a common toxin component in ADC preparation (ADC Cytotoxin) and an inhibitor of DNA topoisomerase I (IC50 = 2.2 μM).

Ethyl 7-aminoheptanoate hydrochloride is a PROTAC linker that can be used in the synthesis of PROTACs.

Eniporide mesylate (EMD 96785 mesylate) is a Na(+)/H(+) exchange (NHE) inhibitor. Eniporide mesylate specifically inhibits the NHE-1 isoform. Eniporide mesylate improves cardiac performance inhibition associated with myocardial ischemia/reperfusion in animals, and limits infarct size in experimental models. Eniporide mesylate regulates cardiac performance and high-energy phosphate content.

DRL-17822 is a selective cholesteryl ester transfer protein (CETP) inhibitor. DRL-17822 increases high-density lipoprotein levels. The exposure of DRL-17822 nanocrystal formulation increases significantly after a high-fat breakfast. The exposure of DRL-17822 in the fasted state is higher than that of its nanocrystal formulation. DRL-17822 can be used in the research of type II hyperlipidemia and atherosclerotic cardiovascular disease.

DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection.

Dihydrogalanthamine hydrobromide is an acetylcholinesterase inhibitor. Dihydrogalanthamine hydrobromide can be used in research on neurological diseases such as sequelae of poliomyelitis and myasthenia gravis.

Desmethyl-K777 is a one of the main metabolites of K777.

Decarboxy ciprofloxacin (Decarboxylated ciprofloxacin) is an antibacterial agent. Decarboxy ciprofloxacin displays antibacterial activities against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Bacillus subtilis, Enterobacter cloacae, Serratia marcescens and especially potent activity against Escherichia coli.

CQ80 is a PEPD/XPNPEP1 inhibitor and selective CARD8 inflammasome activator. CQ80 has IC50 values of 0.91 μM for PEPD, 43 μM for XPNPEP1. CQ80 promotes the accumulation of Xaa-Pro peptides by inhibiting PEPD and XPNPEP1, releases the fragment of CARD8 for inflammasome formation, and induces pyroptosis via GSDMD cleavage. CQ80 can be used for research on inflammasome, CARD8-expressing cancer cells, HIV-1-infected cell clearance, acute myeloid leukemia (AML).

Clogestone acetate (AY-11440) is an orally active progesterone receptor agonist. Clogestone acetate reduces adrenal and ovarian weight, as well as serum and adrenocortical ketone levels in rats.

nNOS-IN-3 (compound 4) is a selective neuronal nitric oxide synthase (nNOS) inhibitor with a human hnNOS Ki of 25 nM, rat rnNOS Ki of 18 nM, human heNOS Ki of 58140 nM, human hiNOS Ki of 6422 nM. nNOS-IN-3 binds to nNOS active sites via hydrogen bonds with Glu and chalcogen bonds with Met, fails to form chalcogen bonds with heNOS, and undergoes passive transcellular transport with minimal efflux liability. nNOS-IN-3 can be used for the research of neurodegenerative diseases and melanoma.

Cholesterol heptanoic acid is a lipophilic Cholesterol derivative. Cholesterol heptanoic acid can combine with peptides (such as peptides P1 and P2) to form lipopeptides, which possess antiviral activity. Cholesterol heptanoic acid can be used for research of HIV infection.

CE-1037 (MDL 201,404YA) is a selective inhibitor of human neutrophil elastase (HNE) (Ki: 0.45 nM). CE-1037 prevents the pulmonary hemorrhage induced by intratracheal instillation of HNE. CE-1037 can be used for research of pulmonary diseases, such as COPD.

BRD9 ligand-13 is a BRD9 ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD9 Degrader-8.

BMS-856 is a 17β-HSD3 inhibitor. BMS-856 inhibits enzymatic activity of 17β-HSD3, with IC50s of 60 and 300 nM respectively in the enzyme and whole cell assays.

BMS-142 is a PDL1 inhibitor (IC50 = 96.7 nM) (kd = 13.2 nM). BMS-142 can reduce the survival rate of acute T-lymphoblastic leukemia cells and ovarian cancer cells. BMS-142 can be used in research on cancers such as acute T-lymphoblastic leukemia and ovarian cancer.

BCR-ABL-IN-13 is a dual c-Src and Abl inhibitor, with a Ki value of 0.55 μM against c-Src, 0.10 μM against wild-type Abl, and 0.40 μM against the AblT315I mutant. BCR-ABL-IN-13 exerts competitive/mixed-type inhibitory effects on wild-type Abl, and non-competitive inhibitory effects on the drug-resistant AblT315I mutant. BCR-ABL-IN-13 can be used for the research of chronic myeloid leukemia.

Azetirelin (YM-14673) is an analogue of thyrotropin-releasing hormone (TRH).

Azalanstat dihydrochloride (RS-21607 dihydrochloride) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). Azalanstat dihydrochloride reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats.

AY 25674 is an orally active antiallergic agent and a PDE inhibitor. AY 25674 inhibits the release of allergic histamine from mast cells. AY 25674 suppresses passive anaphylaxis induced by reaginic (IgE) antibodies. AY 25674 does not inhibit the increased vascular permeability caused by non-reaginic antibodies, serotonin or histamine. AY 25674 reaches its peak activity shortly after administration; rapid tolerance occurs at high doses. AY 25674 can be used in research related to passive anaphylaxis.

Axl-IN-20 (Compound w11) is a selective, orally active AXL inhibitor, with an IC50 of 5 nM. Axl-IN-20 has antitumor activity against hematological malignancies.

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.

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.

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.

Antimetastatic agent-1 (Compound A-23) is a MET inhibitor. Antimetastatic agent-1 can inhibit cancer metastasis.

Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer.

Anticancer agent 285 is an orally active anticancer agent with highly effective and selective haspin-inhibiting IC50 = 18 nM) activity. Anticancer agent 285 can be used for the study of colorectal cancer[1].