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ALX-270-047 Revised 26-Sep-07
Aristolochic acid
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SYNONYMS 8-Methoxy-6-nitrophenanthrol(3,4-d)-1,3-dioxide-5-carboxylic acid
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-270-047-M025   25 mg 25.00 USD Add To Cart
ALX-270-047-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H11NO7
MW: 341.3
CAS NUMBER: 313-67-7
MERCK INDEX: 14: 786
RTECS: CF3325000
SOURCE/HOST: Isolated from Aristolochia clematis.
PURITY: ≥97% (~1:1 mixture of aristolochic acids I (A) and II (B))
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: MAY BE CARCINOGENIC. TOXIC. MAY BE MUTAGENIC.

Product Description
Phospholipase A2 (PLA2) inhibitor active against the enzymes found in many snake venoms as well as those of human platelets and synovial fluids. Inhibits ionophore-stimulated PLA2 activity in human neutrophils. Has been shown to be nephropathic and carcinogenic.
Product Specific Literature References
Characterization of three edema-inducing phospholipase A2 enzymes from habu (Trimeresurus flavoviridis) venom and their interaction with the alkaloid aristolochic acid: B.S. Vishwanath, et al.; Toxicon 25, 501 (1987) Abstract
Interaction of aristolochic acid with Vipera russelli phospholipase A2: its effect on enzymatic and pathological activities: B.S. Vishwanath & T.V. Gowda; Toxicon 25, 929 (1987) Abstract
Interaction of phospholipase A2 from Vipera russelli venom with aristolochic acid: a circular dichroism study: B.S. Vishwanath, et al.; Toxicon 25, 939 (1987) Abstract
Edema-inducing activity of phospholipase A2 purified from human synovial fluid and inhibition by aristolochic acid: B.S. Vishwanath, et al.; Inflammation 12, 549 (1988) Abstract
Effects of aristolochic acid on phospholipase A2 activity and arachidonate metabolism of human neutrophils: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1001, 3 (1989) Abstract
Suramin alters phosphoinositide synthesis and inhibits growth factor receptor binding in HT-29 cells: R. Kopp & A. Pfeiffer; Cancer Res. 50, 6490 (1990) Abstract
The effects of the phospholipase A2 inhibitors aristolochic acid and PGBx on A23187-stimulated mobilization of arachidonate in human neutrophils are overcome by diacylglycerol or phorbol ester: M.D. Rosenthal, et al.; Biochim. Biophys. Acta 1126, 319 (1992) Abstract
Evidence for different mechanisms involved in the formation of lyso platelet-activating factor and the calcium-dependent release of arachidonic acid from human neutrophils: J.D. Winkler, et al.; Biochem. Pharmacol. 44, 2055 (1992) Abstract
Selective inhibition of group II phospholipase A2 by quercetin: M. Lindahl & C. Tagesson; Inflammation 17, 573 (1993) Abstract
Detection of DNA adducts formed by aristolochic acid in renal tissue from patients with Chinese herbs nephropathy: H.H. Schmeiser, et al.; Cancer Res. 56, 2025 (1996) Abstract
Aristolochic acid and ’Chinese herbs nephropathy’: a review of the evidence to date: J.P. Cosyns; Drug Saf. 26, 33 (2003), Review Abstract
Effect of aristolochic acid on intracellular calcium concentration and its links with apoptosis in renal tubular cells: Y.H. Hsin, et al.; Apoptosis 11, 2167 (2006) Abstract
Further Categories Containing This Product:
PLA2 Inhibitors • Carcinogens & Tumor Promoters Other Products • Natural Products - Other Tumor Promoters • Other Toxins • Alkaloids
 
 
ALX-270-256 Revised 28-Apr-05
Clofibrate
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SYNONYMS 2-(p-Chlorophenoxy)-2-methylpropionic acid ethyl ester
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-256-M500   500 mg 15.00 USD Add To Cart
ALX-270-256-G001   1 g 25.00 USD Add To Cart
Product Specification
FORMULA: C12H15ClO3
MW: 242.7
CAS NUMBER: 637-07-0
MERCK INDEX: 14: 2377
PURITY: ≥98%
APPEARANCE: Colorless oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions are stable for up to 6 months when stored at –20°C.

Product Description
Activates PPARα and induces cytochrome P450 4A1 and 4A3.
Product Specific Literature References
Fatty acids activate a chimera of the clofibric acid-activated receptor and the glucocorticoid receptor: M. Göttlicher, et al.; PNAS 89, 4653 (1992) Abstract
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Further Categories Containing This Product:
Cytochrome P450 [CYP450] / Related Products • Carcinogens & Tumor Promoters Other Products • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-419 Revised 08-Oct-08
NU6102
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SYNONYMS O6-Cyclohexylmethyl-2-(4’-sulfamoylanilino)purine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-419-M001   1 mg 50.00 USD Add To Cart
ALX-270-419-M005   5 mg 145.00 USD Add To Cart
Product Specification
FORMULA: C18H22N6O3S
MW: 402.5
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Packaged under inert gas. Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
1,000-fold more potent inhibitor of CDK1/cyclin B (IC50=9.5nM) and CDK2/cyclin A3 (IC50=5.4nM) than NU2058 (Prod. No. ALX-270-394). Selective for CDK1 and CDK2 compared to CDK4/D1 (IC50=1.6µM), DYRK1A (IC50=0.9µM), PDK1 (IC50=0.8µM) and ROCKII (IC50=0.6µM).
Product Specific Literature References
Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor: T.G. Davies, et al.; Nat. Struct. Biol. 9, 745 (2002) Abstract
Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2: K.L. Sayle, et al.; Bioorg. Med. Chem. Lett. 13, 3079 (2003) Abstract
N2-substituted O6-cyclohexylmethylguanine derivatives: potent inhibitors of cyclin-dependent kinases 1 and 2: I.R. Hardcastle, et al.; J. Med. Chem. 47, 3710 (2004) Abstract
Further Categories Containing This Product:
Carcinogens & Tumor Promoters Other Products
 
 
ALX-350-004 Revised 08-Apr-08
Thapsigargin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Tumor Promoters
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-004-M001   1 mg 50.00 USD Add To Cart
ALX-350-004-M005   5 mg 200.00 USD Add To Cart
ALX-350-004-M010   10 mg 350.00 USD Add To Cart
ALX-350-004-M025   25 mg 690.00 USD Add To Cart
Product Specification
FORMULA: C34H50O12
MW: 650.8
CAS NUMBER: 67526-95-8
MERCK INDEX: 14: 9272
PURITY: ≥95% (HPLC)
APPEARANCE: Clear colorless film.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and oxygen.
HAZARD: HIGHLY IRRITANT. HARMFUL.

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Product Description
Cell permeable tumor promoter by specific inhibition of the (sarco)endoplasmatic reticulum Ca2+-ATPase (SERCA). Inhibition of SERCA reveals a significant change in intracellular Ca2+ homeostasis and pH regulation in tumor cells. Does not increase inositol phosphates. Shows no effect on protein kinase C (PKC). Increases Ca2+-dependent Na+ influx in human platelets in a dose-dependent manner. Induces apoptosis. Stimulates nitric oxide (NO) production, contributing to hepatocyte apoptosis.
Product Specific Literature References
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Thapsigargin, a Ca(2+)-ATPase inhibitor, depletes the intracellular Ca2+ pool and induces apoptosis in human hepatoma cells: A. Tsukamoto & Y. Kaneko; Cell Biol. Int. 17, 969 (1993) Abstract
The role of calcium, pH, and cell proliferation in the programmed (apoptotic) death of androgen-independent prostatic cancer cells induced by thapsigargin: Y. Furuya, et al.; Cancer Res. 54, 6167 (1994) Abstract
Intracellular Ca2+ signals activate apoptosis in thymocytes: studies using the Ca(2+)-ATPase inhibitor thapsigargin: S. Jiang, et al.; Exp. Cell Res. 212, 84 (1994) Abstract
Role of EGR-1 in thapsigargin-inducible apoptosis in the melanoma cell line A375-C6: S. Muthukkumar, et al.; Mol. Cell. Biol. 15, 6262 (1995) Abstract; Full Text
Baculovirus p35 and Z-VAD-fmk inhibit thapsigargin-induced apoptosis of breast cancer cells: X.M. Qi, et al.; Oncogene 15, 1207 (1997) Abstract
Signal transduction of thapsigargin-induced apoptosis in osteoblast: H.J. Chae, et al.; Bone 25, 453 (1999) Abstract
Nitric oxide is involved in apoptosis induced by thapsigargin in rat mesangial cells: A.M. Rodriguez-Lopez, et al.; Cell Physiol. Biochem. 9, 285 (1999) Abstract
Thapsigargin induces apoptosis in cultured human aortic smooth muscle cells: C. Peiro, et al.; J. Cardiovasc. Pharmacol. 36, 676 (2000) Abstract
Thapsigargin induces a calmodulin/calcineurin-dependent apoptotic cascade responsible for the death of prostatic cancer cells: B. Tombal, et al.; Prostate 43, 303 (2000) Abstract
Changes in intracellular Ca2+ and pH in response to thapsigargin in human glioblastoma cells and normal astrocytes: G.G. Kovacs, et al.; Am. J. Physiol. Cell. Physiol. 289, C361 (2005) Abstract
Thapsigargin, a selective inhibitor of sarco-endoplasmic reticulum Ca2+ -ATPases, modulates nitric oxide production and cell death of primary rat hepatocytes in culture: N.K. Canova, et al.; Cell Biol. Toxicol. 23, 337 (2007) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Dissolving of 0.65mg Thapsigargin in 1ml gives a stock solution of 1mM.
General Literature References
Role of Ca2(+)-ATPases in regulation of cellular Ca2+ signalling, as studied with the selective microsomal Ca2(+)-ATPase inhibitor, thapsigargin: O. Thastrup; Agents Actions 29, 8 (1990), (Review) Abstract
Thapsigargin, a high affinity and global inhibitor of intracellular Ca2+ transport ATPases: G. Inesi and Y. Sagara; Arch. Biochem. Biophys. 298, 313 (1992), (Review) Abstract
Use of thapsigargin to study Ca2+ homeostasis in cardiac cells: T.B. Rogers, et al.; Biosci. Rep. 15, 341 (1995), (Review) Abstract
The sarcoplasmic reticulum Ca2+ pump: inhibition by thapsigargin and enhancement by adenovirus-mediated gene transfer: G. Inesi, et al.; Ann. NY Acad. Sci. 853, 195 (1998), (Review) Abstract; Full Text
A tool coming of age: thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca(2+)-ATPases: M. Treiman, et al.; TIPS 19, 131 (1998), (Review) Abstract
Further Categories Containing This Product:
Ca2+-ATPase / Related Products • Endoplasmatic Reticulum Stress • Other Natural Products - DNA Regulation / Transcription • Carcinogens & Tumor Promoters Other Products • Natural Products - ATPase Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • Natural Products - Apoptosis Inducers & Inhibitors • Nuclear Envelope & Nuclear Transport • Autophagy Other Products
 
 
ALX-350-012 Revised 23-Oct-08
Microcystin-LR
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Microcystins
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-012-C050   50 µg 24.00 USD Add To Cart
ALX-350-012-C100   100 µg 46.00 USD Add To Cart
ALX-350-012-C500   500 µg 175.00 USD Add To Cart
ALX-350-012-M001   1 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C49H74N10O12
MW: 995.2
CAS NUMBER: 101043-37-2
RTECS: GT2810000
SOURCE/HOST: Isolated from Microcystis aeruginosa.
PURITY: ≥95% (HPLC)
APPEARANCE: Whitish film adhered to inside of the vial.
SOLUBILITY: Soluble in 100% ethanol, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at -20°C. Unstable at pH>7.7.
HANDLING: For maximum product recovery after thawing, centrifuge the vial before opening the cap.
HAZARD: MAY BE CARCINOGENIC. VERY TOXIC. HIGHLY IRRITANT.

Product Description
Heptapeptide ester hepatotoxin. Tumor promoter. Equally potent and selective inhibitor of protein phosphatase 1 (PP1) and 2A (PP2A). PP2B is less sensitive and PP2C is not inhibited up to 4µM. Useful for affinity-purification of PP2A. The product is not cell permeable except in liver cells, which appear to have a functional uptake system. Has no effect on protein kinases. Less toxic than the more hydrophobic analogs microcystin-LY, -LW and -LF. Frequently contaminates fresh-water lakes and ponds. Causes livestock poisonings. Ozonation did lead to complete loss of toxicity and toxins from contaminated samples.
Product Specific Literature References
Structural studies on cyanoginosins-LR, -YR, -YA, and -YM, peptide toxins from Microcystis aeruginosa: D.P. Botes, et al.; JCS Perkin Trans. I, 2747 (1985)
Nodularin, microcystin, and the configuration of Adda: K.L. Rinehart, et al.; JACS 110, 8557 (1988)
Characterization of microcystin-LR, a potent inhibitor of type 1 and type 2A protein phosphatases: R.E. Honkanen, et al.; J. Biol. Chem. 265, 19401 (1990) Abstract; Full Text
Cyanobacterial microcystin-LR is a potent and specific inhibitor of protein phosphatases 1 and 2A from both mammals and higher plants: C. MacKintosh, et al.; FEBS Lett. 264, 187 (1990) Abstract
Protein phosphatase 2A is a specific protamine-kinase-inactivating phosphatase: G.D. Amick, et al.; Biochem. J. 287, 1019 (1992) Abstract
Evidence for the regulation of exocytic transport by protein phosphorylation: H.W. Davidson, et al.; J. Cell. Biol. 116, 1343 (1992) Abstract
Liver tumor promotion by the cyanobacterial cyclic peptide toxin microcystin-LR: R. Nishiwaki-Matsushima, et al.; J. Cancer Res. Clin. Oncol. 118, 420 (1992) Abstract
Two significant aspects of microcystin-LR: specific binding and liver specificity: R. Nishiwaki, et al.; Cancer Lett. 83, 283 (1994) Abstract
Comparative toxicity of four microcystins of different hydrophobicities to the protozoan, Tetrahymena pyriformis: C.J. Ward & G.A. Codd; J. Appl. Microbiol. 86, 874 (1999) 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
The toxicology of microcystin-LR: occurrence, toxicokinetics, toxicodynamics, diagnosis and treatment: K. Bischoff; Vet. Hum. Toxicol. 43, 294 (2001), Review Abstract
Negative regulation of ERK and Elk by protein kinase B modulates c-Fos transcription: I. Galetic, et al.; J. Biol. Chem. 278, 4416 (2003) Abstract; Full Text
Decrease in toxicity of microcystins LA and LR in drinking water by ozonation: S. Brooke, et al.; Toxicon. 48, 1054 (2006) Abstract
Mitochondria a key role in microcystin-LR kidney intoxication: R. La-Salete, et al.; J. Appl. Toxicol. 28, 55 (2008) Abstract
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Further Categories Containing This Product:
Other Toxins • Natural Products - Other Tumor Promoters • Carcinogens & Tumor Promoters Other Products • Marine Natural Products
 
 
ALX-350-014 Revised 03-Apr-08
Calyculin A
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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-350-016 Revised 31-Jul-08
(+)-Aphidicolin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-016-M001   1 mg 65.00 USD Add To Cart
ALX-350-016-M005   5 mg 260.00 USD Add To Cart
ALX-350-016-M025   25 mg 890.00 USD Add To Cart
Product Specification
FORMULA: C20H34O4
MW: 338.5
CAS NUMBER: 38966-21-1
MERCK INDEX: 14: 727
RTECS: PB9185000
SOURCE/HOST: Isolated from Nigrospora oryzae.
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), methanol (10mg/ml) or 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Reversible inhibitor of eukaryotic nuclear DNA replication. Useful for cell synchronization. Blocks the cell cycle at early S phase. Prolongs the half life of DNA methyl