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

SAR407899 – 25 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}  

 

Out of stock

Add to quotes
SKU: 21717 - Category:

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

Related products

  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 100 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 100 µg

    Available on backorder

    Add to quotes
    View product page
  • CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}

    CAY10512 – 500 mg

    The nuclear factor-κB (NF-κB) regulates the expression of numerous genes involved in immunity and inflammation, cellular stress responses, growth, and apoptosis. Resveratrol, a polyphenolic trans-stilbene, is a known inhibitor of the activation of NF-κB and exhibits activity against a wide variety of cancer cells. CAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.{14545}  

     

    Brand:
    Cayman
    SKU:10009536 - 500 mg

    Available on backorder

    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 1 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 1 mg

    Available on backorder

    Add to quotes
    View product page
  • PtdIns-(3

    PtdIns-(3,4,5)-P3-biotin (sodium salt) – 10 µg

    The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.  

     

    Brand:
    Cayman
    SKU:10009531 - 10 µg

    Available on backorder

    Add to quotes
    View product page