Name: SLx-2119
Price: 278.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SLx-2119(KD-025) is a selective inhibitor of ROCK2 with IC50 of 105 nM [1].Rho-associated protein kinase (ROCK) is a serine-threonine kinase and is involved in regulating cytoskeletal dynamics. It is associated with many intracellular processes, which are relevant to stroke. ROCK2 is the predominant isoform mainly expressed in vasculature and neurons [2].In smooth muscle cells isolated from human intestine with radiation-induced fibrosis (RE-SMC), SLx-2119 reduced mRNA level of CTGF. Over-expression of which is associated with fibrotic diseases. While, in SMC isolated from normal human intestine (N-SMC), SLx-2119 didn’t change CTGF mRNA level [1].In focal cerebral ischemia mice, after transient middle cerebral artery occlusion, KD025 reduced infarct volume in a dose-dependant way. And the efficacy maintained for at least 4 weeks. In aged male and female mice, as well as in type 2 diabetes mice, KD025 reduced infarct volume by 34%, 42% and 32% in aged male mice, female mice and diabetic mice respectively compared to vehicle in mice [2].
    
    [1]. Boerma M, Fu Q, Wang J, 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, 19(7): 709-718.
    [2]. Lee JH, Zheng Y, von Bornstadt D, et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol, 2014, 1(1): 2-14.
- Properties
  - Alternative Name
    
    SLx 2119;SLx2119;ROCK inhibitor;KD-025; 2-(3-(4-((1H-indazol-5-yl)amino)quinazolin-2-yl)phenoxy)-N-isopropylacetamide
    
    CAS Number
    
    911417-87-3
    
    Molecular Formula
    
    C26H24N6O2
    
    Molecular Weight
    
    452.51
    
    Purity
    
    98.29%
    
    Solubility
    
    ≥22.65 mg/mL in DMSO; insoluble in H2O; ≥26.4 mg/mL in EtOH with gentle warming and ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Dale A. Kinzenbaw, Lucy Langmack, et al. "Angiotensin II‐induced endothelial dysfunction: Impact of sex, genetic background, and rho kinase." Physiol Rep. 2022 Jun;10(11):e15336. PMID: 35681278
    2. Wei L, Surma M, et al. "ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice." FASEB J. 2020;34(1):474–493. PMID: 31914704
    3. Nagai Y, Matoba K, et al. "ROCK2 regulates TGF-β-induced expression of CTGF and profibrotic genes via NF-κB and cytoskeleton dynamics in the mesangial cells." Am J Physiol Renal Physiol. 2019 Jul 31. PMID: 31364374
    4. De Silva TM, Modrick ML, et al. "Changes in Cerebral Arteries and Parenchymal Arterioles With Aging: Role of Rho Kinase 2 and Impact of Genetic Background." Hypertension. 2018 Mar 12. pii: HYPERTENSIONAHA.118.10865. PMID: 29531174

SLx-2119

SLx-2119

Background

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