KD025 (Belumosudil, SLx-2119)

Chemical Structure : KD025

CAS No.: 911417-87-3

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货号: PC-73191Not For Human Use, Lab Use Only.

KD025 (Belumosudil, SLx-2119) is a potent, selective ROCK2 inhibitor with IC50 of 105 nM.

规格	价格	库存
10 mg	￥980	In stock
25 mg	￥1580	In stock
50 mg	￥2580	In stock
100 mg		Get quote

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生物&药学活性

KD025 (Belumosudil, SLx-2119) is a potent, selective ROCK2 inhibitor with IC50 of 105 nM.
KD025 displays >200-fold selectivity over ROCK1 (IC50>20 uM).
KD025 dose-dependently reduced infarct volume after transient middle cerebral artery occlusion, cortical perfusion in a distal middle cerebral artery occlusion model.
KD025 significantly diminished STAT3 phosphorylation and binding to IL-17 and IL-21 promoters and reduced IRF4 and nuclear hormone RAR-γt protein levels in T cells derived from healthy subjects or rheumatoid arthritis patients.
KD025 in vivo down-regulates the progression of collagen-induced arthritis in mice via targeting of the Th17-mediated pathway.
KD025 inhibits the secretion of IL-21, IL-17, and INF-γ along with decreasing p-STAT3 and reduced protein expression of IRF4 and BCL6 in human PBMCs purified from active cGVHD patients.

物理化学性质&存储条件

分子量	452.518
分子式	C26H24N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(3-(4-((1H-Indazol-5-yl)amino)quinazolin-2-yl)phenoxy)-N-isopropylacetamide

参考文献

1. Flynn R, et al. Blood. 2016 Apr 28;127(17):2144-54.

2. Zanin-Zhorov A, et al. Proc Natl Acad Sci U S A. 2014 Nov 25;111(47):16814-9.

3. Lee JH, et al. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14.