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PKC Inhibitors
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ALX-270-021 Revised 03-Jul-08
Gö 6976
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SYNONYMS 12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-021-MC05   0.5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C24H18N4O
MW: 378.4
CAS NUMBER: 136194-77-9
PURITY: ≥95% (HPLC)
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in DMSO (25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for at least 3-4 months when  stored at -20°C.
HANDLING: Protect from light.

Product Description
Very potent protein kinase C (PKC) inhibitor with high selectivity for the PKC isotypes (α, β and γ). Potent antagonist of HIV-1 induction.
Product Specific Literature References
Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C: J. Kleinschroth, et al.; Bioorg. Med. Chem. Lett 3, 1959 (1993)
Selective inhibition of protein kinase C isozymes by the indolocarbazole Go 6976: G. Martiny-Baron, et al.; J. Biol. Chem. 268, 9194 (1993) Abstract; Full Text
Go 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low- level-producing reservoir cells in vitro: K.O. Qatsha, et al.; PNAS 90, 4674 (1993) Abstract
N-protein kinase C isoenzymes may be involved in the regulation of various neutrophil functions: K. Wenzel-Seifert, et al.; BBRC 200, 1536 (1994) Abstract
Atypical isoforms of pKc and insulin secretion from pancreatic beta- cells: evidence using Go 6976 and Ro 31-8220 as Pkc inhibitors: T.E. Harris, et al.; BBRC 227, 672 (1996) Abstract
 
 
ALX-350-113 Revised 28-May-08
Gossypol
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SYNONYMS 2,2’-bis[8-Formyl-1,6,7-trihydroxy-5-isopropyl-3-
methylnaphthalene]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-113-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C30H30O8
MW: 518.6
CAS NUMBER: 303-45-7
MERCK INDEX: 14: 4528
RTECS: DU3100000
SOURCE/HOST: Isolated from Gossypium genus, Malvaceae.
PURITY: ≥90%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in acetone or DMSO; sparingly soluble in 100% ethanol (2mg/ml) or methanol (2mg/ml). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Mixture of ~65% (+)- and ~35% (-)-enantiomers. Male antifertility agent. Shows antitumor, antiviral and antioxidant actions. Small molecule inhibitor of Bcl-2/Bcl-XL. Induces apoptosis. Synergizes with radiation and chemotherapy in vitro. Reversible inhibitor of protein phosphatase 2B (PP2B; calcineurin). Protein kinase C (PKC) inhibitor.
Product Specific Literature References
Binding of gossypol to purified tubulin and inhibition of its assembly into microtubules: F.J. Medrano and J.M. Andreu; Eur. J. Biochem. 158, 63 (1986) Abstract
Differential inhibition of protein kinase C subtypes: J.M. Pelosin, et al.; BBRC 169, 1040 (1990) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Gossypol arrests human benign prostatic hyperplastic cell growth at G0/G1 phase of the cell cycle: F. Shidaifat, et al.; Anticancer Res. 17, 1003 (1997) Abstract
Inhibition of huntingtin fibrillogenesis by specific antibodies and small molecules: implications for Huntington’s disease therapy: V. Heiser, et al.; PNAS 97, 6739 (2000) Abstract; Full Text
Cytotoxic effect of gossypol on colon carcinoma cells: X. Wang, et al.; Life Sci. 67, 2663 (2000) Abstract
Reversible inhibition of calcineurin by the polyphenolic aldehyde gossypol: R. Baumgrass, et al.; J. Biol. Chem. 276, 47914 (2001) Abstract; Full Text
Toxicity of (+)- and (-)-gossypol to the plant pathogen, Rhizoctonia solani: L.S. Puckhaber, et al.; J. Agric. Food Chem. 50, 7017 (2002) Abstract
Telomerase inhibitors in anticancer therapy: gossypol as a potential telomerase inhibitor: M. Mego; Bratisl. Lek. Listy 103, 378 (2002) Abstract
An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines: M. Le Blanc, et al.; Pharmacol. Res. 46, 551 (2002) Abstract
Gossypol induces chloride secretion in rat proximal colon: G. Kuhn, et al.; Eur. J. Pharmacol. 457, 187 (2002) Abstract
Determination of the absolute configuration and solution conformation of gossypol by vibrational circular dichroism: T.B. Freedman, et al.; Chirality 15, 196 (2003) Abstract
In vitro effects of the BH3 mimetic, (-)-gossypol, on head and neck squamous cell carcinoma cells: C.L. Oliver, et al.; Clin. Cancer Res. 10, 7757 (2004) Abstract; Full Text
The inhibitory effects of gossypol on human prostate cancer cells-PC3 are associated with transforming growth factor beta1 (TGFbeta1) signal transduction pathway: J. Jiang, et al.; Anticancer Res. 24, 19 (2004) Abstract
(-)-Gossypol enhances response to radiation therapy and results in tumor regression of human prostate cancer: L. Xu, et al.; Mol. Cancer Ther. 4, 197 (2005) Abstract; Full Text
Investigations on gossypol: past and present developments: K. Dodou; Expert Opin. Investig. Drugs 14, 1419 (2005) Abstract
An in vitro study of cytotoxic effects of gossypol on human epidermoid larynx carcinoma cell line (HEp-2): E. Konac, et al.; Exp. Oncol. 27, 81 (2005) Abstract; Full Text
Further Categories Containing This Product:
Bcl-2 Family Modulators • PKC Inhibitors • Natural Products - Protein Kinase Inhibitors • PP2B [Calcineurin] / Related Products • Antitumor Agents (Apoptosis Inducers) • Natural Products - Antioxidants • Polyphenols Other Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antiviral / anti-HIV Agents
 
 
ALX-270-016 Revised 05-May-08
H-7 . dihydrochloride
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SYNONYMS (±)-1-(5-Isoquinolinesulfonyl)-2-methylpiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-016-M010   10 mg 60.00 USD Add To Cart
ALX-270-016-M025   25 mg 120.00 USD Add To Cart
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Product Specification
FORMULA: C14H17N3O2S . 2 HCl
MW: 291.4 . 73.0
CAS NUMBER: 108930-17-2
PURITY: ≥98%
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in water, 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of protein kinase C (PKC), cAMP- and cGMP-dependent protein kinase (PKA and PKG). Also inhibits myosin light chain kinase. Induces apoptotic DNA fragmentation and cell death. Inhibits telomerase activity in treated NPC-076 cells.
Product Specific Literature References
1-(5-Isoquinolinesulfonyl)-2-methylpiperazine (H-7) is a selective inhibitor of protein kinase C in rabbit platelets: S. Kawamoto & H. Hidaka; BBRC 125, 258 (1984) Abstract
Stimulus-dependent inhibition of platelet aggregation by the protein kinase C inhibitors polymyxin B, H-7 and staurosporine: C. Schächtele, et al.; BBRC 151, 542 (1988) Abstract
Blockade of the spinal excitatory effect of cAMP on the startle reflex by intrathecal administration of the isoquinoline sulfonamide H-8: comparison to the protein kinase C inhibitor H-7: N.M. Boulis & M. Davis; Brain Res. 525, 198 (1990) Abstract
Potent selective inhibition of 7-O-methyl UCN-01 against protein kinase C: I. Takahashi, et al.; J. Pharmacol. Exp. Ther. 255, 1218 (1990) Abstract
The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source: J. Quick, et al.; BBRC 187, 657 (1992) Abstract
Modulation of neutrophil superoxide generation by inhibitors of protein kinase C, calmodulin, diacylglycerol and myosin light chain kinases, and peptidyl prolyl cis-trans isomerase: H. Bergstrand, et al.; J. Pharmacol. Exp. Ther. 263, 1334 (1992) Abstract
C. Gimond and M. Aumailley; Exp. Cell Res. 203, 365 (1992) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; Biochem. Biophys. Res. Commun. 241, 730 (1997) Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • PKA Inhibitors
 
 
ALX-270-040 Revised 04-Feb-05
H-7, Iso-, . dihydrochloride
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SYNONYMS Iso-H-7 . 2HCl
(±)-1-(5-Isoquinolinesulfonyl)-3-methylpiperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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ALX-270-040-M010   10 mg 120.00 USD Add To Cart
ALX-270-040-M025   25 mg 270.00 USD Add To Cart
Product Specification
FORMULA: C14H17N3O2S . 2HCl
MW: 291.4 . 73.0
CAS NUMBER: 8447-73-6
PURITY: ≥99%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Inhibitor of protein kinase C (PKC), but less potent than H-7 (Prod. No. ALX-270-016).
Product Specific Literature References
The structure and biological activities of the widely used protein kinase inhibitor, H7, differ depending on the commercial source: J. Quick, et al.; BBRC 187, 657 (1992) Abstract
 
 
ALX-270-017 Revised 27-Apr-06
H-89 . dihydrochloride
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SYNONYMS N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-017-M001   1 mg 22.00 USD Add To Cart
ALX-270-017-M005   5 mg 55.00 USD Add To Cart
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Product Specification
FORMULA: C20H20BrN3O2S . 2HCl
MW: 446.4 . 73.0
CAS NUMBER: 127243-85-0
PURITY: ≥97% (1H-NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or methanol; also soluble in ethanol: water (1:1).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for at least 3-4 weeks when stored at +4°C. We recommend using a fresh solution each day.

Product Description
Cell permeable potent and selective inhibitor of cAMP- and cGMP-dependent protein kinases (PKA and PKG) and protein kinase Cµ (PKCµ). In contrast, most other protein kinase C (PKC) isotypes are much more weakly inhibited. Also inhibits Ca2+/calmodulin-dependent protein kinase II, casein kinase I and myosin light chain kinase. Induces apoptosis.
Product Specific Literature References
Polyamines differentially inhibit cyclic AMP-dependent protein kinase- mediated phosphorylation in the brain of the tobacco hornworm, Manduca sexta: W.L. Combest, et al.; J. Neurochem. 51, 1581 (1988) Abstract
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5- isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma: T. Chijiwa, et al.; J. Biol. Chem. 265, 5267 (1990) Abstract; Full Text
A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2- bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells: C.C. Geilen; FEBS Lett. 309, 381 (1992) Abstract
Protein kinase A inhibitors enhance radiation-induced apoptosis: D. Findik, et al.; J. Cell. Biochem. 57, 12 (1995) Abstract
Characterization of activators and inhibitors of protein kinase C mu: F.-J. Johannes, et al.; Eur. J. Biochem. 227, 303 (1995) Abstract
Crystal structures of catalytic subunit of cAMP-dependent protein kinase in complex with isoquinolinesulfonyl protein kinase inhibitors H7, H8, and H89. Structural implications for selectivity: R.A. Engh, et al.; J. Biol. Chem. 271, 26157 (1996) Abstract; Full Text
Stimulation of the ERK pathway by GTP-loaded Rap1 requires the concomitant activation of Ras, protein kinase C, and protein kinase A in neuronal cells: T. Bouschet, et al.; J. Biol. Chem. 278, 4778 (2003) Abstract; Full Text
Further Categories Containing This Product:
CAM Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products • Casein Kinase Inhibitors
 
 
ALX-270-069 Revised 04-Feb-05
HA-100 . dihydrochloride
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SYNONYMS 1-(5-Isoquinolinylsulfonyl)piperazine . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
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ALX-270-069-M005   5 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C13H15N3O2S . 2HCl
MW: 277.3 . 73.0
CAS NUMBER: 84468-24-6
PURITY: ≥99%
APPEARANCE: Lyophilized solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of myosin light chain kinase, cAMP-dependent protein kinase (PKA) and protein kinase C (PKC).
Product Specific Literature References
Role of protein kinases in stimulation of human polymorphonuclear leukocyte oxidative metabolism by various agonists. Differential effects of a novel protein kinase inhibitor: C. Gerard, et al.; J. Clin. Invest. 77, 61 (1986) Abstract
Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives: M. Hagiwara, et al.; Mol. Pharmacol. 32, 7 (1987) Abstract
Further Categories Containing This Product:
PKC Inhibitors • Myosin Light Chain Kinase Inhibitors
 
 
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-350-030 Revised 20-Oct-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% (HPLC)
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 and oxygen.
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)