Src Inhibitor

Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC₅₀ values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC₅₀=16.1 nM), VEGFR2 (IC₅₀=1.5 nM), and Src (IC₅₀=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.

TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

7-Hydroxychromone is a Src kinase inhibitor with an IC₅₀ of <300 μM.

Squarunkin A is a potent and selective UNC119-cargo interaction inhibitor, interrupting the UNC119A-myristoylated Src N-terminal peptide interaction (IC₅₀=10 nM). Squarunkin A interferes with the activation of Src kinase in cells.

SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC₅₀ = 60 nM). SB 220025 also inhibits p56^Lck and PKC with IC₅₀ values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.

HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC₅₀s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC₅₀>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.

Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC₅₀s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.

XL228 is a multi-targeted tyrosine kinase inhibitor with IC₅₀s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.

JNJ-49095397 (RV568) is an inhaled narrow-spectrum kinase inhibitor (NSKI) against both the α and γ isoforms of p38 MAPK. JNJ-49095397 also inhibits SRC kinase family, specifically haematopoietic kinase (HCK) JNJ-49095397 shows potent anti-inflammatory effects and can be used for the research of chronic obstructive pulmonary disease (COPD) and asthma.

Chemerin15 is an anti-inflammatory peptide derived from Chemerin. Chemerin15 binds to ChemR23. Chemerin15 inhibits TNFα-induced activation of Syk, ERK and Src kinases. Chemerin15 increases the expression of p-p38 mRNA and protein. Chemerin15 mediates phagocytosis, resolution of inflammation, CD62L shedding and downregulation of PSGL-1 expression in macrophages and microglia. Chemerin15 inhibits neutrophil-mediated vascular inflammation and myocardial ischemia-reperfusion injury via ChemR23. Chemerin15 enhances microglial phagocytosis, thereby alleviating cerebral ischemia-reperfusion injury.

Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56^lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 ^lck autophosphorylation and phosphorylation of exogenous substrates with IC₅₀s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.

1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of src family kinases and Protein Kinase D. 1-Naphthyl PP1 hydrochloride inhibits v-Src and c-Fyn, c-Abl, CDK2 and CAMK II with IC₅₀s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively.

Lck inhibitor 2 is a bisanilino pyrimidine-derived tyrosine kinase inhibitor targeting LCK, BTK, LYN, SYK and TXK, with a K_d value of 10 nM against TXK.

TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC₅₀ values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively.

YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization.

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

2-Hydroxy-3-methylanthraquinone (compound 1) is a natural compound isolated from a water extract of Hedyotis diffusa WILLD. 2-Hydroxy-3-methylanthraquinone shows inhibitory activity against protein tyrosine kinases v-src and pp60src, and induces growth arrest and apoptosis in the HepG2 cancer cells.

HPK1-IN-2 dihydrochloride is an orally active HPK1 inhibitor (IC₅₀ < 0.05 µM) with antitumor activity. HPK1-IN-2 dihydrochloride inhibits the activity of Lck (IC₅₀ < 0.05 µM) and Flt3 (IC₅₀ < 0.05 µM) kinases.

PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC₅₀: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models..

Lavendustin C is a potent Ca²⁺ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC₅₀ of 0.2 μM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC₅₀=0.012 μM) and pp60^c-src(+) kinase (IC₅₀=0.5 μM) .