Inhibitors

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

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

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

Civorebrutinib (WS-413) is an inhibitor of Bruton's tyrosine kinase that exhibits antineoplastic activity [1].

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].

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].

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

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

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

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

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

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

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

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 (

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].

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

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.

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

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.

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

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

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.

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

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.

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.

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].

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

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

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

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.

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.