A potent inhibitor of ROCK-II

HA-1077 (hydrochloride) – 100 mg

Brand:
Cayman
CAS:
203911-27-7
Storage:
-20
UN-No:
Non-Hazardous - /

Rho-associated kinase (ROCK), an effector of the small GTP-binding protein Rho, plays an important role in various cellular functions including vascular smooth muscle contraction, proliferation, and migration as well as inflammatory cell mobility.{16260} HA-1077 is a potent inhibitor of ROCK-II and additionally inhibits protein kinase c-related kinase 2 (PRK2), mitogen- and stress-activated protein kinase (MSK1), and mitogen activated protein kinase-activated protein kinase 1b (MAPKAP-K1b) with IC50 values of 1.9, 4, 5, and 15 µM, respectively.{12847} By inhibiting the activity of ROCK, HA-1077 has been shown to reduce blood vessel constriction, decrease pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in various rodent models.{16259,16257,16258} While originally marketed for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage, oral formulations of HA-1077 are used for the treatment of a wide range of cardiovascular diseases including pulmonary arterial hypertension and stable angina.  

 

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SKU: 10010559 - 100 mg Category:

Description

A potent inhibitor of ROCK-II, PRK-2, MSK1, and MAPKAP-K1b with IC50 values of 1.9, 4, 5, and 15 µM, respectively; has been shown to reduce blood vessel constriction, decreases pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in a diabetic rat model; drug forms are marketed for the treatment of pulmonary arterial hypertension and stable angina

Formal name: hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine, dihydrochloride

Synonyms:  Fasudil

Molecular weight: 364.3

CAS: 203911-27-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Kinase Inhibitors|S6K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|ROCK Signaling||Research Area|Cancer|Cell Signaling|S6K Signaling||Research Area|Cardiovascular System|Cardiovascular Diseases|Angina||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Cell Signaling|ERK/MAPK Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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