Inhibiteurs

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

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

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].

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

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

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

Davelizomib is a proteasome inhibitor that exhibits antineoplastic 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.

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

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

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

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

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

(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.

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.

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

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].

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 (

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

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

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

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

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].

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

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

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

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

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

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

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

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

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.

Civorebrutinib (WS-413) is an inhibitor of Bruton's tyrosine kinase that exhibits antineoplastic activity [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].

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

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

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

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.

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.

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

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

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

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

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

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].

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

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.

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

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

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

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

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 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

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

BPH-628 is a bioactive chemical.