An ATP-competitive inhibitor of ROCK-I and ROCK-II (IC50s = 102 and 276 nM

SAR407899 – 5 mg

Brand:
Cayman
CAS:
923359-38-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

SAR407899 is an ATP-competitive inhibitor of the Rho-associated kinases ROCK-I and ROCK-II (IC50s = 102 and 276 nM, respectively at a concentration of 40 μM ATP).{37269} SAR407899 is selective for ROCK over 79 other kinases at IC50 values up to 10 μM but had IC50 values ranging from 1 to 10 μM for RSK, PKB, PKCδ, and MSK-1. It is also selective for ROCK over 115 receptor and enzyme targets at IC50 values up to 10 μM, but it does inhibit the serotonin transporter and µ-opioid receptors with IC50 values of 1.1 and 8.9 μM, respectively. In vitro, SAR407899 inhibits ROCK-mediated phosphorylation of myosin phosphatase (MYPT), thrombin-induced stress fiber formation, PDGF-induced proliferation, and monocyte chemotactic protein-1-stimulated chemotaxis. SAR407899 relaxes precontracted isolated arteries from various species (IC50s = 122-280 nM) and precontracted corpora cavernosa in both healthy and diabetic animals (IC50s = 0.05-0.42 μM).{37269},{37270} It inhibits constriction of rat and human arteries induced by endothelin-1 (ET-1; Emaxs = 24-83% of control).{37271}  

 

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Description

An ATP-competitive inhibitor of ROCK-I and ROCK-II (IC50s = 102 and 276 nM, respectively at a concentration of 40 μM ATP); selective for ROCK over 79 other kinases at IC50 values up to 10 μM but had IC50 values ranging from 1 to 10 μM for RSK, PKB, PKCδ, and MSK-1; selective for ROCK over 115 receptor and enzyme targets at IC50 values up to 10 μM, but it does inhibit the serotonin transporter and µ-opioid receptors with IC50s values of 1.1 and 8.9 μM, respectively; inhibits ROCK-mediated phosphorylation of MYPT, thrombin-induced stress fiber formation, PDGF-induced proliferation, and MCP-1-stimulated chemotaxis; relaxes precontracted isolated arteries from various species (IC50s = 122-280 nM) and precontracted corpora cavernosa in both healthy and diabetic animals (IC50s = 0.05-0.42 μM); inhibits ET-1-induced constriction of rat and human arteries (Emaxs = 24-83% of control)

Formal name: 6-(4-piperidinyloxy)-1(2H)-isoquinolinone

Synonyms: 

Molecular weight: 244.3

CAS: 923359-38-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation

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