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Kinases / Related Products
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ALX-270-070 Revised 16-Jun-06
HA-1004 . dihydrochloride
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SYNONYMS N-(2'-Guanidinoethyl)-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-070-M005   5 mg 35.00 USD Add To Cart
ALX-270-070-M025   25 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C12H15N5O2S . 2HCl
MW: 293.3 . 73.0
CAS NUMBER: 92564-34-6
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Inhibitor of cAMP- and cGMP-dependent kinases (PKA and PKG). Intracellular Ca2+ antagonist with no effect on cardiac function. Causes selective pulmonary vasodilation during pulmonary hypertension.
Product Specific Literature References
Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C: H. Hidaka, et al.; Biochemistry 23, 5036 (1984) Abstract
Differential effects of isoquinolinesulfonamide protein kinase inhibitors on CA1 responses in hippocampal slices [published erratum appears in Neuroscience 1993 Apr;53(4):1173]: J.C. Leahy & M.L. Vallano; Neuroscience 44, 361 (1991) Abstract
Further Categories Containing This Product:
PKG Inhibitors
 
 
ALX-270-071 Revised 06-Aug-07
HA-1077 . dihydrochloride
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SYNONYMS Fasudil
1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Rho-associated Protein Kinases [ROCK] / Related Products
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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-350-029 Revised 07-Oct-08
Herbimycin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Protein Kinase Inhibitors
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ALX-350-029-C100   100 µg 110.00 USD Add To Cart
ALX-350-029-M001   1 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C30H42N2O9
MW: 574.7
CAS NUMBER: 70563-58-5
RTECS: LX8930000
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥97%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Antibiotic. Cell permeable tyrosine kinase inhibitor. Inhibitor of HSP90, NF-κB activation and angiogenesis. Increases the sensitivity of certain cancer cells to chemotherapeutic agents. Blocks mitotic activity. Neurotoxic.
Product Specific Literature References
Herbimycin, a new antibiotic produced by a strain of Streptomyces: S. Omura, et al.; J. Antibiot. (Tokyo) 32, 255 (1979) Abstract
A new activity of herbimycin A: inhibition of angiogenesis: T. Yamashita, et al.; J. Antibiot. (Tokyo) 42, 1015 (1989) Abstract
Stimulation by Bt2cAMP of epidermal mucous metaplasia in retinol- pretreated chick embryonic cultured skin, and its inhibition by herbimycin A, an inhibitor for protein-tyrosine kinase: A. Obinata, et al.; Exp. Cell. Res. 193, 36 (1991) Abstract
IgE-induced tyrosine phosphorylation of phospholipase C-gamma 1 in rat basophilic leukemia cells: D.J. Park, et al.; J. Biol. Chem. 266, 24237 (1991) Abstract; Full Text
Bacterial lipopolysaccharide stimulates protein tyrosine phosphorylation in macrophages: S.L. Weinstein, et al.; PNAS 88, 4148 (1991) Abstract
Inhibition of interleukin 3 and granulocyte-macrophage colony- stimulating factor stimulated increase of active ras.GTP by herbimycin A, a specific inhibitor of tyrosine kinases: T. Satoh, et al.; J. Biol. Chem. 267, 2537 (1992) Abstract; Full Text
New insight into oncoprotein-targeted antitumor effect: herbimycin A as an antagonist of protein tyrosine kinase against Ph1-positive leukemia cells: M. Okabe and M. Uehara; Leuk. Lymphoma 12, 41 (1993) Abstract
Prevention of anti-CD3 monoclonal antibody-induced thymic apoptosis by protein tyrosine kinase inhibitors: K. Migita, et al.; J. Immunol. 153, 3457 (1994) Abstract
Inhibition of heat shock protein HSP90-pp60v-src heteroprotein complex formation by benzoquinone ansamycins: essential role for stress proteins in oncogenic transformation: L. Whitesell, et al.; PNAS 91, 8324 (1994) Abstract; Full Text
Inhibition of PDGF-induced phospholipase D but not phospholipase C activation by herbimycin A: B.Y. Kim; BBRC 212, 1061 (1995) Abstract
Controlling the vasculature: angiogenesis, anti-angiogenesis and vascular targeting of gene therapy: T.-P.D. Fan, et al.; TIPS 16, 57 (1995), (Review) Abstract
Herbimycin A enhances apoptotic effect of chemotherapeutic drugs on K562 cells: H. Ren, et al.; Chin. Med. J. (Engl.) 111, 678 (1998) Abstract
Hsp-90-associated oncoproteins: multiple targets of geldanamycin and its analogs: M.V. Blagosklonny; Leukemia 16, 455 (2002) Abstract; Full Text
Geldanamycin and herbimycin A induce apoptotic killing of B chronic lymphocytic leukemia cells and augment the cells’ sensitivity to cytotoxic drugs: D.T. Jones, et al.; Blood 103, 1855 (2004) Abstract; Full Text
Herbimycin A abrogates nuclear factor-kappaB activation by interacting preferentially with the IkappaB kinase beta subunit: S. Ogino, et al.; Mol. Pharmacol. 65, 1344 (2004) Abstract; Full Text
Herbimycin A suppresses mitotic activity and egg production of female Schistosoma mansoni: J. Knobloch, et al.; Int. J. Parasitol. 36, 1261 (2006) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Neurotoxins • Phospholipase D / Related Products • Antibiotics for Angiogenesis Research • HSP90 / HtpG / Related Products
 
 
ALX-340-037 Revised 08-Jul-08
8(S)-HETE
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SYNONYMS 8-Hydroxy-[S-(E,Z,Z,Z)]-5,9,11,14-eicosatetraenoic acid
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Hydroxy, Hydroperoxy & Oxo Fatty Acids / Related Products
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ALX-340-037-C025   25 µg 165.00 USD Add To Cart
Product Specification
FORMULA: C20H32O3
MW: 320.5
CAS NUMBER: 98462-03-4
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in PBS, pH 7.2 (0.8mg/ml) or 0.1M Na2CO3 (2mg/ml)
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Stable for at least 6 months in other organic solvents when stored at -20°C. Keep aqueous solutions on ice and use within 12 hours.
HANDLING: Protect from light and oxygen.

Product Description
Activator of PPARα. Activates mouse skin protein kinase C (PKC).
Product Specific Literature References
Investigation of the mechanism of biosynthesis of 8-hydroxyeicosatetraenoic acid in mouse skin: M.A. Hughes & A.R. Brash; Biochim. Biophys. Acta 1081, 347 (1991) Abstract
In vitro activation of mouse skin protein kinase C by fatty acids and their hydroxylated metabolites: H.H. Lo, et al.; Lipids 29, 547 (1994) Abstract
Differential activation of peroxisome proliferator-activated receptors by eicosanoids: K. Yu, et al.; J. Biol. Chem. 270, 23975 (1995) Abstract; Full Text
Expression of peroxisome proliferator-activated receptors in urinary tract of rabbits and humans: Y. Guan, et al.; Am. J. Physiol. 273, F1013 (1997) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
PPAR Agonists • PKC Activators
 
 
ALX-300-084 Revised 02-Dec-04
1-O-Hexadecyl-2-O-methyl-rac-glycerol
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Mono- & Diacylglycerols
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ALX-300-084-M250   250 mg 45.00 USD Add To Cart
ALX-300-084-G001   1 g 150.00 USD Add To Cart
Product Specification
FORMULA: C20H42O3
MW: 330.6
CAS NUMBER: 111188-59-1
PURITY: ≥97%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
Product Description
Inhibitor of protein kinase C (PKC).
Product Specific Literature References
1-O-hexadecyl-2-Q-methylglycerol, a novel inhibitor of protein kinase C, inhibits the respiratory burst in human neutrophils: I.M. Kramer, et al.; J. Biol. Chem. 264, 5876 (1989) Abstract; Full Text
Further Categories Containing This Product:
PKC Inhibitors
 
 
ALX-300-093 Revised 23-Mar-05
Hexadecyl-phosphocholine (C16:0)
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SYNONYMS Miltefosine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-093-M250   250 mg 50.00 USD Add To Cart
ALX-300-093-G001   1 g 150.00 USD Add To Cart
Product Specification
FORMULA: C21H46NO4P
MW: 407.6
CAS NUMBER: 58066-85-6
MERCK INDEX: 14: 6198
PURITY: ≥99%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Potent antitumor agent. Inhibitor of protein kinase C (PKC) and phosphatidylcholine biosynthesis. Costimulates human T cell activation.
Product Specific Literature References
H.R. Berger, et al.; Akt. Onkologie 34, 27 (1987)
The phospholipid analogue, hexadecylphosphocholine, inhibits protein kinase C in vitro and antagonises phorbol ester-stimulated cell proliferation: C.C. Geilen, et al.; Eur. J. Cancer 27, 1650 (1991) Abstract
The phospholipid analogue hexadecylphosphocholine inhibits phosphatidylcholine biosynthesis in Madin-Darby canine kidney cells: R. Haase, et al.; FEBS Lett. 288, 129 (1991) Abstract
Hexadecylphosphocholine-mediated enhancement of T-cell responses to interleukin 2: K. Vehmeyer, et al.; Cellular Immunology 137, 232 (1991) Abstract
Further Categories Containing This Product:
PKC Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Parasitic Diseases Other Products
 
 
ALX-158-001 Revised 28-Feb-06
Histone H1-7 Substrate
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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ALX-158-001-M001   1 mg 70.00 USD Add To Cart
ALX-158-001-M005   5 mg 280.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Arg-Lys-Ala-Ser-Gly-Pro-OH
FORMULA: C31H58N14O9
MW: 770.9
PURITY: ≥98%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cAMP-dependent protein kinase (PKA). The peptide is derived from the phosphorylation site (Ser38) in calf thymus histone H1.
Product Specific Literature References
Studies on the mechanism of phosphorylation of synthetic polypeptides by a calf thymus cyclic AMP-dependent protein kinase: A.H. Pomerantz, et al.; PNAS 74, 4261 (1977) Abstract
Further Categories Containing This Product:
Peptides • PKA Substrates
 
 
ALX-158-003 Revised 04-Jul-03
Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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ALX-158-003-M001   1 mg 50.00 USD Add To Cart
ALX-158-003-M005   5 mg 200.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ser-Arg-Lys-Glu-OH
FORMULA: C38H74N18O11
MW: 959.1
PURITY: ≥97%
APPEARANCE: White powder.
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for cGMP-dependent protein kinase corresponding to residues 29-35 of histone H2B. For the corresponding alanine-for-serine substituted peptides see Prod. No. ALX-158-002 and Prod. No. ALX-158-004.
Product Specific Literature References
Comparison of the substrate specificity of adenosine 3':5'- monophosphate- and guanosine 3':5'-monophosphate-dependent protein kinases. Kinetic studies using synthetic peptides corresponding to phosphorylation sites in histone H2B: D.B. Glass & E.G. Krebs; J. Biol. Chem. 254, 9728 (1979) Abstract; Full Text
Further Categories Containing This Product:
PKG Substrates • Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products • Peptides
 
 
ALX-158-002 Revised 28-Feb-06
[Ala32]-Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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ALX-158-002-M001   1 mg 75.00 USD Add To Cart
ALX-158-002-M005   5 mg 300.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Lys-Arg-Ala-Arg-Lys-Glu-OH
FORMULA: C38H74N18O10
MW: 943.1
PURITY: ≥97%
APPEARANCE: White lyophilized powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Inhibitor of cGMP-dependent protein kinase, derived by a serine-to-alanine substitution at position 32 of histone H2B (29-35). For the corresponding unsubstituted histone fragment see Prod. No. ALX-158-003.
Product Specific Literature References
D.B. Glass & M.D. Miller; Fed. Proc. 39, 867 (1980)
Differential responses of cyclic GMP-dependent and cyclic AMP-dependent protein kinases to synthetic peptide inhibitors: D.B. Glass; Biochem. J. 213, 159 (1983) Abstract
Further Categories Containing This Product:
Peptides • PKG Inhibitors
 
 
ALX-158-004 Revised 13-Jan-05
[Ala34]-Histone H2B (29-35)
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Histones / Related Products
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ALX-158-004-M001   1 mg 60.00 USD Add To Cart
ALX-158-004-M005   5 mg 240.00 USD Add To Cart