Inhibitors

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.

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

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

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

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

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

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

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

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

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.

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

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

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

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

BET-IN-1 is a bromodomain inhibitor extracted from patent WO/2013024104A1 (example 2, plC50: 6.0 - 7.0).

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

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.

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

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].

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

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

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

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

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [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,

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

Py-MAA-Val-Cit-PAB-MMAE (AAJ8D6-PY-Val-Cit-MMAE) serves as an ADC linker for Zapadcine-3a, a broad-spectrum anti-TRAILR2 ADC with antineoplastic properties.

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

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

JAK1-IN-11 (compound 11) serves as a potent inhibitor of Janus kinases, exhibiting nanomolar inhibitory concentrations with IC50 values of 0.02 nM (JAK1) and 0.

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

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.

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.

BPH-628 is a bioactive chemical.

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

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

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

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.