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Protein Kinase C [PKC] / Related Products
You are here: Product Lines > Signal Transduction > Protein Kinase C [PKC] / Related Products
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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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
Antitumor Agents (Enzyme Inhibitors)PKC InhibitorsParasitic Diseases Other Products
 
 
ALX-350-030 Revised 07-Apr-08
Hypericin (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-030-M001   1 mg 50.00 USD Add To Cart
ALX-350-030-M005   5 mg 200.00 USD Add To Cart
ALX-350-030-M010   10 mg 370.00 USD Add To Cart
Product Specification
FORMULA: C30H16O8
MW: 504.4
CAS NUMBER: 548-04-9
MERCK INDEX: 14: 4863
SOURCE/HOST: Isolated from Hypericum perforatum.
PURITY: ≥98%
APPEARANCE: Black to black-red powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone, ethylmethylketone, pyridine or other organic solvents and bases.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE TERATOGENIC. HARMFUL. MAY BE MUTAGENIC.

Product Description
Inhibitor of protein kinase C (PKC). Shows anti-viral and anti-retroviral activity. Displays antineoplastic and antitumor activities. Inhibits casein kinase II (CKII) and MAP kinase. Bright red fluorescence emission and photostability. Antidepressant.
Product Specific Literature References
Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin: D. Meruelo, et al.; PNAS 85, 5230 (1988) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Evaluation of the antiviral activity of anthraquinones, anthrones and anthraquinone derivatives against human cytomegalovirus: D.L. Barnard, et al.; Antiviral Res. 17, 63 (1992) Abstract
Photosensitized inhibition of growth factor-regulated protein kinases by hypericin: P. Agostinis, et al.; Biochem. Pharmacol. 49, 1615 (1995) Abstract
Growth inhibition and apoptosis in human neuroblastoma SK-N-SH cells induced by hypericin, a potent inhibitor of protein kinase C: W. Zhang, et al.; Cancer Lett. 96, 31 (1995) Abstract
Hypericin-induced photosensitization of HeLa cells leads to apoptosis or necrosis. Involvement of cytochrome c and procaspase-3 activation in the mechanism of apoptosis: A. Vantieghem, et al.; FEBS Lett. 440, 19 (1998) Abstract
The activation of the c-Jun N-terminal kinase and p38 mitogen-activated protein kinase signaling pathways protects HeLa cells from apoptosis following photodynamic therapy with hypericin: Z. Assefa, et al.; J. Biol. Chem. 274, 8788 (1999) Abstract; Full Text
Over-expression of Bcl-2 does not protect cells from hypericin photo- induced mitochondrial membrane depolarization, but delays subsequent events in the apoptotic pathway: R. Chaloupka, et al.; FEBS Lett. 462, 295 (1999) Abstract
Hypericin induces both differentiation and apoptosis in human promyelocytic leukemia HL-60 cells: K.T. Lee, et al.; Biol. Pharm. Bull. 22, 1271 (1999) Abstract
Apoptotic and anti-apoptotic signaling pathways induced by photodynamic therapy with hypericin: P. Agostinis, et al.; Adv. Enzyme Regul. 40, 157 (2000) Abstract
Hypericin--a new antiviral and antitumor photosensitizer: mechanism of action and interaction with biological macromolecules: P. Miskovsky; Curr. Drug Targets 3, 55 (2002), (Review) Abstract
Hypericin--the facts about a controversial agent: A. Kubin, et al.; Curr. Pharm. Des. 11, 233 (2005), (Review) Abstract
Cellular mechanisms and prospective applications of hypericin in photodynamic therapy: T. Kiesslich, et al.; Curr. Med. Chem. 13, 2189 (2006), (Review) Abstract
 
 
ALX-159-001 Revised 01-Mar-06
IL-2 Receptor Fragment (human)
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SYNONYMS Interleukin-2 Receptor Fragment (human)
PRODUCT LINE Chemokines & Cytokines
PRODUCT CATEGORY Interleukin Receptors
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ALX-159-001-M001   1 mg 80.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gln-Arg-Arg-Gln-Arg-Lys-Ser-Arg-Arg-Thr-Ile-OH
FORMULA: C59H113N29O16
MW: 1484.7
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Substrate for protein kinase C (PKC). The peptide is derived from the cytoplasmic C-terminus of the human interleukin-2 receptor.
Product Specific Literature References
Phosphorylation of the human interleukin-2 receptor and a synthetic peptide identical to its C-terminal, cytoplasmic domain: B. Gallis, et al.; J. Biol. Chem. 261, 5075 (1986) Abstract; Full Text
Further Categories Containing This Product:
PKC SubstratesCD25 [IL-2Ralpha] / Related ProductsPeptides
 
 
ALX-420-010 Revised 12-Jan-07
(+)-Indolactam V
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Negative Controls
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ALX-420-010-C300   300 µg 110.00 USD Add To Cart
ALX-420-010-M001   1 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C17H23N3O2
MW: 301.4
CAS NUMBER: 90365-56-3
PURITY: ≥95% (1H-NMR)
APPEARANCE: White to off-white solid.
PURITY DETAIL: May contain traces of (-)-Indolactam V.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Used as negative control compound in studies with (-)-indolactam V (Prod. No. ALX-420-011).
 
 
ALX-420-011 Revised 12-Jan-07
(-)-Indolactam V
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Activators
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ALX-420-011-C300   300 µg 110.00 USD Add To Cart
ALX-420-011-M001   1 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C17H23N3O2
MW: 301.4
CAS NUMBER: 90365-57-4
RTECS: UY8547000
PURITY: ≥95% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: HARMFUL. MAY BE CARCINOGENIC.
IDENTITY: May contain traces of (+)-Indolactam V.

Product Description
Moderately potent indolactam activator of protein kinase C (PKC). Increases cytoplasmic mRNAs.
Product Specific Literature References
Structure-activity studies on synthetic analogues (indolactams) of the tumor promoter teleocidin: H. Fujiki, et al.; Gann 75, 866 (1984) Abstract
(-)-Indolactam V activates protein kinase C and induces changes in muscarinic receptor functions in SH-SY5Y human neuroblastoma cells: J. Heikkilä & K. Akerman; BBRC 162, 1207 (1989) Abstract
Interleukin-4 signals regulating CD23 gene expression in human B cells: protein kinase C-independent signaling pathways: C.E. Lee, et al.; Cell Immunol. 146, 171 (1993) Abstract
Differential protein kinase C ligand regulation detected in vivo by a phenotypic yeast assay: H.L. Shieh, et al.; Mol. Carcinogen. 12, 166 (1995) Abstract
Further Categories Containing This Product:
Carcinogens & Tumor Promoters Other Products
 
 
ALX-350-031 Revised 07-Apr-08
Ingenol (high purity)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-031-M001   1 mg 45.00 USD Add To Cart
ALX-350-031-M005   5 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C20H28O5
MW: 348.4
CAS NUMBER: 30220-46-3
PURITY: ≥98%
APPEARANCE: Solid.
SOLUBILITY: Soluble in DMSO and 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Extremely weak protein kinase C (PKC) activator. Starting material for synthesis of ingenol derivatives.
Product Specific Literature References
Specific binding to protein kinase C by ingenol and its induction of biological responses: C.M. Hasler, et al.; Cancer Res. 52, 202 (1992) Abstract
Preconditioning of isolated rabbit cardiomyocytes: effects of glycolytic blockade, phorbol esters, and ischaemia: S. Armstrong & C.E. Gonote; Cardiovasc. Res. 28, 1700 (1994) Abstract
Total synthesis of ingenol: I. Kuwajima & K. Tanino; Chem. Rev. 105, 4661 (2005), (Review) Abstract
Further Categories Containing This Product:
PKC ActivatorsChemical Synthesis - Reagents & Intermediates
 
 
ALX-380-103 Revised 17-Jun-08
K-252c
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SYNONYMS Staurosporinone
Staurosporine Aglycone
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-380-103-M001   1 mg 80.00 USD Add To Cart
ALX-380-103-M005   5 mg 320.00 USD Add To Cart
ALX-380-103-M100   100 mg Inquire
ALX-380-103-M500   500 mg Inquire
ALX-380-103-G001   1 g Inquire
Product Specification
FORMULA: C20H13N3O
MW: 311.4
CAS NUMBER: 85753-43-1
PURITY: ≥95%
APPEARANCE: Yellow crystalline solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of protein kinase C (PKC). Aglycone of staurosporine.
Product Specific Literature References
K-252b, c and d, potent inhibitors of protein kinase C from microbial origin: S. Nakanishi, et al.; J. Antibiot. 39, 1066 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989) Abstract
Synthesis of the Staurosporine aglycon: C.J. Moody & K.F. Rahimtoola; J. Org. Chem. 57, 2105 (1992)
Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C: J. Kleinschroth, et al.; Bioorg. Med. Chem. Lett. 3, 1959 (1993)
Protein kinase C inhibitors; structure-activity relationships in K252c-related compounds: S. Fabre, et al.; Bioorg. Med. Chem. 1, 193 (1993) Abstract
Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976: G. Martiny-Baron, et al.; J. Biol. Chem. 268, 9194 (1993) Abstract
Oxidative cyclisations with palladium acetate. A short synthesis of staurosporine aglycone: W. Harris, et al.; Tetrahedron Lett. 34, 8361 (1993)
Staurosporine aglycone (K252-c) and arcyriaflavin A from the marine ascidian, Eudistoma sp: P.A. Horton, et al.; Experientia 50, 843 (1994) Abstract
A facile synthesis of staurosporine aglycone: G. Xie& J.W. Lown; Tetrahedron Lett. 35, 5555 (1994)
Staurosporine, a potentially important gift from a microorganism: S. Omura, et al.; J. Antibiot. 48, 535 (1995) Abstract
A General Approach to the Synthesis of Bisindolylmaleimides: Synthesis of Staurosporine Aglycone: M.M. Faul et al.; Synthesis 1511 (1995)
Design and implementation of an efficient synthesis approach to furanosylated indolocarbazoles: total synthesis of (+)- and (-)-K252a: J.L. Wood, et al.; J. Am. Chem. Soc. 119, 9641 (1997)
Advances in indolo[2,3-a]carbazole chemistry: design and synthesis of protein kinase C and topoisomerase I inhibitors: U. Pindur, et al.; Curr. Med. Chem. 6, 29 (1999) Abstract
Synthesis of pyrrolidin-2-ones and of Staurosporine aglycon (K-252c) by intermolecular Michael reaction: S. Mahboobi, et al.; J. Org. Chem. 64, 4697 (1999)
Kinase inhibitors: not just for kinases anymore: S.L. McGovern & B.K. Shoichet; J. Med. Chem. 46, 1478 (2003) Abstract
A short synthesis of staurosporinone (K-252c): S.P. Gaudencio; Tetrahedron Lett. 44, 2577 (2003)
Biological targets of antitumor indolocarbazoles bearing a sugar moiety: M. Prudhomme; Curr. Med. Chem. Anticancer Agents 4, 509 (2004) Abstract
Staurosporine and rebeccamycin aglycones are assembled by the oxidative action of StaP, StaC, and RebC on chromopyrrolic acid: A.R. Howard-Jones & C.T. Walsh; J. Am. Chem. Soc. 128, 12289 (2006) Abstract
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a: R.L. Hudkins, et al.; J. Med. Chem. 50, 433 (2007) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Please also see our Product Flyer "K-252c - A Key Aglycone for Medicinal Chemistry".
Further Categories Containing This Product:
Staurosporine / Related ProductsAlkaloids
 
 
ALX-380-027 Revised 09-May-08
K-252a
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-380-027-C100   100 µg 98.00 USD Add To Cart
ALX-380-027-C500   500 µg 290.00 USD Add To Cart
ALX-380-027-M001   1 mg 395.00 USD Add To Cart
Product Specification
FORMULA: C27H21N3O5
MW: 467.5
CAS NUMBER: 97161-97-2
SOURCE/HOST: Isolated from Nocardiopsis sp.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, methanol or methylene chloride (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Alkaloid isolated from soil fungi. General, cell permeable protein kinase inhibitor. Potent inhibitor of Ca2+/calmodulin kinase II. Inhibits myosin light chain kinase, cAMP-dependent protein kinase (PKA), protein kinase C (PKC), and cGMP-dependent protein kinase (PKG). Induces apoptosis.
Product Specific Literature References
K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986) Abstract
The structures of the novel protein kinase C inhibitors K-252a, b, c and d: T. Yasuzawa, et al.; J. Antibiot. (Tokyo) 39, 1072 (1986) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990) Abstract
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991) Abstract
Differentiation of PC12 cells with K-ras: comparison with nerve growth factor: D.L. Simpson, et al.; J. Neurosci. Res. 28, 486 (1991) Abstract
K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity: M.M. Berg, et al.; J. Biol. Chem. 267, 13 (1992) Abstract; Full Text
K-252 compounds: modulators of neurotrophin signal transduction: B. Knusel & F. Hefti; J. Neurochem. 59, 1987 (1992) Abstract
pp42/44MAP kinase is a component of the neurogenic pathway utilized by nerve growth factor in PC12 cells: E.D. Lloyd & M.W. Wooten; J. Neurochem. 59, 1099 (1992) Abstract
K-252a and staurosporine selectively block autophosphorylation of neurotrophin receptors and neurotrophin-mediated responses: S.H. Nye, et al.; Mol. Biol. Cell 3, 677 (1992)