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ALX-380-014 Revised 15-May-08
Staurosporine
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SYNONYMS Antibiotic AM-2282
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-014-C100   100 µg 47.00 USD Add To Cart
ALX-380-014-C250   250 µg 112.00 USD Add To Cart
ALX-380-014-M001   1 mg 270.00 USD Add To Cart
ALX-380-014-M005   5 mg 790.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O3
MW: 466.5
CAS NUMBER: 62996-74-1
MERCK INDEX: 14: 8802
RTECS: KC655000
SOURCE/HOST: Isolated from Streptomyces staurosporeus.
PURITY: ≥98%
APPEARANCE: Off-white to green powder.
SOLUBILITY: Soluble in ethyl acetate, DMSO or dimethyl formamide; only slightly soluble in chloroform and methanol. Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years after receipt when stored +4°C.
HANDLING: Protect from light and moisture.
HAZARD: HARMFUL. MAY BE CARCINOGENIC.

Product Description
Model apoptosis inducer. Potent cell-permeable inhibitor of a variety of protein kinases, e.g. protein kinase C (PKC), CDK1/cyclin B (IC50~5nM), CDK2/cyclin A (IC50=7nM), CDK4/cyclin D (IC50=3-10µM), CDK5/p25 (IC50=4nM) and GSK-3β (IC50=15nM).
Product Specific Literature References
A new alkaloid AM-2282 of Streptomyces origin. Taxonomy, fermentation, isolation and preliminary characterization: S. Omura, et al.; J. Antibiot. (Tokyo) 30, 275 (1977) Abstract
A. Furusaki, et al.; J. C. S. Chem. Commun. 800 (1978)
Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase: T. Tamaoki, et al.; BBRC 135, 397 (1986) Abstract
Staurosporine, a potent platelet aggregation inhibitor from a Streptomyces species: S. Oka, et al.; Agric. Biol. Chem. 50, 2723 (1986)
Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60: N. Nakano, et al.; J. Antibiot. (Tokyo) 40, 706 (1987) Abstract
Contrasting actions of staurosporine, a protein kinase C inhibitor, on human neutrophils and primary mouse epidermal cells: T. Sako, et al.; Cancer Res. 48, 4646 (1988) Abstract
Staurosporine, a protein kinase C inhibitor interferes with proliferation of arterial smooth muscle cells: H. Matsumoto & Y. Sasaki; Biochem. Biophys. Res. Commun. 158, 105 (1989) Abstract
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989), (Review) Abstract
Staurosporine: an effective inhibitor for Ca2+/calmodulin-dependent protein kinase II: N. Yanagihara, et al.; J. Neurochem. 56, 294 (1991) Abstract
Is staurosporine a specific inhibitor of protein kinase C in intact porcine coronary arteries?: M. Kageyama, et al.; J. Pharmacol. Exp. Ther. 259, 1019 (1991) Abstract
Induction of a common pathway of apoptosis by staurosporine: R. Bertrand, et al.; Exp. Cell Res. 211, 314 (1994) Abstract
First total synthesis of Staurosporine and ent-Staurosporine: J.T. Link et al.; J. Am. Chem. Soc. 117, 552 (1995)
Staurosporine induces programmed cell death in embryonic neurons and activation of the ceramide pathway: D.A. Wiesner & G. Dawson; J. Neurochem 66, 1418 (1996) Abstract
Staurosporine and ent-staurosporine: the first total synthesis, prospects for a regioselective approach, and activity profile: J.T. Link et al.; J. Am. Chem. Soc. 118, 2825 (1996)
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996), Review Abstract
Characterization of the cell death process induced by staurosporine in human neuroblastoma cell lines: J. Boix, et al.; Neuropharmacology 36, 811 (1997) Abstract
Caspase-3-dependent cleavage of Bcl-2 promotes release of cytochrome c: D.G. Kirsch, et al.; J. Biol. Chem. 274, 21155 (1999) Abstract; Full Text
Molecular mechanism of staurosporine-induced apoptosis in osteoblasts: H.J. Chae, et al.; Pharmacol. Res. 42, 373 (2000) Abstract
Glycogen synthase kinase-3beta facilitates staurosporine- and heat shock-induced apoptosis. Protection by lithium: G.N. Bijur, et al.; J. Biol. Chem. 275, 7583 (2000) Abstract; Full Text
Dissociation of staurosporine-induced apoptosis from G2-M arrest in SW620 human colonic carcinoma cells: initiation of the apoptotic cascade is associated with elevation of the mitochondrial membrane potential (deltapsim): B.G. Heerdt, et al.; Cancer Res. 60, 6704 (2000) Abstract
Changes in mitochondrial membrane potential during staurosporine- induced apoptosis in Jurkat cells: J.L. Scarlett, et al.; FEBS Lett. 475, 267 (2000) Abstract
Equivalent death of P-glycoprotein expressing and nonexpressing cells induced by the protein kinase C inhibitor staurosporine: K.M. Tainton, et al.; BBRC 276, 231 (2000) Abstract
Caspase-8 activation and bid cleavage contribute to MCF7 cellular execution in a caspase-3-dependent manner during staurosporine-mediated apoptosis: D. Tang, et al.; J. Biol. Chem. 275, 9303 (2000) Abstract; Full Text
Insulin-stimulated protein kinase B phosphorylation on Ser-473 is independent of its activity and occurs through a staurosporine-insensitive kinase: M.M. Hill, et al.; J. Biol. Chem. 276, 25643 (2001) Abstract; Full Text
Single-cell fluorescence resonance energy transfer analysis demonstrates that caspase activation during apoptosis is a rapid process. Role of caspase-3: M. Rehm, et al.; J. Biol. Chem. 277, 24506 (2002) Abstract; Full Text
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Further Categories Containing This Product:
CDK & Cyclin Inhibitors • PKC Inhibitors • Myosin Light Chain Kinase Inhibitors • Staurosporine/Related Products • Antibiotics - Protein Kinase Inhibitors • Alkaloids • Antibiotics for Cell Cycle Research
 
 
ALX-630-116 Revised 15-Aug-08
Sterigmatocystin
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SYNONYMS 3a,12c-Dihydro-8-hydroxy-6-methoxy-7H-furol[3’,2’:4,5]furo[2,3-c]xanthen-7-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Mycotoxins
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ALX-630-116-M001   1 mg 35.00 USD Add To Cart
ALX-630-116-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C18H12O6
MW: 324.3
CAS NUMBER: 10048-13-2
RTECS: LV1750000
SOURCE/HOST: Isolated from Aspergillus versicolor.
PURITY: ≥98% (TLC, HPLC)
APPEARANCE: Pale yellow solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol or acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description

Mycotoxin produced by strains of the common molds. Inhibitor of DNA synthesis. Induces sister chromatid exchanges in bone marrow cells of mice. Causes necrosis.
Product Specific Literature References
Effect of sterigmatocystin on rat liver nuclear RNA: W. Nel & H.E. Pretorius; Biochem. Pharmacol. 19, 957 (1970) Abstract
Massive and single cell necrosis in the rat liver induced by aflatoxin B1 and sterigmatocystin: K. Terao; Acta Pathol. Jpn. 23, 647 (1973) Abstract
Induction of sister-chromatid exchanges in vivo in mice by the mycotoxins sterigmatocystin and griseofulvin: P.T. Curry, et al.; Mutat. Res. 137, 111 (1984) Abstract
Cytotoxicity of occupationally and environmentally relevant mycotoxins: J. Bünger, et al.; Toxicology 202, 199 (2004) Abstract
An aflatoxin biosynthesis cluster gene encodes a novel oxidase required for conversion of versicolorin a to sterigmatocystin: K.C. Ehrlich, et al.; Appl. Environ. Microbiol. 71, 8963 (2005) Abstract; Full Text
Aspergillus mycotoxins and their effect on the host: K. Kamei & A. Watanabe; Med. Mycol. 43, S95 (2005) Abstract
A novel biosensor for sterigmatocystin constructed by multi-walled carbon nanotubes (MWNT) modified with aflatoxin-detoxifizyme (ADTZ): D.S. Yao, et al.; Bioelectrochemistry 68, 126 (2006) Abstract
Further Categories Containing This Product:
DNA Replication Inhibitors • Non-apoptotic Cell Death/Necrosis
 
 
ALX-270-400 Revised 31-Mar-05
SU 9516
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SYNONYMS 3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-400-M005   5 mg 80.00 USD Add To Cart
ALX-270-400-M025   25 mg 320.00 USD Add To Cart
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Product Specification
FORMULA: C13H11N3O2
MW: 241.3
PURITY: ≥95%
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC50=22nM), CDK1/cyclin B (IC50=40nM) and CDK4/cyclin D1 (IC50=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC50>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells. Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.
Product Specific Literature References
A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells: M.E. Lane, et al.; Cancer Res. 61, 6170 (2001) Abstract
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells: B. Yu, et al.; Biochem Pharmacol. 64, 1091 (2002) Abstract
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2: D.J. Moshinsky, et al.; BBRC 310, 1026 (2003) Abstract
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors: X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003) Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Anti-proliferative)
 
 
ALX-385-027 Revised 08-Feb-08
Tangeretin
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SYNONYMS 2-(4-Methoxyphenyl)-5,6,7,8-tetramethoxy-4H-1-benz-1-benzopyran-4-one
4’,5,6,7,8-Pentamethoxyflavone
Ponkanetin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavonoids/Related Products
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ALX-385-027-M010   10 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C20H20O7
MW: 372.4
CAS NUMBER: 481-53-8
RTECS: DJ3102725
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol or ethyl acetate; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Flavonoid found in the peel of citrus fruits where it provides natural resistance to fungi. Induces G1 cell cycle arrest in cancer cells. Counteracts tumor promoter-induced inhibition of intercellular communication and inhibits cell proliferation in several cancer lines. Reduces elevation of blood pressure and plasma glucose levels.
Product Specific Literature References
Nobiletin Is Main Fungistat in Tangerines Resistant to Mal Secco: A. Ben-Aziz; Science 155, 1026 (1967) Abstract
Flavonoids (apigenin, tangeretin) counteract tumor promoter-induced inhibition of intercellular communication of rat liver epithelial cells: C. Chaumontet, et al.; Cancer Lett. 114, 207 (1997) Abstract
Antiproliferative activity of flavonoids on several cancer cell lines: S. Kawaii; Biosci. Biotechnol. Biochem. 63, 896 (1999) Abstract
Tangeretin inhibits extracellular-signal-regulated kinase (ERK) phosphorylation: S. Van Slambrouck, et al.; FEBS Lett. 579, 1665 (2005) Abstract
Tangeretin and nobiletin induce G1 cell cycle arrest but not apoptosis in human breast and colon cancer cells: K.L. Morley, et al.; Cancer Lett. 251, 168 (2007) Abstract
Tangeretin suppresses IL-1beta-induced cyclooxygenase (COX)-2 expression through inhibition of p38 MAPK, JNK, and AKT activation in human lung carcinoma cells: K.H. Chen, et al.; Biochem. Pharmacol. 73, 215 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products • Active Substances from Fruit and Vegetables • Natural Products - Antifungal Agents • Natural Products - Antitumor Reagents • Natural Products for Cell Cycle Research
 
 
ALX-350-340 Revised 14-Nov-07
Thielavin B
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
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ALX-350-340-MC05   0.5 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C31H34O10
MW: 566.6
CAS NUMBER: 71950-67-9
SOURCE/HOST: Isolated from an unidentified fungus MST-FP1888.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Fungal metabolite. Glucose-6-phosphatase inhibitor. Potent inhibitor of phospholipase C. Inhibits telomerase, viral reverse transcriptase, peptidoglycan formation and prostaglandin biosynthesis.
Product Specific Literature References
Thielavin A and B, new inhibitors of prostaglandin biosynthesis produced by Thielavia terricola: N. Kitahara, et al.; J. Antibiot. (Tokyo) 34, 1562 (1981) Abstract
The structures of thielavins A, B and C. Prostaglandin synthetase inhibitors from fungi: N. Kitahara, et al.; J. Antibiot. (Tokyo) 36, 599 (1983) Abstract
Screening systems for detecting inhibitors of cell wall transglycosylation in Enterococcus. Cell wall transglycosylation inhibitors in Enterococcus: N. Mani, et al.; J. Antibiot. (Tokyo) 51, 471 (1998) Abstract
Inhibition of telomerase activity by fungus metabolites, CRM646-A and thielavin B: K. Togashi, et al.; Biosci. Biotechnol. Biochem. 65, 651 (2001) Abstract; Full Text
Thielavins as glucose-6-phosphatase (G6Pase) inhibitors: producing strain, fermentation, isolation, structural elucidation and biological activitie: S. Sakemi, et al.; J. Antibiot. (Tokyo) 55, 941 (2002) Abstract
Further Categories Containing This Product:
Phospholipase C/Related Products • Telomerase/Related Products • Prostaglandin Synthases/Related Products
 
 
ALX-270-439 Revised 18-Sep-06
Trans-24
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SYNONYMS (5R,11aS)-2-Benzyl-5-(3-hydroxyphenyl)-6H-1,2,3,5,11,11a-hexahydroimidazo[1,5-b]-β-carboline-1,3-dione
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY Cell Cycle Blockers & Inhibitors/Related Products
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ALX-270-439-M001   1 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C26H21N3O3
MW: 423.5
CAS NUMBER: 869304-55-2
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 6 months when stored at -20°C in the dark.
HANDLING: Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Potent, cell permeable non-tubulin-interacting mitosis inhibitor. Blocks mitosis (IC50=650nM) by binding to the mitotic kinesin Eg5.
Product Specific Literature References
Synthesis and biological evaluation of new tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin Eg5: N. Sunder-Plassmann, et al.; Bioorg. Med. Chem. 13, 6094 (2005) Abstract
Further Categories Containing This Product:
Kinesin & Kinesin-like Proteins/Related Products
 
 
ALX-380-068 Revised 09-Apr-08
Trichostatin A
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SYNONYMS TSA
[R-(E,E)]-7-[4-(Dimethylamino)phenyl]-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Antibiotics - DNA Regulation/Transcription
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-068-M001   1 mg 115.00 USD Add To Cart
ALX-380-068-M005   5 mg 385.00 USD Add To Cart
Product Specification
FORMULA: C17H22N2O3
MW: 302.4
CAS NUMBER: 58880-19-6
MERCK INDEX: 14: 9649
SOURCE/HOST: Isolated from Streptomyces hygroscopicus.
PURITY: ≥98% (HPLC)
APPEARANCE: Whitish film adhered to inside of vial.
SOLUBILITY: Soluble in DMSO, dimethyl formamide, acetonitrile, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Potent, reversible inhibitor of histone deacetylase (HDAC). Mediates the activation of O6-methylguanine-DNA methyltransferase (MGMT). May be involved in cell cycle progression of several cell types. Induces cell growth arrest at both G1 and G2/M phases. May induce apoptosis in some cases. Induces acetylation of histone-3/4 and expression of p300.
Product Specific Literature References
A new antifungal antibiotic, trichostatin: N. Tsuji, et al.; J. Antibiot. 29, 1 (1976) Abstract
Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A: M. Yoshida, et al.; J. Biol. Chem. 265, 17174 (1990) Abstract; Full Text
Trichostatin A induces morphological changes and gelsolin expression by inhibiting histone deacetylase in human carcinoma cell lines: Y. Hoshikawa, et al.; Exp. Cell Res. 214, 189 (1994) Abstract
Trichostatin A inhibits both ras-induced neurite outgrowth of PC12 cells and morphological transformation of NIH3T3 cells: M. Futamura, et al.; Oncogene 10, 1119 (1995) Abstract
Trichostatin A and trapoxin: novel chemical probes for the role of histone acetylation in chromatin structure and function: M. Yoshida, et al.; Bioessays 17, 423 (1995) Abstract
Selective inhibition of IL-2 gene expression by trichostatin A, a potent inhibitor of mammalian histone deacetylase: I. Takahashi, et al.; J. Antibiot. 49, 453 (1996) Abstract
A mammalian histone deacetylase related to the yeast transcriptional regulator Rpd3p: J. Taunton, et al.; Science 272, 408 (1996) Abstract
Transcriptional activation and chromatin remodeling of the HIV-1 promoter in response to histone acetylation: C. Van Lint, et al.; EMBO J. 15, 1112 (1996) Abstract
Induction of caspase-3 protease activity and apoptosis by butyrate and trichostatin A (inhibitors of histone deacetylase): dependence on protein synthesis and synergy with a mitochondrial/cytochrome c- dependent pathway:: V. Medina, et al.; Cancer Res. 57, 3697 (1997) Abstract
A histone deacetylase inhibitor potentiates retinoid receptor action in embryonal carcinoma cells: S. Minucci, et al.; PNAS 94, 11295 (1997) Abstract; Full Text
Histone deacetylase inhibitor activates the WAF1/Cip1 gene promoter through the Sp1 sites: Y. Sowa, et al.; BBRC 241, 142 (1997) Abstract
Retinoblastoma protein recruits histone deacetylase to repress transcription: A. Brehm, et al.; Nature 391, 597 (1998) Abstract
Effects of cell density and trichostatin A on the expression of HDAC1 and p57Kip2 in Hep 3B cells: S.G. Gray & T.J. Ekstrom; BBRC 245, 423 (1998) Abstract
Regulation of the human O6-methylguanine-DNA methyltransferase gene by transcriptional coactivators cAMP response element-binding protein- binding protein and p300: K.K. Bhakat & S. Mitra; J. Biol. Chem. 275, 34197 (2000) Abstract; Full Text
Histone deacetylase inhibitors: inducers of differentiation or apoptosis of transformed cells: P.A. Marks, et al.; J. Natl. Cancer Inst. 92, 1210 (2000) Abstract
Trichostatin A is a histone deacetylase inhibitor with potent antitumor activity against breast cancer in vivo: D.M. Vigushin, et al.; Clin. Cancer Res. 7, 971 (2001) Abstract
Chromatin remodeling agent trichostatin A: a key-factor in the hepatic differentiation of human mesenchymal stem cells derived of adult bone marrow: S. Snykers, et al.; BMC Dev. Biol. 7, 24 (2007) Abstract
Trichostatin A induces myocardial differentiation of monkey ES cells: M. Hosseinkhani, et al.; BBRC 356, 386 (2007) Abstract
Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors/Related Products • Antibiotics - Other Signal Transduction Pathway Modulators • Antibiotics - Apoptosis Inducers & Inhibitors • HDAC Inhibitors • PKC Activators • Antibiotics - Antifungal • Antitumor Antibiotics • Antibiotics for Cell Cycle Research • DNA Repair Other Products • DNA & RNA Methyl & Alkyl Transferases/Related Products
 
 
ALX-550-310 Revised 03-Jun-08
Trifluoperazine . dihydrochloride
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calmodulin Inhibitors
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ALX-550-310-G001   1 g 20.00 USD Add To Cart
ALX-550-310-G005   5 g 75.00 USD Add To Cart
Product Specification
FORMULA: C21H24F3N3S . 2HCl
MW: 407.5 . 73.0
CAS NUMBER: 440-17-5
MERCK INDEX: 14: 9680
RTECS: SP1750000
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and moisture.
HAZARD: HARMFUL.