SLX-2119
CAS No. | 911417-87-3 | Cat. No. | BCP15921 |
Name | SLX-2119 | ||
Synonyms | SLX 2119;SLX2119;KD-025;KD 025;KD025;ROCK inhibitor; | ||
Formula | C26H24N6O2 | M. Wt | 452.51 |
Description | in vitro: SLx-2119 selectively inhibits activity of human ROCK2 (IC50 = 105 nM), while effects on human ROCK1 in this cell-free system were minimal (IC50 = 24 μM). SLx-2119 at 40 μM induced significant down-regulations of Tsp-1 and CTGF mRNA levels. SLx-2119 induced a significant down-regulation of Tsp-1 transcripts in HMVEC and PASMC only and induced a down-regulation of CTGF transcripts, although non-significant, in all 3 cell types(HMVEC, PASMC, and NHDF). SLx-2119 induced a down-regulation of the genes COL1A1, COL1A2, COL3A1, and COL5A2 in PASMC, an up-regulation of the gene MMP1 in PASMC, a down-regulation of the gene COL3A1 in NHDF, and an up-regulation of the genes COL7A1, COL4A2, MMP1, MMP3, MMP14, and MMP17 in NHDF. in vivo: SLX-2119 200 mg/kg twice a day for 36 h starting 1 h after ischemia onset, significantly reduced tissue loss in the ipsilateral hemisphere compared with vehicle when measured 4 weeks after ischemia.SLX-2119 appeared even more efficacious in females (42% re | ||
Pathways | Cell Cycle/DNA Damage TGF beta/Smad Wnt/Stem Cell | ||
Targets | ROCK |
Structure
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