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DDR1-IN-4

Catalog No. T39572 CAS 2125676-13-1

Synonyms: DDR1-IN-4

DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation. This compound demonstrates exceptional efficacy with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.

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DDR1-IN-4, CAS 2125676-13-1

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Biological Description

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Storage & Solubility Information

Description	DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation. This compound demonstrates exceptional efficacy with IC50 values of 29 nM and 1.9 μM for DDR1 and DDR2, respectively.
Targets&IC50	DDR2:1900 nM (IC50), DDR1:29 nM (IC50)
In vitro	DDR1-IN-4 (Compound 2.45) demonstrates a dose-dependent suppression of DDR1 phosphorylation in HT1080 cells with DDR1 overexpression, achieving over 70% inhibition at 1 μM concentration, while maintaining selectivity against DDR2 [1].
In vivo	DDR1-IN-4 (Compound 2.45, ip, 90 mg/kg) effectively maintains renal function and mitigates tissue damage in Col4a3 –/– mice, serving as a preclinical model for Alport syndrome, by implementing a therapeutic dose regimen. This demonstrates the potential benefits of targeting DDR1 phosphorylation inhibition in vivo[1]. In this Col4a3 –/– mouse model, depicting Alport syndrome[1], administration of 90 mg/kg via intraperitoneal injection daily notably decreased fibrosis, evident from assessments using Picro Sirius Red, smooth muscle actin staining, and collagen I levels. Additionally, there was a considerable reduction in pDDR1 levels in these mice compared to control groups, underlining the compound's efficacy.

Synonyms	DDR1-IN-4
Molecular Weight	565.351
Formula	C23H20BrF3N6O3
CAS No.	2125676-13-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

DDR1-IN-4 2125676-13-1 DDR1 IN 4 DDR-1-IN-4 DDR1IN4 inhibitor inhibit

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