Inhibitors

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

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

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

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

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

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

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

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

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.

CYY292 is a chemical compound acting as an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, with respective IC50 values of 5.35, 4.6, 28, 28, and 78 nM.

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

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),

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

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

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.

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

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

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

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

Lerzeparib is a PARP (ADP-ribose polymerase) inhibitor that exhibits antineoplastic activity [1].

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

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

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

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

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

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

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

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

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

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

Mal-VC-PAB-PNP-CDN-A is a conjugate comprised of an agent and a linker, utilized in antibody-drug conjugates (ADC) [1] [2].

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

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].

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

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.

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

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

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

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

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

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.

Azilsartan medoxomil potassium (QR-01019K), an angiotensin II receptor antagonist, exhibits a potent and sustained antihypertensive effect, along with a more

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

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

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

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 (

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

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].

VISTA-IN-2 (Compound 1) is a V-domain Ig suppressor of T-cell activation (VISTA) inhibitor that promotes the degradation of VISTA in cells via autophagy,

Immune cell migration-IN-1 (compound 2) serves as a potent inhibitor of immune cell migration, with potential research applications for mitigating conditions

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

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

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

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].

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

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

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

Sakura 6, a synthetic serotonin transporter (SERT)-binding peptide, enhances the interaction between SERT and neuronal nitric oxide synthase.

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.

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.

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.

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 is a potent and selective TxA2/PGH2 receptor antagonist.

BPH-628 is a bioactive chemical.