A potent ROCK inhibitor (IC50s = 122

AS-1892802 – 1 mg

Brand:
Cayman
CAS:
928320-12-1
Storage:
-20
UN-No:
Non-Hazardous - /

AS-1892802 is a potent inhibitor of Rho-associated serine-threonine protein kinases (ROCKs; IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively).{40426} It is selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM. However, AS-1892802 inhibits protein kinase catalytic subunit (PKACα) and protein kinase X gene (PRKX) with IC50 values of 200 and 325 nM, respectively. AS-1892802 reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis. It also has analgesic-like effects in a rat model of diabetic neuropathy induced by streptozotocin (Item No. 13104) and reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.{40427,40428}  

 

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Description

A potent ROCK inhibitor (IC50s = 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2, respectively); selective for ROCK1 and 2 over a panel of 167 kinases and a panel of 63 ion channels, receptors, and enzymes at a concentration of 10 μM; inhibits PKACα and PRKX (IC50s = 200 and 325 nM, respectively); reduces weight imbalance deficits (ED50 = 0.15 mg/kg) in rats in a monoiodoacetate-induced model of non-inflammatory arthritis; has analgesic-like effects in a rat model of streptozotocin-induced diabetic neuropathy; reduces cartilage damage and weight imbalance deficits in a rat model of osteoarthritis.,

Formal name: N-[(1S)-2-hydroxy-1-phenylethyl]-N’-[4-(4-pyridinyl)phenyl]-urea

Synonyms: 

Molecular weight: 333.4

CAS: 928320-12-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Immunology & Inflammation|Arthritis (Non-autoimmune)||Research Area|Neuroscience|Pain Research

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