Name | DDR1-IN-4 |
Description | DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2. |
In vitro | DDR1-IN-4 (Compound 2.45) exhibits dose-dependent inhibition of DDR1 phosphorylation in DDR1-overexpressing HT1080 cells, achieving over 70% inhibition at a 1 μM concentration, while maintaining selectivity against DDR2 [1]. |
In vivo | DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) maintains renal function and mitigates tissue damage in Col4a3 –/– mice, a preclinical model for Alport syndrome, through DDR1 phosphorylation inhibition. In this model, daily 90 mg/kg intraperitoneal injections reduced fibrosis, indicated by Picro Sirius Red, smooth muscle actin staining, collagen I levels, and decreased pDDR1 levels, demonstrating efficacy. |
Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 200 mg/mL (353.77 mM), Sonication is recommended.
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Keywords | DDR1IN4 | DDR1 IN 4 | DDR-1-IN-4 | DDR1-IN-4 |
Inhibitors Related | DDR-TRK-1 | DDR Inhibitor | Ddr1-In-1 | VU6015929 | FGFR1/DDR2 inhibitor 1 | Sitravatinib | LCB 03-0110 | DDR1-IN-2 | Merestinib | (S)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-2-(pyrimidin-5-yl)-1,2,3,4-tetrahydroisoquinoline-7-carboxamide |