ALEXIS Biochemicals: Rottlerin

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ALX-270-039

Revised 15-Nov-06

A-3 . hydrochloride
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
ALX-270-039-M050		50 mg	260.00 USD

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 • Casein Kinase Inhibitors • PKG Inhibitors

ALX-270-095

Revised 07-May-08

5,6-Dichloro-1-β-D-ribofuranosyl benzimidazole
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
ALX-270-095-M025		25 mg	70.00 USD

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-270-017

Revised 27-Apr-06

H-89 . dihydrochloride
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
ALX-270-017-M005		5 mg	55.00 USD

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 • Casein Kinase Inhibitors • Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Apoptosis Inducers & Inhibitors Other Products

ALX-350-030

Revised 07-Apr-08

Hypericin (native)
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
ALX-350-030-M005		5 mg	200.00 USD
ALX-350-030-M010		10 mg	370.00 USD

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

Further Categories Containing This Product:

Casein Kinase Inhibitors • MAPK Pathway Inhibitors • PKC Inhibitors • Natural Products - Antiviral/anti-HIV Agents • Natural Products - Antitumor Reagents • Natural Products for Neurological Research • Neuroactive Agents Other Products

ALX-350-075

Revised 08-Apr-08

Rottlerin
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
ALX-350-075-M025		25 mg	95.00 USD

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

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