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KD025
- SLx-2119 - Belumosudil
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C26H24N6O2
- MW: 452.51
Description
KD025 (belumosudil) is a selective, ATP-competitive inhibitor of Rho-associated kinase 2 (ROCK2) with an IC50 value of 105 nM, compared with 24 µM for ROCK1. This approximately 200-fold biochemical selectivity enables preferential interrogation of ROCK2-dependent signaling.
KD025 modulates cytoskeletal and transcriptional pathways downstream of ROCK2 and has been used to study immune-cell differentiation and fibrotic signaling, including effects on STAT3/STAT5 balance and Th17-associated cytokine programs. It is useful in cellular and in vivo models of fibrosis, inflammation and vascular remodeling.
Key Features
- Selective ATP-competitive ROCK2 inhibitor
- IC50: 105 nM for ROCK2
- Approximately 200-fold biochemical selectivity over ROCK1
- Modulates immune and fibrotic signaling
Applications
- ROCK2 kinase research & Rho–ROCK signaling studies
- T-cell differentiation assays
- Fibrosis models
- Inflammation and vascular-remodeling research
More Information
| Parent CAS No. | 911417-87-3 |
|---|---|
| Chemical Name | 2-(3-(4-(1H-Indazol-5-ylamino)quinazolin-2-yl)phenoxy)-N-isopropylacetamide |
| SMILES | C1C=C2C(NC3C=CC4NN=CC=4C=3)=NC(C3C=C(OCC(=O)NC(C)C)C=CC=3)=NC2=CC=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C26H24N6O2/c1-16(2)28-24(33)15-34-20-7-5-6-17(13-20)25-30-23-9-4-3-8-21(23)26(31-25)29-19-10-11-22-18(12-19)14-27-32-22/h3-14,16H,15H2,1-2H3,(H,27,32)(H,28,33)(H,29,30,31) |
| InChiKey | GKHIVNAUVKXIIY-UHFFFAOYSA-N |
| CID | 11950170 |
| Short Description | ROCK2 inhibitor |
References
- M Boerma et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18.
- DTV Diep et al. Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells. Sci Rep. 2018 Feb 6;8(1):2477.
- JH Lee et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14.
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