Molecular structure of Src kinase inhibitor I, CAS Number: 179248-59-0
Src kinase inhibitor I (CAS 179248-59-0)
See product citations (11)
Alternate Names:
4-(4′-Phenoxyanilino)-6,7-dimethoxyquinazoline
Application:
Src kinase inhibitor I is a potent dual site inhibitor of Src family kinases
CAS Number:
179248-59-0
Purity:
≥97%
Molecular Weight:
373.40
Molecular Formula:
C22H19N3O3
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Src kinase inhibitor I is a 4-anilinoquinazole competitive inhibitor of Src family tryosine kinases. Src kinase inhibitor I is a dual site inhibitor, described to compete at both the ATP and peptide binding sites of the kinase. A particularly potent inhibitor of the Src kinases, Src Kinase inhibitor I demonstrates nanomolar inhibition of c-Src (IC50 = 44 nM) and Lck (IC50 = 88 nM). Low micromolar inhibition of Flk-1 (VEGFR2, IC50 = 0.32 muM) and C-fms (IC50 = 30 muM) are also reported. Src Kinase inhibitor I demonstrates a strong selectivity for Src over the other kinases, a property attributed to the dual site inhibition action of this compound. Use of Src Kinase inhibitor I in parallel with PP 1 (sc-203212) and PP 2 (sc-202769) for Src family kinase inhibition has also been described.
Src kinase inhibitor I (CAS 179248-59-0) References
- Structural determinants for potent, selective dual site inhibition of human pp60c-src by 4-anilinoquinazolines. | Tian, G., et al. 2001. Biochemistry. 40: 7084-91. PMID: 11401553
- The selectivity of protein kinase inhibitors: a further update. | Bain, J., et al. 2007. Biochem J. 408: 297-315. PMID: 17850214
- Enhanced ex vivo expansion of human adipose tissue-derived mesenchymal stromal cells by fibroblast growth factor-2 and dexamethasone. | Lee, SY., et al. 2009. Tissue Eng Part A. 15: 2491-9. PMID: 19292683
- Enhancement of mesenteric artery contraction to 5-HT depends on Rho kinase and Src kinase pathways in the ob/ob mouse model of type 2 diabetes. | Matsumoto, T., et al. 2010. Br J Pharmacol. 160: 1092-104. PMID: 20590603
- Sorafenib induces apoptosis in HL60 cells by inhibiting Src kinase-mediated STAT3 phosphorylation. | Zhao, W., et al. 2011. Anticancer Drugs. 22: 79-88. PMID: 20881478
- Extracellular ATP stimulates epithelial cell motility through Pyk2-mediated activation of the EGF receptor. | Block, ER., et al. 2011. Cell Signal. 23: 2051-5. PMID: 21840393
- Downregulation of carbonic anhydrase IX promotes Col10a1 expression in chondrocytes. | Maruyama, T., et al. 2013. PLoS One. 8: e56984. PMID: 23441228
- Chemical interrogation of the neuronal kinome using a primary cell-based screening assay. | Al-Ali, H., et al. 2013. ACS Chem Biol. 8: 1027-36. PMID: 23480631
- Redox-regulated pathway of tyrosine phosphorylation underlies NF-κB induction by an atypical pathway independent of the 26S proteasome. | Cullen, S., et al. 2015. Biomolecules. 5: 95-112. PMID: 25671697
- Critical Roles of STAT3 in β-Adrenergic Functions in the Heart. | Zhang, W., et al. 2016. Circulation. 133: 48-61. PMID: 26628621
- Specific role of N-methyl-D-aspartate (NMDA) receptor in elastin-derived VGVAPG peptide-dependent calcium homeostasis in mouse cortical astrocytes in vitro. | Szychowski, KA. and Gmiński, J. 2019. Sci Rep. 9: 20165. PMID: 31882909
- Elastin-Derived Peptides in the Central Nervous System: Friend or Foe. | Szychowski, KA., et al. 2022. Cell Mol Neurobiol. 42: 2473-2487. PMID: 34374904
- Tyrosine phosphorylation of DEPTOR functions as a molecular switch to activate mTOR signaling. | M Gagné, L., et al. 2021. J Biol Chem. 297: 101291. PMID: 34634301
Inhibitor of:
c-Src, FAM21C, Fer, Flk-1, GPR115, KIR2DS4, Lck, SH3TC1, and Tyrosine Kinase.Activator of:
BRDG1, GAP-assoc p190, p130 Cas, REPS2, SH2D3A, and SH3YL1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Src kinase inhibitor I, 1 mg | sc-204303 | 1 mg | $53.00 | |||
Src kinase inhibitor I, 10 mg | sc-204303A | 10 mg | $204.00 |