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Kinases / Related Products
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ALX-270-055 Revised 07-Dec-04
Bisindolylmaleimide VII
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-055-M001   1 mg 45.00 USD Add To Cart
ALX-270-055-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C27H27N5O2
MW: 453.5
CAS NUMBER: 137592-47-3
PURITY: ≥96%
APPEARANCE: Orange solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective inhibitor of protein kinase C (PKC).
 
 
ALX-270-056 Revised 18-Jan-08
Bisindolylmaleimide VIII . acetate
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SYNONYMS Ro 31-7549 . acetate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-056-M001   1 mg 45.00 USD Add To Cart
ALX-270-056-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C24H22N4O2 . CH3COOH
MW: 398.5 . 60.1
CAS NUMBER: 138516-31-1
PURITY: ≥98%
APPEARANCE: Red powder.
SOLUBILITY: Soluble in DMSO, methanol or water; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective inhibitor of protein kinase C (PKC). Enhances Fas- and TRAIL-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
Product Specific Literature References
Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases: T. Zhou, et al.; Nat. Med. 5, 42 (1999) Abstract
Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways: T. Ohtsuka & T. Zhou; J. Biol. Chem. 277, 29294 (2002) Abstract; Full Text
Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors: D. Brehmer, et al.; Mol. Cell Proteomics 3, 490 (2004) Abstract; Full Text
 
 
ALX-270-057 Revised 18-Jan-08
Bisindolylmaleimide X . hydrochloride
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SYNONYMS Ro 31-8425 . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-057-M001   1 mg 45.00 USD Add To Cart
ALX-270-057-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C26H24N4O2 . HCl
MW: 424.5 . 36.5
PURITY: ≥98%
APPEARANCE: Red solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective inhibitor of protein kinase C (PKC).
Product Specific Literature References
Proteome-wide identification of cellular targets affected by bisindolylmaleimide-type protein kinase C inhibitors: D. Brehmer, et al.; Mol. Cell Proteomics 3, 490 (2004) Abstract; Full Text
 
 
ALX-270-058 Revised 28-May-08
Bisindolylmaleimide XI . hydrochloride
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SYNONYMS Ro 32-0432 . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-058-M001   1 mg 45.00 USD Add To Cart
ALX-270-058-M005   5 mg 150.00 USD Add To Cart
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Product Specification
FORMULA: C28H28N4O2 . HCl
MW: 452.6 . 36.5
PURITY: ≥98% (NMR)
APPEARANCE: Orange to brown red solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selective inhibitor of protein kinase C (PKC).
 
 
ALX-270-097 Revised 07-Sep-06
Ebselen
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SYNONYMS 2-Phenyl-1,2-benzisoselenazol-3-(2H)-one
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Peroxynitrite / Scavengers / Detection
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ALX-270-097-M001   1 mg 12.00 USD Add To Cart
ALX-270-097-M005   5 mg 20.00 USD Add To Cart
ALX-270-097-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C13H9NOSe
MW: 274.2
CAS NUMBER: 60940-34-3
PURITY: ≥98% (NMR)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase. Anti-inflammatory antioxidant. Mimics glutathione peroxidase. Inhibits oxidative modifications of low density lipoproteins (LDL).
Product Specific Literature References
A novel biologically active seleno-organic compound--III. Effects of PZ 51 (Ebselen) on glutathione peroxidase and secretory activities of mouse macrophages: M.J. Parnham & S. Kindt; Biochem. Pharmacol. 33, 3247 (1984) Abstract
Seleno-organic compounds and the therapy of hydroperoxide-linked pathological conditions: M.J. Parnham & E. Graf; Biochem. Pharmacol. 36, 3095 (1987) Abstract
Kinetic mechanism and substrate specificity of glutathione peroxidase activity of ebselen (PZ51): M. Maiorino, et al.; Biochem. Pharmacol. 37, 2267 (1988) Abstract
Studies on the anti-inflammatory activity of ebselen. Ebselen interferes with granulocyte oxidative burst by dual inhibition of NADPH oxidase and protein kinase C?: I.A. Cotgreave, et al.; Biochem. Pharmacol. 38, 649 (1989) Abstract
T. Nikawa, et al.; Biochem. Pharmacol. 47, 1007 (1994) Abstract
Effects of ebselen and probucol on oxidative modifications of lipid and protein of low density lipoprotein induced by free radicals: N. Noguchi, et al.; Biochim. Biophys. Acta 1213, 176 (1994) Abstract
Strong inhibition of mammalian lipoxygenases by the antiinflammatory seleno-organic compound ebselen in the absence of glutathione: C. Schewe, et al.; Biochem. Pharmacol. 48, 65 (1994) Abstract
Ebselen: a glutathione peroxidase mimic: H. Sies; Meth. Enzymol. 234, 476 (1994) Abstract
Molecular actions of ebselen-an antiinflammatory antioxidant: T. Schewe; Gen. Pharmacol. 26, 1153 (1995) Abstract
Ebselen: H. Sies; Meth. Enzymol. 252, 341 (1995) Abstract
Ebselen as a glutathione peroxidase mimic and as a scavenger of peroxynitrite: H. Sies & H. Masumoto; Adv. Pharmacol. 38, 229 (1997) Abstract
Free radical generation by selenium compounds and their prooxidant toxicity: J.E. Spallholz; Biomed. Environ. Sci. 10, 260 (1997) Abstract
Protection against peroxynitrite by selenoproteins: H. Sies, et al.; Z. Naturforsch. [C] 53, 228 (1998) Abstract
Ebselen protects mice against T cell-dependent, TNF-mediated apoptotic liver injury: G. Tiegs, et al.; J. Pharmacol. Exp. Ther. 287, 1098 (1998) Abstract; Full Text
Further Categories Containing This Product:
Antioxidants, Flavonoids & Free Radical Scavengers Other Products • PKC Inhibitors • Malaria / Related Products • Lipoxygenases / Related Products • Anti-inflammatory Agents Other Products • COX Inhibitors
 
 
ALX-270-104 Revised 21-Mar-07
NPC-15437 . dihydrochloride
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SYNONYMS (S)-2,6-diamino-N-{[1'-(1''-oxotridecyl)-2'-piperidinyl]methyl}hexanamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-104-M001   1 mg 90.00 USD Add To Cart
ALX-270-104-M005   5 mg 350.00 USD Add To Cart
Product Specification
FORMULA: C25H50N4O2 . 2 HCl
MW: 438.7 . 73.0
CAS NUMBER: 136449-85-9; 141774-20-1
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water, DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Hygroscopic.

Product Description
Selective inhibitor of protein kinase C (PKC).
Product Specific Literature References
NPC 15437 interacts with the C1 domain of protein kinase C. An analysis using mutant PKC constructs: J.P. Sullivan, et al.; FEBS Lett. 285, 120 (1991) Abstract
2,6-Diamino-N-([1-oxotridecyl)-2-piperidinyl]methyl)hexanamide (NPC 15437): a selective inhibitor of protein kinase C: J.P. Sullivan, et al.; Agents Actions 34, 142 (1991) Abstract
2,6-Diamino-N-([1-(1-oxotridecyl)-2-piperidinyl] methyl)hexanamide (NPC 15437): a novel inhibitor of protein kinase C interacting at the regulatory domain: J.P. Sullivan, et al.; Mol. Pharmacol. 41, 38 (1992) Abstract
 
 
ALX-270-113 Revised 08-Apr-08
Phloretin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-270-113-M100   100 mg 37.00 USD Add To Cart
Product Specification
FORMULA: C15H14O5
MW: 274.3
CAS NUMBER: 60-82-2
MERCK INDEX: 14: 7326
PURITY: ≥98%
APPEARANCE: Off-white to beige solid.
SOLUBILITY: Soluble in acetone, DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Flavonoid. Protein kinase C (PKC) inhibitor. PGF2a receptor antagonist. In astrocytes, these receptors are linked to phospholipase C, thus affecting phosphoinositide hydrolysis and intracellular Ca2+ levels. Inhibits myo-inositol uptake and 5’-iodothyronine deiodinase. Prevents TNF-α stimulated upregulation of VCAM-1, ICAM-1 and E-selectin. Enhances adiponectin expression.
Product Specific Literature References
Effects on water diffusion of inhibitors affecting various transport processes in human red blood cells: G. Benga, et al.; Eur. J. Cell Biol. 59, 219 (1992) Abstract
Phloretin as an antagonist of prostaglandin F2 alpha receptor in cultured rat astrocytes: J. Kitanaka, et al.; J. Neurochem. 60, 704 (1993) Abstract
Characterization of the inhibition by stilbene disulphonates and phloretin of lactate and pyruvate transport into rat and guinea-pig cardiac myocytes suggests the presence of two kinetically distinct carriers in heart cells: X. Wang, et al.; Biochem. J. 290, 249 (1993) Abstract
The effect of glucose and galactose toxicity on myo-inositol transport and metabolism in human skin fibroblasts in culture: G.T. Berry, et al.; Pediat. Res. 35, 141 (1994) Abstract
Activating effect of the flavonoid phloretin on Ca(2+)-activated K+ channels in myelinated nerve fibers of Xenopus laevis: D.S. Koh, et al.; Neurosci. Lett. 165, 167 (1994) Abstract
Thyroid hormones in tissues from fetal and adult rats: G. Morreale de Escobar; Endocrinology 134, 2410 (1994) Abstract
Gonadotropin-releasing hormone induced Ca2+ influx in nonsecreting pituitary adenoma cells: role of voltage-dependent Ca2+ channels and protein kinase C: N. Prevarskaya, et al.; Mol. Cell. Neurosci. 5, 699 (1994) Abstract
The flavonoid phloretin suppresses stimulated expression of endothelial adhesion molecules and reduces activation of human platelets: V. Stangl, et al.; J. Nutr. 135, 172 (2005) Abstract
Phloretin enhances adipocyte differentiation and adiponectin expression in 3T3-L1 cells: M. Hassan, et al.; BBRC 361, 208 (2007) Abstract
Further Categories Containing This Product:
Adiponectin [ACRP30] / Related Products • Adhesion Molecules & Receptors Other Products • PKC Inhibitors • Active Substances from Fruit and Vegetables
 
 
ALX-270-348 Revised 07-Jul-08
LY-333,531 . hydrochloride
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SYNONYMS (S)-13-[(Dimethylamino)methyl-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H-13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)dione . HCl
Ruboxistaurin . hydrochloride
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-348-M001   1 mg Inquire
ALX-270-348-M005   5 mg Inquire
Product Specification
FORMULA: C28H28N4O3 . HCl
MW: 468.6 . 36.5
CAS NUMBER: 169939-93-9
MERCK INDEX: 14: 8290
PURITY: ≥98% (1H-NMR)
APPEARANCE: Red solid
SOLUBILITY: Soluble in DMSO; slightly soluble in 100% ethanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Isozyme selective inhibitor of protein kinase Cβ (PKCβ). Inhibits both the PKCβI (IC50=4.7nM) and PKCβII (IC50=5.9nM) isozymes. 76- and 61-fold more selective for inhibition of PKCβI and PKCβII over PKCα.

Not offered in the US.
Product Specific Literature References
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase : M.R. Jirousek, et al.; J. Med. Chem. 39, 2664 (1996) Abstract
Effects of the protein kinase C beta inhibitor LY333531 on neural and vascular function in rats with streptozotocin-induced diabetes: M.A. Cotter, et al.; Clin Sci (Lond) 103, 311 (2002) Abstract
Protein kinase Cbeta selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neurons: H. Kim, et al.; Diabetes 52, 2102 (2003) Abstract; Full Text
Role of p90 ribosomal S6 kinase (p90RSK) in reactive oxygen species and protein kinase C beta (PKC-beta)-mediated cardiac troponin I phosphorylation: S. Itoh, et al.; J. Biol. Chem. 280, 24135 (2005) Abstract; Full Text
Protein kinase C beta inhibitor LY333531 attenuates intercellular adhesion molecule-1 and monocyte chemotactic protein-1 expression in the kidney in diabetic rats: Y. Wu, et al.; J. Pharmacol. Sci. 101, 335 (2006) Abstract; Full Text
Ruboxistaurin: C.A. Taulien & S.V. Joy; Drugs Today (Barc) 42, 577 (2006) Abstract
Ruboxistaurin: LY 333531: Drugs R. D. 8, 193 (2007), (Review) Abstract
Role of PKC and TGF-beta receptor in glucose-induced proliferation of smooth muscle cells: Y. Yasuda, et al; BBRC 281, 71 (2001) Abstract
General Literature References
Protein kinase C and the development of diabetic vascular complications: K.J. Way, et al.; Diabet. Med. 18, 945 (2001), Review Abstract
 
 
ALX-300-004 Revised 13-Mar-08
1-O-Octadecyl-2-O-methyl-sn-glycero-3-phosphocholine
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SYNONYMS 2-O-Methyl-PAF-C-18
sn-ET-18-OCH3
Edelfosine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phospholipids / Related Products
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ALX-300-004-M050   50 mg 40.00 USD Add To Cart
ALX-300-004-M250   250 mg 160.00 USD Add To Cart
ALX-300-004-G001   1 g 480.00 USD Add To Cart
Product Specification
FORMULA: C27H58NO6P
MW: 523.7
CAS NUMBER: 77286-66-9
PURITY: ≥98%
APPEARANCE: White amorphous powder.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.

Product Description
Produces strong antitumor and antimetastatic activities. Inhibits phosphatidylinositol specific phospholipase C and protein kinase C from various leukemic cells. Antineoplastic activity.
Product Specific Literature References
Selective destruction of human leukemic cells by alkyl- lysophospholipids: R. Andreesen, et al.; Cancer Res. 38, 3894 (1978) Abstract
Disturbance of phospholipid metabolism during the selective destruction of tumor cells induced by alkyl-lysophospholipids: M. Modolell, et al.; Cancer Res. 39, 4681 (1979) Abstract
Phospholipid-sensitive Ca2+-dependent protein phosphorylation system in various types of leukemic cells from human patients and in human leukemic cell lines HL60 and K562, and its inhibition by alkyl- lysophospholipid: D.M. Helfman, et al.; Cancer Res. 43, 2955 (1983) Abstract
Purging leukemic cells from simulated human remission marrow with alkyl- lysophospholipid: S. Okamoto, et al.; Blood 69, 1381 (1987) Abstract
HL-60 cells become resistant towards antitumor ether-linked phospholipids following differentiation into a granulocytic form: D.S. Vallari, et al.; BBRC 156, 1 (1988) Abstract
The ether lipid 1-octadecyl-2-methyl-rac-glycero-3-phosphoch