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Ras Signalling Pathway
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ALX-270-423 Revised 11-Oct-06
H-1152 . dihydrochloride
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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
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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
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Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products
 
 
ALX-270-429 Revised 11-Oct-06
3-(4-Pyridyl)-1H-indole
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
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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
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Protein Kinase Inhibitors Other Products
 
 
ALX-270-433 Revised 02-Sep-08
N-(4-Pyridyl)-N’-(2,4,6-trichlorophenyl)urea
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
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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
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Protein Kinase Inhibitors Other Products
 
 
ALX-270-451 Revised 20-Jun-08
HA-1100 . hydrochloride
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SYNONYMS Hydroxyfasudil
1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
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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-290-001 Revised 29-Nov-04
N-Acetyl-S-farnesyl-L-cysteine
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SYNONYMS AFC
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-001-M005   5 mg 50.00 USD Add To Cart
ALX-290-001-M025   25 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C20H33NO3S
MW: 367.6
CAS NUMBER: 135304-07-3
PURITY: ≥97%
APPEARANCE: Clear oil.
SOLUBILITY: Soluble in DMSO, methanol or ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Specific inhibitor of S-farnesylcysteine methyl transferase.
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ALX-290-002 Revised 13-Dec-04
S-Farnesylated Cysteine Tetrapeptide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-002-M001   1 mg 45.00 USD Add To Cart
ALX-290-002-M005   5 mg 150.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Cys(farnesyl)-Val-Ile-Met-OH
FORMULA: C36H62N4O6S2
MW: 711.0
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic. Protect from light and oxygen.
Product Description
Tetrapeptide substrate for the protein endoprotease that cleaves the modified protein at the isoprenylated cysteine residue.
Product Specific Literature References
Inhibitors of the isoprenylated protein endoprotease: Y.-T. Ma, et al.; Biochemistry 32, 2386 (1993) Abstract
 
 
ALX-290-003 Revised 30-Jun-08
Farnesylpyrophosphate . triammonium salt
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SYNONYMS FPP . 3NH4
3,7,11-Trimethyl-2,6,10-dodecatrien-1-ol pyrophosphate . 3NH4
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-003-C200   200 µg 62.00 USD Add To Cart
Product Specification
FORMULA: C15H25O7P2 . 3NH4
MW: 379.3 . 54.1
CAS NUMBER: 13058-04-3
PURITY: ≥98% (TLC)
APPEARANCE: Liquid. Solution in 0.25M ammonium bicarbonate containing 70% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY:

Store solutions at -20°C for up to 3 months.
HANDLING: Protect from light and moisture.

Product Description
Farnesyl donor in enzymatic protein farnesylation catalyzed by farnesyltransferase.
Product Specific Literature References
Tautomycin from the bacterium Streptomyces verticillatus. Another potent and specific inhibitor of protein phosphatases 1 and 2A: C. MacKintosh & S. Klumpp; FEBS Lett. 277, 137 (1990) Abstract
M. Ubukata, et al.; J. C. S. Chem. Commun. 244 (1990)
Divalent cation and prenyl pyrophosphate specificities of the protein farnesyltransferase from rat brain, a zinc metalloenzyme: Y. Reiss, et al.; J. Biol. Chem. 267, 6403 (1992) Abstract; Full Text
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994) Abstract
 
 
ALX-290-004 Revised 25-Oct-06
Farnesylthioacetic acid
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SYNONYMS FTA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-004-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H28O2S
MW: 296.5
CAS NUMBER: 135784-48-4
PURITY: ≥98%
APPEARANCE: Yellow viscous oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 6 months when stored at -20°C. Product is not sterile.
HANDLING: Protect from light.

Product Description
Potent and specific inhibitor of methyl esterification of farnesylated proteins (e.g. the γ subunit of transducin). This compound is not a methyltransferase substrate.
Product Specific Literature References
Identifying the recognition unit for G protein methylation: E.W. Tan, et al.; J. Biol. Chem. 266, 10719 (1991) Abstract; Full Text
 
 
ALX-290-005 Revised 10-Aug-05
Farnesyltransferase Inhibitor
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SYNONYMS B581
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation / Isoprenylation Reagents
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ALX-290-005-M001   1 mg 85.00 USD Add To Cart
ALX-290-005-M005   5 mg 320.00 USD Add To Cart
Product Specification
SEQUENCE: N-[(2S)-((2R)-Amino-3-mercaptopropylamino)-3-methylbutyl]-Phe-Met-OH
FORMULA: C22H38N4O3S2
MW: 470.7
PURITY: ≥96%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.

Product Description
Stable, membrane permeable inhibitor of farnesyltransferase. Has 30-fold higher selectivity for farnesyltransferase over geranylgeranyltransferase. Potential anticancer drug.
Product Specific Literature References
Peptidomimetic inhibitors of Ras farnesylation and function in whole cells: A.M. Garcia, et al.; J. Biol. Chem. 268, 18415 (1993) Abstract; Full Text
 
 
ALX-290-006 Revised 25-Jun-08
Geranylgeranylpyrophosphate . triammonium salt
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SYNONYMS 3,7,11,15-Tetramethyl-2,6,10,14-hexadecatetraenyl pyrophosphate . 3NH3
GGPP . 3NH3
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Geranyl-related Reagents
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ALX-290-006-C200   200 µg 60.00 USD Add To Cart
Product Specification
FORMULA: C20H36O7P2 . 3NH3
MW: 450.5 . 51.1
CAS NUMBER: 6699-20-3
CONCENTRATION: 1mg/ml
PURITY: ≥98%
FORMULATION: Liquid. In 70% ethanol in 0.25M NH4HCO3.
SOLUBILITY: Soluble in water; also soluble in methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL. FLAMMABLE

Product Description
Geranylgeranyl donor utilized by geranylgeranyltransferase for isoprenylation of target proteins.
Product Specific Literature References
Effects of tautomycin, a protein phosphatase inhibitor, on recycling of mammalian cell surface molecules: T. Kurisaki, et al.; J. Antibiot. 45, 252 (1992) Abstract
Steady-state kinetic mechanism of Ras farnesyl:protein transferase: D.L. Pompliano, et al.; Biochemistry 31, 3800 (1992)