KD025 (SLx-2119) - ≥98%, high purity , CAS No.911417-87-3, Inhibitor of Rho associated coiled-coil containing protein kinase 1;Inhibitor of Rho associated coiled-coil containing protein kinase 2
KD025 (SLx-2119) - ≥98%, high purity , CAS No.911417-87-3, Inhibitor of Rho associated coiled-coil containing protein kinase 1;Inhibitor of Rho associated coiled-coil containing protein kinase 2
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 induce
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of Rho associated coiled-coil containing protein kinase 1;Inhibitor of Rho associated coiled-coil containing protein kinase 2
Product Description
SLx-2119(KD-025) is a small molecule and selective inhibitor of ROCK2 with IC50 of 105 nM; > 200 fold selecivity over ROCK1(IC50 =24 uM)
1.Boerma M, Fu Q, Wang J, Loose DS, Bartolozzi A, Ellis JL, McGonigle S, Paradise E, Sweetnam P, Fink LM et al.. (2008) Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin.. Blood Coagul Fibrinolysis, 19 (7):(709-18). [PMID:18832915]
2.Tengesdal IW, Kitzenberg D, Li S, Nyuydzefe MS, Chen W, Weiss JM, Zhang J, Waksal SD, Zanin-Zhorov A, Dinarello CA. (2018) The selective ROCK2 inhibitor KD025 reduces IL-17 secretion in human peripheral blood mononuclear cells independent of IL-1 and IL-6.. Eur J Immunol, 48 (10):(1679-1686). [PMID:30098001]
3.Jagasia M, Lazaryan A, Bachier CR, Salhotra A, Weisdorf DJ, Zoghi B, Essell J, Green L, Schueller O, Patel J et al.. (2021) ROCK2 Inhibition With Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease.. J Clin Oncol, 39 (17):(1888-1898). [PMID:33877856]
4.Cutler CS, Lee SJ, Arai S, Rotta M, Zoghi B, Lazaryan A, Ramakrishnan A, DeFilipp Z, Salhotra A, Chai-Ho W et al.. (2021) Belumosudil for Chronic Graft-versus-Host Disease (cGVHD) After 2 or More Prior Lines of Therapy: The ROCKstar Study.. Blood, 129 (3):(589-97). [PMID:34265047]
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A2217023