An orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM

KD 025 – 10 mg

Brand:
Cayman
CAS:
911417-87-3
Storage:
-20
UN-No:
Non-Hazardous - /

Rho-associated protein kinase II (ROCK-II) regulates the formation of actin stress fibers and focal adhesions, smooth muscle contraction, and gene expression. KD 025 is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).{28734} Treatment of fibrosis-derived smooth muscle cells with KD 025 (40 µM) for 24 hours reduces the expression of connective tissue growth factor and remodels actin cytoskeleton.{28734} KD 025 decreases cell-spanning F-actin fibers and increases motility of microvascular endoethelial cells.{28735} In mice, KD 025 given by oral gavage dose-dependently reduces infarct volume after transient middle cerebral artery occlusion without causing significant hypotension.{28736} In humans, oral KD 025 diminishes STAT3 phosphorylation and pro-inflammatory cytokine production in CD4+ T cells while up-regulating phosphorylation of STAT5 in regulatory T cells, altering the immune response.{27716}  

 

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Description

An orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively); increases motility of microvascular endoethelial cells; alters cell function and inflammatory responses in vivo

Formal name: 2-[3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy]-N-(1-methylethyl)-acetamide

Synonyms:  SLx-2119

Molecular weight: 452.5

CAS: 911417-87-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cytoskeleton & Motor Proteins||Research Area|Immunology & Inflammation|Adaptive Immunity

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