| Hazard Information | Back Directory | [Description]
DDR1-IN-1 is a potent and selective DDR1 inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2. DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity as assessed against a panel of 451 kinases measured. DDR1-IN-1 provides a useful pharmacological probe for DDR1-dependent signal transduction. The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion. | [Uses]
DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM)[1]. | [IC 50]
DDR1: 105 nM (IC50); DDR2: 413 nM (IC50) | [storage]
Desiccate at RT | [References]
[1] Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. DOI:10.1021/cb400430t |
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BOC Sciences
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https://www.bocsci.com |
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