Inhibitors

Estrogen Receptor Modulator 8 (compound 4) is an orally active inhibitor targeting Estrogen Receptor/ERR α with potent efficacy (IC50 = 0.437 nM in MCF-7 cells

MDL-811, an allosteric activator of SIRT6, markedly enhances the deacetylation of histone H3 at lysine residues 9, 18, and 56 (H3K9Ac, H3K18Ac, and H3K56Ac),

(αR)-Cyclopropaneacetamide-Exatecan (compound 2-A), an Exenotecan derivative, serves as a cytotoxic agent that effectively inhibits the proliferation of U87MG

Antibacterial Agent 160 is a potent antibacterial agent that rapidly eradicates bacteria and inhibits the formation of bacterial biofilms.

PI3Kδ-IN-13 (compound 89), with an IC50 value of 2.6 nM, is an inhibitor of PI3Kδ, applicable for researching diseases involving cell proliferation, including

BTK-IN-25 (compound 71) is a potent BTK inhibitor, demonstrating an IC50 of 0.77 nM against BTK(C481S) and achieving an IC50 of 1 nM in DOHH2 cells [1].

JAK-IN-27, also known as compound 1, is an orally active, potent inhibitor of the JAKS family kinases, displaying inhibitory concentrations (IC50s) of 3.0 nM

JAK1-IN-10 (compound 9), a cyano-substituted cyclic hydrazine derivative, functions as a potent and selective inhibitor of JAK1 [1].

Cap-dependent endonuclease-IN-9, a strong influenza inhibitor, shows low toxicity, good pharmacokinetics, and dynamic action.

TrkB-IN-1 is a potent, orally active agonist of the TrkB receptor, with favorable pharmacokinetic (PK) properties.

JDB175, a selective BTK inhibitor with oral bioavailability, demonstrates excellent penetration through the blood-brain barrier.

AEF0117 is a signaling inhibitor of CB1-SSi that inhibits cannabinoid self-administration and can be used to study cannabis withdrawal.

FAP-IN-2 is a 99mTc-labeled, isonitrile-containing derivative of a fibroblast activation protein (FAPI) inhibitor suitable for tumor imaging [1].

S-72 acts as a microtubule polymerization inhibitor, effective in cell-free assays at concentrations of 1, 3, and 10 µM.

HPK1-IN-38 (compound 15) is an inhibitor of MAP4K1/HPK1, suitable for research into disorders related to HPK1 [1].

LM2I, a derivative of Spinosyn A (SPA), serves both as an argininosuccinate synthase (ASS1) enzyme activator and a tumor inhibitor through direct interaction

Davelizomib is a proteasome inhibitor that exhibits antineoplastic activity [1].

Anti-MI/R injury agent 1 (compound 18), derived from Panaxatriol, represents an orally administered, potent agent against myocardial ischemia/reperfusion (MI/R

DiMal-O-CH2COOH is a cleavable linker utilized in antibody-drug conjugates (ADCs).

Compound S6, Mc-Alanyl-Alanyl-Asparagine-PAB-MMAE, is a potent anticancer agent specifically activated by the tumor microenvironment; it demonstrates efficacy

APG-2449 is an orally active inhibitor targeting ALK, ROS1, and FAK, demonstrating antitumor efficacy in mouse models of non-small cell lung cancer (NSCLC) [1].

Compound Im (Insecticidal agent 6) is a potent inhibitor of insect ryanodine receptors (RyRs), exhibiting an EC50 of 0.6308 µM against S.

Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan is a linker molecule employed in the synthesis of antibody-drug conjugates (ADCs), demonstrating potent antitumor

STAT3-IN-18 (compound SPP), a platinum (IV) complex featuring an axial ligand from sandalwood, suppresses the JAK2-STAT3 pathway in breast cancer (BC) cells and

BTK-IN-27 (example 8), a potent BTK inhibitor with an IC50 of 0.2 nM, demonstrates anti-proliferative effects in TMD8 cells with an IC50 of less than 5 nM.

JAK-IN-34 (compound 11n) is a potent inhibitor of Janus kinases (JAKs), demonstrating IC50 values of 0.40 nM for JAK1, 0.83 nM for JAK2, 2.10 nM for JAK3,

Tauro-obeticholic acid, a farnesoid X receptor (FXR) agonist and semisynthetic derivative of chenodeoxycholic acid, is an active metabolite of obeticholic acid.

DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating

BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor featuring a trimethoxy group [1].

ATR-IN-24 (Compound 1) is an ATR inhibitor with demonstrated anticancer activity [1].

IDO1-IN-22 (Compound 3) is an inhibitor of IDO1, demonstrating potent activity with biochemical hIDO1 IC50 of 67.4 nM and HeLa hIDO1 IC50 of 17.6 nM.

SHP2-IN-14 (compound 27) is a potent, orally active allosteric inhibitor of SHP2, displaying strong anti-tumor activity with an IC50 of 7 nM.

Antitumor Agent-104 (Compound 9) serves as an antineoplastic by impeding DNA repair mechanisms in tumor cells, primarily through the inhibition of PARP1 enzyme

RIOK2-IN-2 (8) functions as an inhibitor of RIOK2, exhibiting IC50 values of 3.02 μM in MKN-1 cells and 5.34 μM in MOLT4 cells [1].

PHI-101 is a checkpoint kinase 2 (Chk2) inhibitor that can be used for the study of refractory acute myeloid leukemia (AML) and ovarian cancer.

hDHODH-IN-8 is a potent human dihydroorotic dehydrogenase (hDHODH) inhibitor (IC50: 16 nM) that exhibits potent antiproliferative effects and has good water solubility, with potential for oncology studies, especially in lymphoma.

Ifetroban is a potent and selective TxA2/PGH2 receptor antagonist.

Ifetroban sodium (BMS-180291), oral TXA2/PGH2 antagonist for researching heart, stroke, BP, thrombosis.

ROCK-IN-6, a selective ROCK2 inhibitor, exhibits potent inhibition with an IC50 of 2.19 nM and holds promise for research into glaucoma and retinal diseases [1

BPH-628 is a bioactive chemical.