• Home
  • Sitemap
  • Help
  • Technical Support
  • Contact
Rho-associated Protein Kinases [ROCK] / Related Products
You are here: Product Lines > Signal Transduction > Ras Signalling Pathway > Rho-associated Protein Kinases [ROCK] / Related Products
Toolbar - View Selection
 
Items 6 of 6
ALX-270-423 Revised 11-Oct-06
H-1152 . dihydrochloride
Add to Clipboard
SYNONYMS H-1152P . 2HCl
(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-423-M001   1 mg 95.00 USD Add To Cart
ALX-270-423-M005   5 mg 380.00 USD Add To Cart
ALX-270-423-M025   25 mg 1'100.00 USD Add To Cart
Product Specification
FORMULA: C16H21N3O2S . 2HCl
MW: 319.4 . 73.0
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic. Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR and 13C-NMR.

Product Description
A cell permeable, highly specific, potent and ATP-competitive inhibitor of Rho kinase (ROCK) (Ki=1.6nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki=630nM for PKA, 9.27mM for PKC and 10.1mM for MLCK). More potent and selective than Y-27632 (Prod. No. ALX-270-333). Inhibits the phosphorylation of MARCKS in cells stimulated by lysophosphatidic acid. Inhibits EP3-stimulated NO formation. Prevents fragmentation of apoptotic cells. Relieves neuropathic pain.
Product Specific Literature References
Inhibition of rho-kinase-induced myristoylated alanine-rich C kinase substrate (MARCKS) phosphorylation in human neuronal cells by H-1152, a novel and specific Rho-kinase inhibitor: M. Ikenoya, et al.; J. Neurochem. 81, 9 (2002) Abstract
The novel and specific Rho-kinase inhibitor (S)-(+)-2-methyl-1-[(4-methyl-5-isoquinoline)sulfonyl]-homopiperazine as a probing molecule for Rho-kinase-involved pathway: Y. Sasaki, et al.; Pharmacol. Ther. 93, 225 (2002) Abstract
New aspects of neurotransmitter release and exocytosis: Rho-kinase-dependent myristoylated alanine-rich C-kinase substrate phosphorylation and regulation of neurofilament structure in neuronal cells: Y. Sasaki; J. Pharmacol. Sci. 93, 35 (2003) Abstract
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity: C. Breitenlechner, et al.; Structure 11, 1595 (2003) Abstract
Involvement of Rho-kinase in inflammatory and neuropathic pain through phosphorylation of myristoylated alanine-rich C-kinase substrate (MARCKS): S. Tatsumi, et al.; Neuroscience 131, 491 (2005) Abstract
Rho-kinase mediates spinal nitric oxide formation by prostaglandin E2 via EP3 subtype: S. Matsumura, et al.; BBRC 338, 550 (2005) Abstract
Rho kinase regulates fragmentation and phagocytosis of apoptotic cells: K.A. Orlando, et al.; Exp. Cell Res. 312, 5 (2006) Abstract
Direct Rho-associated kinase inhibiton induces cofilin dephosphorylation and neurite outgrowth in PC-12 cells: Z. Zhang, et al.; Cell. Mol. Biol. Lett. 11, 12 (2006) Abstract
Regulation of the crossbridge cycle in vascular smooth muscle by cAMP signalling: G. Pfitzer, et al.; J. Muscle Res. Cell. Motil. 27, 445 (2006) Abstract
Involvement of ROCK-mediated endothelial tension development in neutrophil-stimulated microvascular leakage: J.W. Breslin, et al.; Am. J. Physiol. Heart Circ. Physiol. 290, H741 (2006) Abstract
Related Products
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products
 
 
ALX-270-451 Revised 20-Jun-08
HA-1100 . hydrochloride
Add to Clipboard
SYNONYMS Hydroxyfasudil
1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-451-M001   1 mg 40.00 USD Add To Cart
ALX-270-451-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C14H17N3O3S . HCl
MW: 307.4 . 36.5
CAS NUMBER: 105628-72-6
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (20mM, warm).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to one month when stored at -20°C. However it is recommended to prepare fresh solutions if possible.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Packaged under inert gas.

Product Description
Cell permeable, hydroxylated metabolite of HA-1077 . 2HCl (Fasudil) (Prod. No. ALX-270-071) that displays anti-anginal properties. Acts as an ATP-competitive and reversible inhibitor of Rho kinase (ROCK) with ~100-fold greater selectivity over MLCK, MRCKβ and PKC. Inhibits coronary arteriosclerotic lesion formation. Increases osteocalcin expression and has beneficial effects on pulmonary hypertension.
Product Specific Literature References
Rho-kinase-mediated pathway induces enhanced myosin light chain phosphorylations in a swine model of coronary artery spasm: H. Shimokawa, et al.; Cardiovasc. Res. 43, 1029 (1999) Abstract
Hydroxyfasudil, an active metabolite of fasudil hydrochloride, relaxes the rabbit basilar artery by disinhibition of myosin light chain phosphatase: K. Nakamura, et al.; J. Cereb. Blood Flow Metab. 21, 876 (2001) Abstract
Pitavastatin enhanced BMP-2 and osteocalcin expression by inhibition of Rho-associated kinase in human osteoblasts: K. Ohnaka, et al.; BBRC 287, 337 (2001) Abstract
Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina: T. Utsunomiya, et al.; Br. J. Pharmacol. 134, 1724 (2001) Abstract
Rho-kinase mediates hypoxia-induced downregulation of endothelial nitric oxide synthase: M. Takemoto, et al.; Circulation 106, 57 (2002) Abstract
Rho-kinase as a novel therapeutic target in treatment of cardiovascular diseases: H. Shimokawa; J. Cardiovasc. Pharmacol. 39, 319 (2002) Abstract
Essential role of rho kinase in the Ca2+ sensitization of prostaglandin F(2alpha)-induced contraction of rabbit aortae: K. Ito, et al.; J. Physiol. 546, 823 (2003) Abstract
Inhibition of Rho-kinase leads to rapid activation of phosphatidylinositol 3-kinase/protein kinase Akt and cardiovascular protection: S. Wolfrum, et al.; Arterioscler. Thromb. Vasc. Biol. 24, 1842 (2004) Abstract
Beneficial effect of hydroxyfasudil, a specific Rho-kinase inhibitor, on ischemia/reperfusion injury in canine coronary microcirculation in vivo: T. Yada, et al.; J. Am. Coll. Cardiol. 45, 599 (2005) Abstract
Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection: Y. Rikitake, et al.; Stroke 36, 2251 (2005) Abstract
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity: M. Jacobs, et al.; J. Biol. Chem. 281, 260 (2006) Abstract
Sustained Elevation of Serum Cortisol Level Causes Sensitization of Coronary Vasoconstricting Responses in Pigs In Vivo. A Possible Link Between Stress and Coronary Vasospasm: T. Hizume, et al.; Circ. Res. 99, 767 (2006) Abstract; Full Text
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products
 
 
ALX-270-071 Revised 06-Aug-07
HA-1077 . dihydrochloride
Add to Clipboard
SYNONYMS Fasudil
1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-071-M001   1 mg 21.00 USD Add To Cart
ALX-270-071-M005   5 mg 63.00 USD Add To Cart
Product Specification
FORMULA: C14H17N3O2S . 2HCl
MW: 291.4 . 73.0
CAS NUMBER: 103745-39-7
MERCK INDEX: 14: 3942
PURITY: ≥98%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in water, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ.  Cell permeable Ca2+ antagonist with antivasospastic properties.
Product Specific Literature References
The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs: O. Shibuya, et al.; Acta Neurochir. 90, 53 (1988) Abstract
Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase: T. Asano, et al.; Br. J. Pharmacol. 98, 1091 (1989) Abstract
Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator: Y. Sasaki & Y. Sasaki; BBRC 171, 1182 (1990) Abstract
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle: M. Seto, et al.; Eur. J. Pharmacol. 195, 267 (1991) Abstract
A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture: M. Shirotani, et al.; J. Pharmacol. Exp. Ther. 259, 738 (1991) Abstract
Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle: S. Takizawa, et al.; Eur. J. Pharmacol. 250, 431 (1993) Abstract
Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells: H. Nagumo, et al.; Am. J. Physiol. Cell. Physiol. 278, C57 (2000) Abstract
Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCbetaI, PKCbetaII and PKCzeta in human neutrophils: X. Siomboing, et al.; Mediators Inflamm. 10, 315 (2001) Abstract
Effects of HA-1077 and Y-27632, Two Rho-Kinase Inhibitors, in the Human Umbilical Artery: M. Ark, et al.; Cell Biochem. Biophys. 41, 331 (2004) Abstract
Further Categories Containing This Product:
CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
ALX-270-433 Revised 02-Sep-08
N-(4-Pyridyl)-N’-(2,4,6-trichlorophenyl)urea
Add to Clipboard
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-433-M005   5 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C12H8Cl3N3O
MW: 316.6
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light.
IDENTITY: Identity determined by NMR.

Product Description
Potent, selective, and ATP-competitive inhibitor of Rho kinase (ROCK) (IC50=0.2 µM).
Product Specific Literature References
Design and synthesis of Rho kinase inhibitors (I): A. Takami, et al.; Bioorg. Med. Chem. 12, 2115 (2004) Abstract
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products
 
 
ALX-270-429 Revised 11-Oct-06
3-(4-Pyridyl)-1H-indole
Add to Clipboard
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-429-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C13H10N2
MW: 194.2
CAS NUMBER: 7272-84-6
PURITY: ≥98% (TLC)
APPEARANCE: Off-white to beige solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: Protect from light.

Product Description
A cell permeable, selective, and ATP-competitive inhibitor of Rho kinase (ROCK) activity (IC50=25µM). Does not inhibit the activation of Rho nor does it affect the in vitro activities of MLCK, PKCα, and SAPK2a/p38α. Shown to be less potent than Y-27632 (Prod. No. ALX-270-333).
Product Specific Literature References
Screening for cell migration inhibitors via automated microscopy reveals a Rho-kinase inhibitor: J.C. Yarrow, et al.; Chem. Biol. 12, 385 (2005) Abstract
Scratch n’ screen for inhibitors of cell migration: J. Soderholm & R. Heald; Chem. Biol. 12, 263 (2005) Abstract
Related Products
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products
 
 
ALX-270-333 Revised 18-Jan-08
Y-27632 . dihydrochloride
Add to Clipboard
SYNONYMS (R)-(+)-trans-N-(4-Pyridyl)-4-(1-aminoethyl)-cyclohexanecarboxamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-333-M001   1 mg 90.00 USD Add To Cart
ALX-270-333-M005   5 mg 360.00 USD Add To Cart
ALX-270-333-M025   25 mg 1'080.00 USD Add To Cart
Product Specification
FORMULA: C14H21N3O . 2HCl
MW: 247.3 . 73.0
CAS NUMBER: 146986-50-7
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
PURITY DETAIL: Enantiomeric excess ≥96%
SOLUBILITY: Soluble in water (warm, sonication).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING: Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light.
HAZARD: HARMFUL.

Product Description
Highly potent, cell permeable, selective and ATP competitive inhibitor of ROCK1 and ROCK2 (IC50=800nM). Acts as a potent inhibitor of agonist-induced Ca2+ sensitization of myosin phosphorylation and smooth muscle contractions. Blocks cell spreading and suppresses RhoA-induced formation of stress fibers in hepatic stellate cells. Significantly reduces the increase of inflammatory cytokines after reperfusion, preventing the development of acute renal failure. Produces cardioprotective effects. Suppresses tumor cell invasion. Inhibits superoxide production, intrahepatic metastasis of human hepatocellular carcinoma as well as high K+-induced contractions in vascular smooth muscle. Mimics effects of β-agonists on human cells. Has antinociceptive effect.
Product Specific Literature References
Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension: M. Uehata, et al.; Nature 389, 990 (1997) Abstract
Molecular dissection of the Rho-associated protein kinase (p160ROCK)-regulated neurite remodeling in neuroblastoma N1E-115 cells: M. Hirose, et al.; J. Cell Biol. 141, 1625 (1998) Abstract
Signaling from Rho to the actin cytoskeleton through protein kinases ROCK and LIM-kinase: M. Maekawa, et al.; Science 285, 895 (1999) Abstract
Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000) Abstract; Full Text
Use and properties of ROCK-specific inhibitor Y-27632: S. Narumiya, et al.; Meth. Enzymol. 325, 273 (2000) Abstract
Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases: T. Ishizaki, et al.; Mol. Pharmacol. 57, 976 (2000) Abstract
A p160ROCK-specific inhibitor, Y-27632, attenuates rat hepatic stellate cell growth: H. Iwamoto, et al.; J. Hepatol. 32, 762 (2000) Abstract
Y-27632, an inhibitor of rho-associated protein kinase, suppresses tumor cell invasion via regulation of focal adhesion and focal adhesion kinase: F. Imamura, et al.; Jpn. J. Cancer Res. 91, 811 (2000) Abstract
The effect of a Rho kinase inhibitor Y-27632 on superoxide production, aggregation and adhesion in human polymorphonuclear leukocytes: A. Kawaguchi, et al.; Eur. J. Pharmacol. 403, 203 (2000) Abstract
Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxide-independent pathway: K. Chitaley, et al.; Nat. Med. 7, 119 (2001) Abstract
Inhibition of intrahepatic metastasis of human hepatocellular carcinoma by Rho-associated protein kinase inhibitor Y-27632: M. Takamura, et al.; Hepatology 33, 577 (2001) Abstract
Inhibition of high K+-induced contraction by the ROCKs inhibitor Y-27632 in vascular smooth muscle: possible involvement of ROCKs in a signal transduction pathway: K. Sakamoto, et al.; J. Pharmacol. Sci. 92, 56 (2003) Abstract
Comparison of effects of Y-27632 and Isoproterenol on release of cytokines from human peripheral T cells: M. Aihara, et al.; Int. Immunopharmacol. 3, 1619 (2003) Abstract
Y-27632, a Rho-kinase inhibitor, inhibits proliferation and adrenergic contraction of prostatic smooth muscle cells: R.W. Rees, et al.; J. Urol. 170, 2517 (2003) Abstract
Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity: C. Breitenlechner, et al.; Structure 11, 1595 (2003) Abstract
Preventive effect of Y-27632, a selective Rho-kinase inhibitor, on ischemia/reperfusion-induced acute renal failure in rats: K. Teraishi, et al.; Eur. J. Pharmacol. 505, 205 (2004) Abstract
Rho-kinase inhibitor, Y-27632, has an antinociceptive effect in mice: K. Buyukafsar, et al.; Eur. J. Pharmacol. 541, 49 (2006) Abstract
Structural basis for induced-fit binding of Rho-kinase to the inhibitor Y-27632: H. Yamaguchi, et al.; J. Biochem (Tokyo) 140, 305 (2006) Abstract
Molecular characterization of the effects of Y-27632: H. Darenfed, et al.; Cell Motil. Cytoskeleton (2006) Abstract
A Rho-kinase inhibitor, Y-27632, reduces cholinergic contraction but not neurotransmitter release: L. Fernandes, et al.; Eur. J. Pharmacol. 550, 155 (2006) Abstract
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products • Myosins Other Products • Analgesic / Anti-nociceptive Agents / Related Products
 
 
© 2008 ALEXIS Corporation, Privacy Policy, Disclaimer, Feedbackheader picture © micronaut.ch, another CS2 website

Catalogs / Brochures

E-Newsletter

 

Shopping Cart [0]

 

Distributors

Online Product Ordering

Clipboard [0]

Your items will be kept only for the duration of your visit.