Angiogenesis

Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor with anti-tumor properties. It inhibits FAK autophosphorylation in prostate cancer cells and suppresses spheroid formation and in situ tumor growth in vivo. Ifebemtinib (tosylate) is applicable in cancer research, including studies on solid tumors, breast cancer, and malignant pleural mesothelioma.

VEGFR-2-IN-17 (15a) is a potent VEGFR-2 inhibitor with an IC50 of 67.25 nM, showing significant antitumor effects.

VEGFR-2/DHFR-IN-2 inhibits VEGFR-2 & DHFR (IC50: 0.623 & 9.085 μM), toxic to C26, HepG2, MCF7 cells (IC50: 3.59-8.38 μM), promising for cancer study.

M-COPA disrupts Golgi, blocks MET & Arf1 activation, and inhibits angiogenesis via VEGFR & NF-kB pathways.

Potent EGFR/HER2/DHFR inhibitor for MCF-7 breast cancer; IC50: 0.153/0.108/0.291 μM; arrests G1/S phase, triggers apoptosis.

VEGFR-2-IN-15 (Compound 14b) is a potent inhibitor of VEGFR-2. VEGFR-2-IN-15 inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.

CEE321 is an effective pan-JAK inhibitor with an IC50 of 54 nM. It effectively inhibits biomarkers associated with atopic dermatitis.

Bayer-18 is an inhibitor of TYK2. It inhibits the viability of anaplastic large cell lymphoma cells, including K299, SR786, Mac1, and Mac2a, with an IC50 ranging from 2-3 µM. Additionally, Bayer-18 induces apoptosis in K299 and SR786 cells.

Protein kinase inhibitor 11 (Compound I-96) is an agent that inhibits the activity of PIM-1, CDK-2, GSK-3, and SRC. It shows potential for research in cancer, autoimmune diseases, and neurodegenerative disorders.

JAK1/TYK2-IN-3, orally active, selectively inhibits TYK2 (IC50: 6 nM), JAK1 (37 nM), JAK2 (140 nM), JAK3 (362 nM), and has anti-inflammatory effects.

(Rac)-Ibrutinib alkyne (Compound 8) is a Btk inhibitor with an IC50 of 0.72 nM. This compound effectively inhibits B cell receptor signaling functions, with an IC50 of 9 nM for calcium flux inhibition in Ramos cells. (Rac)-Ibrutinib alkyne is applicable in research on diseases such as rheumatoid arthritis.

EGFR/HER2-IN-7: Potent, selective dual inhibitor for MCF-7 cancer; IC50: EGFR 0.18μM, HER2 0.146μM, DHFR 0.907μM.

GNE-431: potent, selective noncovalent Btk inhibitor, IC50=3.2 nM; effective against C481R, T474I, T474M mutants, may counter ibrutinib resistance.

FLT3-ITD-IN-3 (13v) is an orally active inhibitor of FLT3-ITD (internal tandem duplication of FLT3), which works by blocking FLT3 signaling. This inhibition leads to cell cycle arrest in the G0/G1 phase and induces apoptosis. The compound is currently employed in studies related to acute myeloid leukemia (AML).

JP-153 is an inhibitor of Src-FAK-Paxillin signaling. It suppresses Src-dependent phosphorylation of paxillin (Y118) and subsequent activation of Akt (S473). JP-153 reduces VEGF-induced migration and proliferation of retinal endothelial cells and is applicable in the study of neovascular eye diseases.

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.

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.

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.