Inhibiteurs

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

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,

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.

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

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

And1-IN-1, also known as compound III, is a potent inhibitor of And1 [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 I (S1P1 agonist 6) is an S1P1 agonist that mitigates autoimmune activity by inhibiting lymphocyte trafficking and has potential as an immunosuppressive

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

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

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

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.

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

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].

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

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

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

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,

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

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

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

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 (

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

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

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

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

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

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.

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

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

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

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

EST73502 is a compound that functions as a dual agonist for the μ-opioid receptor (MOR) and an antagonist for the σ1 receptor (σ1R). It is selective, orally active, and possesses the ability to penetrate the blood-brain barrier (BBB). The compound exhibits a Ki value of 64 nM for the MOR and 118 nM for the σ1R. Additionally, EST73502 demonstrates antinociceptive 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

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

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

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

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

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

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

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.

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

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

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 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

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

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.