Inhibitors

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].

VMAT2-IN-2 tosylate is a potent inhibitor of VMAT2 and is applicable in the research of tardive dyskinesia [1].

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.

YK-029A, an orally active EGFR mutant inhibitor, targets both EGFR T790M and EGFRex20ins mutations.

URAT1&XO Inhibitor 1 (compound 29) serves as a dual inhibitor with IC50 values of approximately 10 μM for URAT1 and 1.01 μM for Xanthine Oxidase.

DiaFluo is a probe for protein S-sulfinylation from cells.

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

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

CIAC001, a pyruvate kinase PKM2 inhibitor, exhibits anti-neuroinflammatory properties.

DDO-2213 is a potent, orally active inhibitor of the WDR5-MLL1 interaction, demonstrating an IC50 of 29 nM and a Kd of 72.9 nM against WDR5.

LT-540-717 (compound 32), a potent FLT3 inhibitor (IC50=0.62 nM), exhibits antiproliferative activity and effectively inhibits various acquired FLT3 mutations,

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

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),

IDO/Tubulin-IN-2 inhibits TDO/tubulin, effective on U87, HepG2, A549, HCT-116, LO2 cancer cells; IC50 values 0.036-1.04 μM, boosts antitumor action.

Tibremciclib is a cyclin-dependent kinase 4 (CDK4) inhibitor that exhibits antineoplastic properties [1].

URAT1 Inhibitor 5 (compound 16) serves as a powerful inhibitor of URAT1 and is utilized in hyperuricemia research [1].

SARS-CoV-2-IN-68 (compound 6C) is a covalent inhibitor of both SARS-CoV-2 PLpro and Mpro, exhibiting potent antiviral properties by targeting the Zn-finger

LFS-1107, a reversible CRM1 inhibitor (Kd: 12.5 pM), selectively targets and eliminates ENKTL cells, offering potential for cancer research applications [1].

BET-IN-14 is a pan BET inhibitor with an IC50 of 5.35 nM, demonstrating oral activity and anticancer properties [1].

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].

Compound I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive

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

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

And1-IN-1, also known as compound III, is a potent inhibitor of And1 [1].

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

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

FLT3-IN-19 (Comp 50) is a potent, selective inhibitor of FLT3, demonstrating an IC50 value of 0.213 nM, and is applicable in research pertaining to acute

Syk-IN-8 (compound 19q) functions as a Syk inhibitor with demonstrated antiproliferative effects on a variety of hematological tumor cells.

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

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

FOXM1-IN-2, a FOXM1 inhibitor, exhibits antineoplastic activity [1].

MOR Agonist-1 is a μ-opioid receptor (MOR) agonist noted for its potent analgesic properties and is utilized in research concerning pain and associated

ALPK1-IN-3,serves as an ALPK1 inhibitor that dampens proinflammatory gene expression in the kidney and enhances survival in animal models of sepsis-induced

Xilmenolone acts as a positive allosteric modulator of the GABA_A receptor [1].

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

Compound 11, also known as Antitumor Photosensitizer-2, is a potent photosensitizer with remarkable photodynamic anti-tumor properties and minimal skin photo-

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

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

BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant.

Bi-Mc-VC-PAB-MMAE is an agent-linker conjugate for antibody-drug conjugates (ADCs), featuring the linker (Fmoc-Val-Cit-PAB) and the potent tubulin inhibitor (

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

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

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

Canlitinib, a tyrosine kinase inhibitor, holds potential for cancer research.

ROCK2-IN-6 (Comp A) is a selective inhibitor of ROCK2, applicable in the study and treatment of ROCK-mediated, autoimmune, and inflammatory diseases [1].

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

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

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,

Antitumor Photosensitizer-1 (Compound 8) is a potent photosensitizer with remarkable photodynamic anti-tumor properties and minimal skin photo-toxicity,

Yhhu6669 is an anti-HBV agent that suppresses viral DNA and replication by promoting DNA-free capsid assembly, effectively reducing HBV DNA and HBcAg levels in

Compound B12 (Antibacterial agent 157) is a fungicidal agent that can impact protein synthesis in Botrytis cinerea.

HBV-IN-38 (Example 193), an HBV DNA inhibitor with an EC50 value of ≤100 nM, serves as a research tool for investigating viral infections [1].

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

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.

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

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.

BPH-628 is a bioactive chemical.

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