DDR1-IN-4 |
| Catalog No.GC64268 |
DDR1-IN-4 (composé 2.45) est un inhibiteur sélectif et puissant de l'autophosphorylation du récepteur du domaine de la discoÏdine 1 (DDR1), avec des valeurs IC50 de 29 nM et 1,9 μM pour DDR1 et DDR2, respectivement .
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2125676-13-1
Sample solution is provided at 25 µL, 10mM.
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DDR1-IN-4 (Compound 2.45) is a selective and potent Discoidin Domain Receptor 1 (DDR1) autophosphorylation inhibitor, with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively[1].
DDR1-IN-4 (Compound 2.45) shows a clear dose-dependent inhibition of DDR1 phosphorylation in HT1080 cells overexpressing DDR1, with greater than 70% inhibition of phosphorylation at a concentration of 1 μM, and retaining selectivity over inhibition of DDR2[1].
DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) preserves renal function and reduces tissue damage in Col4a3-/- mice (the preclinical mouse model of Alport syndrome) when employing a therapeutic dosing regime, indicating the real therapeutic value of selectively inhibiting DDR1 phosphorylation in vivo[1].
[1]. Hans Richter, et al. DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome. ACS Chem Biol. 2019 Jan 18;14(1):37-49.
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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