Angiogenesi

FGFR4-IN-9 is a selective inhibitor of FGFR4 (IC50: 75.3 nM) that effectively inhibits the growth and angiogenesis of hepatocellular carcinoma cells.

FGFR1 inhibitor-6, IC50: 16.31 nM, blocks cell cycle at pro-G1/G2/M and induces apoptosis.

EGFR-IN-17: potent, selective EGFR inhibitor, IC50 of 0.2 nM, overcomes C797S drug resistance.

MTX-216 is an ATP-competitive inhibitor targeting both PI3K and EGFR. It simultaneously inhibits Ki-67 and ribosomal S6 phosphorylation, inducing apoptosis in NF1LOF cells. Additionally, MTX-216 suppresses SYK kinase activity with an IC50 of 281 nM. This compound is applicable for melanoma research.

E7090 succinate inhibits FGFR1, FGFR2, and FGFR3 with IC50: 0.71, 0.50, 1.2 nM; less so FGFR4 at 120 nM.

Antiallergic agent-1, an Src family kinase inhibitor, is a new and valuable lead compound with potential as an anti-allergic agent.

HER2-IN-6, a potent HER2 inhibitor, may target wild/mutant EGFR and HER2-mediated tumors. (Patent WO2021164697A1, compound 11)

EGFR-IN-146 is an EGFR inhibitor that suppresses the EGFR signaling pathway and improves insulin sensitivity by activating the AMPK pathway. It effectively reduces blood glucose levels and body weight, showing great potential in the study of diabetes and obesity.

TTT 3002: oral FLT3 inhibitor for AML research, blocks D835 mutations, potent at 0.2 nM IC50.

JAK2 JH2 binder-1: potent, selective, Ki=37.1 nM, potential for studying myeloproliferative neoplasms.

BTK-IN-8: potent, selective covalent BTK inhibitor; IC50=0.22 nM, Kd=0.91 nM; effective in blood CD69 cells (IC50=0.029 μM).

EGFR-IN-34 is a low-toxicity, acrylamide derivative antitumor agent that is a potent inhibitor of EGFR.

Vatalanib hydrochloride (PTK787 hydrochloride) is an orally available and highly potent tyrosine kinase (VEGF) inhibitor that reduces the number and size of Aβ plaques in the cortex of 5xFAD mice, which may be useful in the study of Alzheimer's disease and cancer.

NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd<200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases

XMD-17-51 Trifluoroacetate is a pyrimido-diazepinone compound that regulates protein kinases.

JDTic, a 4-phenylpiperidine derivative distantly related to analgesics like meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan, exhibits a notably long duration of action, maintaining effects in animals for weeks following a single dose. This duration is not due to irreversible binding to the kappa opioid receptor but rather to altered activity of c-Jun N-terminal kinases. As a highly selective antagonist for the κ-opioid receptor, without influencing the μ- or δ-opioid receptors, JDTic has shown potential in animal studies for producing antidepressant and anxiolytic effects. It also demonstrates promise in treating addiction to substances such as cocaine and morphine, distinguishing itself structurally from other kappa antagonists like norbinaltorphimine.

JAK2-IN-7 selectively inhibits JAK2 (IC50: 3 nM), shows 14-fold selectivity over JAK1/3, FLT3, induces G0/G1 arrest, apoptosis, and has antitumor effects.

Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.