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TRAP5 [TRACP]

Phosphatases Other Products

ALX-350-014

Revised 03-Apr-08

Calyculin A
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
ALX-350-014-C025		25 µg	110.00 USD
ALX-350-014-C050		50 µg	190.00 USD
ALX-350-014-C100		100 µg	320.00 USD

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:

ALX-270-062

Revised 03-Feb-05

Cantharidic acid . disodium salt
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

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
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
ALX-270-063-M100		100 mg	160.00 USD

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
SYNONYMS	Phosphotrienin CI-920
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Topoisomerase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-065-C010		10 µg	150.00 USD

Product Specification

FORMULA:	C₁₉H₂₆O₉PNa
MW:	452.4
CAS NUMBER:	87860-39-7
RTECS:	UQ0600000
SOURCE/HOST:	Isolated from Streptomyces pulveraceous subsp. fostreus.
PURITY:	≥98% (HPLC)
APPEARANCE:	Colorless solid.
SOLUBILITY:	Soluble in water (50mg/ml), methanol (10mg/ml) or 100% ethanol (10mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for at least 1 year when stored at -20°C. Use fresh solution.
HANDLING:	Protect from light. Packaged under inert gas. Hygroscopic.

Product Description

Antitumor antibiotic. Catalytic inhibitor of topoisomerase II. Strong protein phosphatase 2A (PP2A) inhibitor (IC₅₀=3.2nM). Weak inhibitor for PP1 (IC₅₀=131µM). No apparent effect on PP2B. The binding site for fostriecin on PP2A is different from that of okadaic acid (see Prod. No. ALX-350-003).

Product Specific Literature References

Novel antitumor agents CI-920, PD 113,270 and PD 113,271. II. Isolation and characterization: S.S. Stampwala, et al.; J. Antibiot. (Tokyo) 36, 1601 (1983) Abstract
Novel antitumor agents CI-920, PD 113,270 and PD 113,271. I. Taxonomy, fermentation and biological properties: J.B. Tunac, et al.; J. Antibiot. (Tokyo) 36, 1595 (1983) Abstract
Studies on the biochemical mechanism of the novel antitumor agent, CI- 920: D.W. Fry, et al.; Cancer Chemother. Pharmacol. 13, 171 (1984) Abstract
Anticancer activity of the structurally novel antibiotic Cl-920 and its analogues: W.R. Leopold, et al.; Cancer Res. 44, 1928 (1984) Abstract
Inhibition of type II topoisomerase by fostriecin: T.J. Boritzki, et al.; Biochem. Pharmacol. 37, 4063 (1988) Abstract
Comparison of effects of fostriecin, novobiocin, and camptothecin, inhibitors of DNA topoisomerases, on DNA replication and repair in human cells: C.M. Gedik & A.R. Collins; Nucl. Acids Res. 18, 1007 (1990) Abstract
The cell cycle related differences in susceptibility of HL-60 cells to apoptosis induced by various antitumor agents: W. Gorczyca, et al.; Cancer Res. 53, 3186 (1993) Abstract
Induction of DNA strand breaks associated with apoptosis during treatment of leukemias: W. Gorczyca, et al.; Leukemia 7, 659 (1993) Abstract
Antitumor drug fostriecin inhibits the mitotic entry checkpoint and protein phosphatases 1 and 2A: M. Roberge, et al.; Cancer Res. 54, 6115 (1994) Abstract
Fostriecin: a review of the preclinical data: R.S. de Jong, et al.; Anticancer Drugs 8, 413 (1997) Abstract
Fostriecin, an antitumor antibiotic with inhibitory activity against serine/threonine protein phosphatases types 1 (PP1) and 2A (PP2A), is highly selective for PP2A: A.H. Walsh, et al.; FEBS Lett. 416, 230 (1997) Abstract
Fostriecin, an inhibitor of protein phosphatase 2A, limits myocardial infarct size even when administered after onset of ischemia: C. Weinbrenner, et al.; Circulation 98, 899 (1998) Abstract
Phase I and pharmacokinetic study of the topoisomerase II catalytic inhibitor fostriecin: R.S. de Jong, et al.; Br. J. Cancer 79, 882 (1999) Abstract
Fostriecin: chemistry and biology: D.S. Lewy, et al.; Curr. Med. Chem. 9, 2005 (2002) Abstract

Further Categories Containing This Product:

Antibiotics - Other Signal Transduction Pathway Modulators • PP2A / Related Products • Antitumor Agents (Enzyme Inhibitors) • Antitumor Antibiotics

ALX-350-003

Revised 23-May-08

Okadaic acid (high purity)
SYNONYMS	Halochondrine A (high purity) 9,10-Deepithio-9,10-didehydroacanthifolicin (high purity)
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Okadaic Acids

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-003-C025		25 µg	60.00 USD
ALX-350-003-C050		50 µg	110.00 USD
ALX-350-003-C100		100 µg	180.00 USD
ALX-350-003-M001		1 mg	990.00 USD

Product Specification

FORMULA:	C₄₄H₆₈O₁₃
MW:	805.0
CAS NUMBER:	78111-17-8
MERCK INDEX:	14: 6819
RTECS:	AA8227800
SOURCE/HOST:	Isolated from Prorocentrum concavum by preparative flash, medium pressure and high performance liquid chromatography.
PURITY:	≥98% (HPLC)
APPEARANCE:	White crystalline solid.
SOLUBILITY:	Soluble in DMSO, 100% ethanol or methanol (1mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Use only fresh solutions.
HANDLING:	Protect from light. Packaged under inert gas.
HAZARD:	MAY BE CARCINOGENIC. HIGHLY IRRITANT. TOXIC.

Product Description

Potent inhibitor of protein phosphatases 1 (PP1) and 2A (PP2A) in numerous cell types. Does not affect activity of acid phosphatase, alkaline phosphatase and tyrosine phosphatase. Non-phorbol type tumor promoter. Induces apoptosis in human breast carcinoma cells (MB-231 and MCF-7) and in myeloid cells, but inhibits glucocorticoid-induced apoptosis in T cell hybridomas. Tumor promoter. Has shown contractile effect on smooth muscle and heart muscle. Significantly increases cyclin B1 expression in adult neurons.

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.W. Cohen; J. Biol. Chem. 264, 21435 (1989) Abstract; Full Text
The structure and regulation of protein phosphatases: P. Cohen; Ann. Rev. Biochem. 58, 453 (1989) Abstract
Effects of the tumour promoter okadaic acid on intracellular protein phosphorylation and metabolism: T.A. Haystead, et al.; Nature 337, 78 (1989) Abstract
Okadaic acid: a new probe for the study of cellular regulation: P. Cohen, et al.; TIPS 15, 98 (1990), (Review) Abstract
Nonphorbol tumor promoters okadaic acid and calyculin-A induce membrane translocation of protein kinase C: R. Gopalakrishna, et al.; BBRC 189, 950 (1992) Abstract
Protein phosphatase inhibitors okadaic acid and calyculin A alter cell shape and F-actin distribution and inhibit stimulus-dependent increases in cytoskeletal actin of human neutrophils: P. Kreienbuehl, et al.; Blood 80, 2911 (1992) Abstract
Site-specific dephosphorylation of smooth muscle myosin light chain kinase by protein phosphatases 1 and 2A: M. Nomura, et al.; Biochemistry 31, 11915 (1992) Abstract
Inhibition of apoptosis in human tumour cells by okadaic acid: Q. Song, et al.; J. Cell Physiol. 153, 550 (1992) Abstract
Okadaic acid enhances human T cell activation and phosphorylation of an internal substrate induced by phorbol myristate acetate: Y. Tada, et al.; Immunopharmacol. 24, 17 (1992) Abstract
Okadaic acid inhibits glucocorticoid-induced apoptosis in T cell hybridomas at its late stage: Y. Ohoka, et al.; BBRC 197, 916 (1993) Abstract
Multiple apoptotic death types triggered through activation of separate pathways by cAMP and inhibitors of protein phosphatases in one (IPC leukemia) cell line: B.T. Gjertsen, et al.; J. Cell. Sci. 107, 3363 (1994) Abstract
Differential induction of apoptosis in human breast tumor cells by okadaic acid and related inhibitors of protein phosphatases 1 and 2A: K. Kiguchi, et al.; Cell Growth Differentiation 5, 995 (1994) 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
Okadaic acid: the archetypal serine/threonine protein phosphatase inhibitor: A.B. Dounay & C.J. Forsyth; Curr. Med. Chem. 9, 1939 (2002), Review Abstract
Mechanism of Ca2+-mediated regulation of NDR protein kinase through autophosphorylation and phosphorylation by an upstream kinase: R. Tamaskovic, et al.; J. Biol. Chem. 278, 6710 (2003) Abstract; Full Text
Okadaic acid induced cyclin B1 expression and mitotic catastrophe in rat cortex: B. Chen, et al.; Neurosci. Lett. 406, 178 (2006) Abstract

ALX-350-010	Okadaic acid . ammonium salt (high purity)
ALX-350-011	Okadaic acid . sodium salt (high purity)
ALX-350-063	Okadaic acid . potassium salt (high purity)

ALX-350-003	Okadaic acid (high purity)
ALX-350-011	Okadaic acid . sodium salt (high purity)
ALX-350-063	Okadaic acid . potassium salt (high purity)

ALX-350-010	Okadaic acid . ammonium salt (high purity)
ALX-350-063	Okadaic acid . potassium salt (high purity)
ALX-350-003	Okadaic acid (high purity)

FORMULA:	C₄₄H₆₇O₁₃ . NH₄
MW:	804.0 . 18.0
CAS NUMBER:	155716-06-6
SOURCE/HOST:	Isolated from Prorocentrum concavum by preparative flash, medium pressure and high performance liquid chromatography. Salt form generated in aqueous ammonium hydroxide-methanol solution.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO, 100% ethanol, methanol, acetone, ethyl acetate or distilled water. Dissolve first in organic solvent before diluting in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Packaged under inert gas. Protect from light.
HAZARD:	TOXIC. MAY BE CARCINOGENIC. HIGHLY IRRITANT.

FORMULA:	C₄₄H₆₇O₁₃ . Na
MW:	804.0 . 23.0
CAS NUMBER:	209266-80-8
SOURCE/HOST:	Isolated from Prorocentrum concavum by preparative flash, medium pressure and high performance liquid chromatography. Salt form generated in aqueous sodium hydroxide-methanol solution.
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO (1mg/ml), 100% ethanol, methanol, acetone, ethyl acetate or distilled water. Dissolve first in organic solvent before diluting in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	HIGHLY IRRITANT. MAY BE CARCINOGENIC. TOXIC.