DDR1-IN-1

DDR1-IN-1

Biochem/physiol Actions

DDR1-IN-1 is a type II, subtype-selective discoidin domain receptor (DDR) tyrosine kinase inhibitor (DDR1/2 IC50 = 105 nM/413 nM) that effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 ﹤ 2.5 µM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture (123%, 70%, 50% of control, respectively, post 48-hr 250 nM DDR1-IN-1, 82.5 nM GSK2126458, or combined treatment). ent). ned treatment).

DDR1-IN-1 protects cells from apoptosis by inhibiting collagen-mediated Bcl-2-interacting killer (BIK) induction at both mRNA and protein levels.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576071 DDR1-IN-1 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£449.89 (exc VAT) per 25MG
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3576072 DDR1-IN-1 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£135.11 (exc VAT) per 5MG
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