• Home
  • Sitemap
  • Help
  • Technical Support
  • Contact
Circadian Clock / Related Products
You are here: Product Lines > Signal Transduction > Circadian Clock / Related Products
 
Toolbar - View Selection
 
Items 38 of 38
ALX-270-017 Revised 27-Apr-06
H-89 . dihydrochloride
Add to Clipboard
SYNONYMS N-[2-(p-Bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide . 2HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-017-M001   1 mg 22.00 USD Add To Cart
ALX-270-017-M005   5 mg 55.00 USD Add To Cart
Inquire
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-270-039 Revised 15-Nov-06
A-3 . hydrochloride
Add to Clipboard
SYNONYMS N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-039-M010   10 mg 65.00 USD Add To Cart
ALX-270-039-M050   50 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C12H13ClN2O2S . HCl
MW: 284.8 . 36.5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.
Product Specific Literature References
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Casein Kinase Inhibitors
 
 
ALX-270-095 Revised 07-May-08
5,6-Dichloro-1-β-D-ribofuranosyl benzimidazole
Add to Clipboard
SYNONYMS DRB
5,6-Dichlorobenzimidazole riboside
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Adenosine Derivatives Other Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-095-M005   5 mg 20.00 USD Add To Cart
ALX-270-095-M025   25 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C12H12Cl2N2O4
MW: 319.1
CAS NUMBER: 53-85-0
RTECS: DD7310000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO (100mM) or dimethyl formamide (100mM).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions should be stored in the refrigerator and should be lyophilized and frozen for longer storage periods.
IDENTITY: Identity determined by 1H-NMR, MS and UV.

Product Description
Selective casein kinase II inhibitor. Inhibitor of RNA synthesis in eukaryotic cells.
Product Specific Literature References
Halobenzimidazole ribosides and RNA synthesis of cells and viruses: I. Tamm & P. Sehgal; Adv. Virus Res. 22, 187 (1978) Abstract
Mechanism of action of 5,6-dichloro-1-beta-D- ribofuranosylbenzimidazole. II. A resistant human cell mutant with an altered transcriptional machinery: B. Mittleman, et al.; J. Mol. Biol. 165, 461 (1983) Abstract
Mechanism of action of DRB. III. Effect on specific in vitro initiation of transcription: R. Zandomeni, et al.; J. Mol. Biol. 167, 561 (1983) Abstract
Casein kinase type II is involved in the inhibition by 5,6-dichloro-1- beta-D-ribofuranosylbenzimidazole of specific RNA polymerase II transcription: R. Zandomeni, et al.; J. Biol. Chem. 261, 3414 (1986) Abstract; Full Text
Inhibition of germinal vesicle breakdown in bovine oocytes by 5,6- dichloro-1-beta-D-ribofuranosylbenzimidazole (DRB): C.E. Farin & L. Yang; Mol. Reprod. Dev. 37, 284 (1994) Abstract
Further Categories Containing This Product:
Casein Kinase Inhibitors
 
 
ALX-350-030 Revised 20-Oct-08
Hypericin (native)
Add to Clipboard
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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) 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
Further Categories Containing This Product:
Casein Kinase Inhibitors • MAPK Pathway Inhibitors • PKC Inhibitors • Natural Products - Antitumor Reagents • Neuroactive Agents Other Products • Natural Products for Neurological Research • Natural Products - Antiviral / anti-HIV Agents
 
 
ALX-350-075 Revised 08-Apr-08
Rottlerin
Add to Clipboard
SYNONYMS Mallotoxin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-075-M010   10 mg 40.00 USD Add To Cart
ALX-350-075-M025   25 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C30H28O8
MW: 516.6
CAS NUMBER: 82-08-6
MERCK INDEX: 14: 8272
RTECS: AM6913800
SOURCE/HOST: Isolated from Mallotus philippinensis.
PURITY: ≥98% (HPLC)
APPEARANCE: Orange to brown solid.
SOLUBILITY: Soluble in DMSO, chloroform or 100% ethanol. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Mitochondrial uncoupler that depolarizes the mitochondrial membrane potential, reduces cellular ATP levels, activates 5‘-AMP-activated protein kinase (AMPK) and affects mitochondrial production of reactive oxygen species (ROS). Potent activator of multiple Ca2+-sensitive K+ channels. Blocks several kinases and non-kinase proteins in vitro. Has been widely-used as a selective inhibitor of protein kinase Cδ (PKCδ). However, recent studies indicate that rottlerin has no direct effect on PKCδ and that it should not be used to determine the involvement of PKCδ in biological processes.
Product Specific Literature References
The mouse ear edema: a quantitatively evaluable assay for tumor promoting compounds and for inhibitors of tumor promotion: M. Gschwendt, et al.; Cancer Lett. 25, 177 (1984) Abstract
Rottlerin, a novel protein kinase inhibitor: M. Gschwendt, et al.; BBRC 199, 93 (1994) Abstract
Elongation factor-2 kinase: effective inhibition by the novel protein kinase inhibitor rottlerin and relative insensitivity towards staurosporine: M. Gschwendt, et al.; FEBS Lett. 338, 85 (1994) Abstract
Rottlerin: an inappropriate and ineffective inhibitor of PKCdelta: S.P. Soltoff; TIPS 28, 453 (2007) Abstract
Further Categories Containing This Product:
PKA Inhibitors • CAM Kinase Inhibitors • Casein Kinase Inhibitors • PKC Inhibitors
 
 
ALX-350-014 Revised 03-Apr-08
Calyculin A
Add to Clipboard
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-014-C010   10 µg 65.00 USD Add To Cart
ALX-350-014-C025   25 µg 110.00 USD Add To Cart
ALX-350-014-C050   50 µg 190.00 USD Add To Cart
ALX-350-014-C100   100 µg 320.00 USD Add To Cart
Product Specification
FORMULA: C50H81N4O15P
MW: 1009.2
CAS NUMBER: 101932-71-2
SOURCE/HOST: Isolated from Discodermia calyx.
PURITY: ≥95%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetonitrile, chloroform, methylene chloride or benzene. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: May by subject to isomerization when in solution. Biological activity is not affected by isomerization.
HANDLING: Protect from light and moisture.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Potent cell permeable inhibitor with high specificity for protein phosphatase 1 (PP1) and 2A (PP2A). Inhibits p130cas tyrosine phosphorylation. Enhances the phosphorylation level of NF-κB. Affects intracellular signalling processes that require 14-3-3. Potent non-phorbol type tumor promoter. Prevents γ-radiation induced apoptosis.
Product Specific Literature References
Okadaic acid: an additional non-phorbol-12-tetradecanoate-13-acetate- type tumor promoter: M. Suganuma, et al.; PNAS 85, 1768 (1988) Abstract
Protein phosphatases come of age: P.Cohen & P.T. Cohen; J. Biol. Chem. 264, 21435 (1989) Abstract; Full Text
Calyculin A and okadaic acid: inhibitors of protein phosphatase activity: H. Ishihara, et al.; BBRC 159, 871 (1989) Abstract
The structure and regulation of protein phosphatases: P. Cohen; Ann. Rev. Biochem. 58, 453 (1989) Abstract
Calyculin A, an inhibitor of protein phosphatases, a potent tumor promoter on CD-1 mouse skin: M. Suganuma, et al.; Cancer Res. 50, 3521 (1990) Abstract
Nonphorbol tumor promoters okadaic acid and calyculin-A induce membrane translocation of protein kinase C: R. Gopalakrishna; BBRC 189, 950 (1992) Abstract
Comparative effects of protein phosphatase inhibitors (okadaic acid and calyculin A) on human leukemia HL60, HL60/ADR and K562 cells: K. Sakurada, et al.; BBRC 187, 488 (1992) Abstract
Calyculin A, a potent inhibitor of phosphatases-1 and -2A, prevents apoptosis: Q. Song & M.F. Lavin; BBRC 190, 47 (1993) Abstract
Enhancement of AMPA-mediated synaptic transmission by the protein phosphatase inhibitor calyculin A in rat hippocampal slices: A. Figurov, et al.; Eur. J. Neurosci. 5, 1035 (1993) Abstract
Calyculin A, a non-phorbol ester type tumor promotor, induced oxidative DNA damage in stimulated human neutrophil-like cells: T. Takeuchi, et al.; BBRC 205, 1803 (1994) Abstract
Potassium and calcium channel involvement in induction of long-lasting synaptic enhancement by calyculin A, a protein phosphatase inhibitor, in rat hippocampal CA1 region: N. Murakami, et al.; Neurosci. Lett. 176, 181 (1994) Abstract
Differential toxicity of the protein phosphatase inhibitors microcystin and calyculin A: M.T. Runnegar, et al.; J. Pharmacol. Exp. Ther. 273, 545 (1995) Abstract
Inhibition of p130cas tyrosine phosphorylation by calyculin A: W. Qiu, et al.; J. Leukoc. Biol. 63, 631 (1998) Abstract
Unique features of the okadaic acid activity class of tumor promoters: H. Fujiki & M. Suganuma; J. Cancer Res. Clin. Oncol. 125, 150 (1999), Review Abstract
Calyculin A-induced vimentin phosphorylation sequesters 14-3-3 and displaces other 14-3-3 partners in vivo: G. Tzivion, et al.; J. Biol. Chem. 275, 29772 (2000) Abstract
Calyculin A induces apoptosis and stimulates phosphorylation of p65NF-kappaB in human osteoblastic osteosarcoma MG63 cells: H. Tanaka, et al.; Int. J. Oncol. 31, 389 (2007) Abstract
Further Categories Containing This Product:
PP2A / Related Products • PP1 / Related Products • Natural Products - Other Tumor Promoters • 14-3-3 Proteins / Related Products • Carcinogens & Tumor Promoters Other Products • NF-kB Pathway Modulators • Natural Products - Apoptosis Inducers & Inhibitors • Marine Natural Products
 
 
ALX-270-062 Revised 03-Feb-05
Cantharidic acid . disodium salt
Add to Clipboard
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PP2A / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-062-M010   10 mg 110.00 USD Add To Cart
Product Specification
FORMULA: C10H12O5 . 2Na
MW: 212.2 . 46.0
CAS NUMBER: 28874-45-5
PURITY: ≥95%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water; slightly soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent protein phosphatase 2A inhibitor.
Product Specific Literature References
M. Matsuzawa, et al.; J. Agric. Food Chem. 35, 823 (1987)
Partial characterization of specific cantharidin binding sites in mouse tissues: M.J. Graziano, et al.; Mol. Pharmacol. 33, 706 (1989) Abstract
Cantharidin-binding protein: identification as protein phosphatase 2A: Y.-M. Li & J.E. Casida; PNAS 89, 11867 (1992) Abstract
 
 
ALX-270-063 Revised 03-Apr-08
Cantharidin
Add to Clipboard
SYNONYMS Hexahydro-3a,7a-dimethyl-4,7-epoxyisobenzo-furan-1,3-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-063-M025   25 mg 50.00 USD Add To Cart
ALX-270-063-M100   100 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C10H12O4
MW: 196.2
CAS NUMBER: 56-25-7
MERCK INDEX: 14: 1752
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone, DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Potent protein phosphatase 2A (PP2A) inhibitor. At higher concentrations, also inhibits protein phosphatase 1 (PP1).
Product Specific Literature References
Partial characterization of specific cantharidin binding sites in mouse tissues: M.J. Graziano, et al.; Mol. Pharmacol. 33, 706 (1988) Abstract
Cantharidin-binding protein: identification as protein phosphatase 2A: Y.-M. Li and J.E. Casida; PNAS 89, 11867 (1992) Abstract
Protein phosphatase 2A and its [3H]cantharidin/[3H]endothall thioanhydride binding site. Inhibitor specificity of cantharidin and ATP analogues: Y.-M. Li, et al.; Biochem. Pharmacol. 46, 1435 (1993) Abstract
Further Categories Containing This Product:
PP2A / Related Products
 
 
ALX-380-065 Revised 24-Sep-08
Fostriecin
Add to Clipboard
SYNONYMS Phosphotrienin
CI-920
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Topoisomerase Inhibitors
Ordering Information
Product Numbers: