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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.

Product Description
Calmodulin inhibitor. Antipsychotic and sedative dopamine antagonist. Potent and irreversible inhibitor of cAMP-gated cationic channels. Inhibits DNA repair. Potent neurotoxin.
Product Specific Literature References
New drug evaluations amiloride (Midamor, Merck, Sharp and Dohme): H.L. Macfie, et al.; Drug Intel. Clin. Pharm. 15, 94 (1981) Abstract
Trifluoperazine binding to porcine brain calmodulin and skeletal muscle troponin C: J. Massom, et al.; Biochemistry 29, 671 (1990) Abstract
Inhibition of olfactory cyclic nucleotide-activated current by calmodulin antagonists: S.J. Kleene; Br. J. Pharmacol. 111, 469 (1994) Abstract
Trifluoperazine-induced conformational change in Ca(2+)-calmodulin: M. Vandonselaar, et al.; Nat. Struct. Biol. 1, 795 (1994) Abstract
Inhibition of Nav1.7 and Nav1.4 sodium channels by trifluoperazine involves the local anesthetic receptor: P.L. Sheets, et al.; J. Neurophysiol. 96, 1848 (2006) Abstract
Trifluoperazine protects brain plasma membrane Ca(2+)-ATPase from oxidative damaging: P. Souza dos Santos, et al.; Exp. Brain Res. 177, 347 (2007) Abstract
The antipsychotic drug trifluoperazine inhibits DNA repair and sensitizes non small cell lung carcinoma cells to DNA double-strand break induced cell death: A.G. Polischouk, et al.; Mol. Cancer Ther. 6, 2303 (2007) Abstract
Trifluoperazine stimulates ionizing radiation induced cell killing through inhibition of DNA repair: S. Gangopadhyay, et al.; Mutat. Res. 633, 117 (2007) Abstract
 
 
ALX-380-090 Revised 12-Mar-08
Tryprostatin A
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cytoskeletal Research
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ALX-380-090-C500   500 µg 179.00 USD Add To Cart
Product Specification
FORMULA: C22H27N3O3
MW: 381.5
SOURCE/HOST: Isolated from Aspergillus fumigatus.
PURITY: ≥90%
APPEARANCE: White powder.
SOLUBILITY: Soluble in methanol, 100% ethanol or DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Diketopiperazine. Arrests cell cycle progression at the G2/M phase. Inhibitor of MAP-dependent microtubule assembly. Inhibits the ABC-transporter breast cancer resistance protein (BCRP) and thereby reverses the resistance of cancer cells against antitumor drugs.
Product Specific Literature References
Tryprostatins A and B, novel mammalian cell cycle inhibitors produced by Aspergillus fumigatus: C.B. Cui, et al.; J. Antibiot. 48, 1382 (1995) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. I. Taxonomy, fermentation, isolation and biological properties: C.B. Cui, et al.; J. Antibiot. 49, 527 (1996) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. II. Physico-chemical properties and structures: C.B. Cui, et al.; J. Antibiot. 49, 534 (1996) Abstract
Tryprostatin A, a specific and novel inhibitor of microtubule assembly: T. Usui, et al.; Biochem. J. 333, 543 (1998) Abstract; Full Text
Reversal of breast cancer resistance protein-mediated drug resistance by tryprostatin A: H. Woehlecke, et al.; Int. J. Cancer 107, 721 (2003) Abstract
 
 
ALX-270-168 Revised 18-May-06
Tyrphostin AG 490
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SYNONYMS Tyrphostin B42
N-Benzyl-3,4-dihydroxy-benzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-]N-benzylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-168-M005   5 mg 45.00 USD Add To Cart
ALX-270-168-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C17H14N2O3
MW: 294.3
CAS NUMBER: 133550-30-8
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO and acetone; slightly soluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selectively inhibits CDK2 activation leading to a potent cell cycle arrest at late G1 and S phase. Cell permeable inhibitor of JAK-2 tyrosine kinase. Does not significantly inhibit other kinases, such as Lck, Lyn, Btk, Syk or Src. Blocks IL-7 induced JAK kinase activity in T cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. Valuable tool for studying the cellular role of JAK kinases in signal transduction.
Product Specific Literature References
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors: A. Gazit, et al.; J. Med. Chem. 32, 2344 (1989) Abstract
Tyrosine phosphorylation is an obligatory event in IL-2 secretion [published erratum appears in J Immunol 1991 May 1;146(9):3260]: A. Levitzki; Biochem. Pharmacol. 40, 913 (1990) Abstract
Activation of phosphatidylinositol-3 kinase by ligation of the interleukin-7 receptor is dependent on protein tyrosine kinase activity: H. Dadi, et al.; Blood 84, 1579 (1994) Abstract; Full Text
JAK3 protein tyrosine kinase mediates interleukin-7-induced activation of phosphatidylinositol-3’ kinase: N. Sharfe, et al.; Blood 86, 2077 (1995) Abstract; Full Text
Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor: N. Meydan, et al.; Nature 379, 645 (1996) Abstract
Tyrphostin AG-490 inhibits cytokine-mediated JAK3/STAT5a/b signal transduction and cellular proliferation of antigen-activated human T cells: R.A. Kirken, et al.; J. Leukoc. Biol. 65, 891 (1999) Abstract
JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response: L.H. Wang, et al.; J. Immunol. 162, 3897 (1999) Abstract
JAK2 tyrosine kinase inhibitor tyrphostin AG490 downregulates the mitogen-activated protein kinase (MAPK) and signal transducer and activator of transcription (STAT) pathways and induces apoptosis in myeloma cells: J. De Vos, et al.; Br. J. Haematol. 109, 823 (2000) Abstract
 
 
ALX-270-143 Revised 20-Feb-08
Tyrphostin AG 494
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SYNONYMS Tyrphostin B48
N-Phenyl-3,4-dihydroxybenzylidenecyanoacetamide
α-Cyano-(3,4-dihydroxy)-N-phenylcinnamamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrphostins
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ALX-270-143-M005   5 mg 25.00 USD Add To Cart
ALX-270-143-M025   25 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C16H12N2O3
MW: 280.3
CAS NUMBER: 133550-35-3
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Blocks CDK2 activation and causes cells to arrest at late G1 and during S phase.
Product Specific Literature References
Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases: A. Gazit, et al.; J. Med. Chem. 34, 1896 (1991) Abstract
Tyrphostin AG 494 blocks Cdk2 activation: N. Osherov & A. Levitzki; FEBS Lett. 410, 187 (1997) Abstract
Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase: N. Kleinberger-Doron, et al.; Exp. Cell Res. 241, 340 (1998) Abstract
 
 
ALX-380-222 Revised 03-Jul-08
UCN-01
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SYNONYMS 7-Hydroxystaurosporine
Staurosporine, 7-Hydroxy-
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Staurosporine/Related Products
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ALX-380-222-M001   1 mg 105.00 USD Add To Cart
ALX-380-222-M005   5 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O4
MW: 482.5
CAS NUMBER: 112953-11-4
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5345.
PURITY: ≥99% (HPLC)
APPEARANCE: White film.
SOLUBILITY: Soluble in methanol, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description

Inhibitor of protein kinase C (PKC) and cyclin-dependent kinases (CDKs) resulting in accumulation of cells in the G1 phase and induction of apoptosis. Enhances the cytotoxicity of other anticancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by these agents.

Product Specific Literature References
UCN-01, a selective inhibitor of protein kinase C from Streptomyces: I. Takahashi, et al.; J. Antibiot. (Tokyo) 40, 1782 (1987) Abstract
UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract
UCN-01, 7-hydroxyl-staurosporine, inhibits kinase activity of cyclin-dependent kinases and reduces the phosphorylation of the retinoblastoma susceptibility gene product in A549 human lung cancer cell line: K. Kawakami, et al.; BBRC 219, 778 (1996) Abstract
UCN-01 (7-hydroxystaurosporine) and other indolocarbazole compounds: a new generation of anti-cancer agents for the new century?: S. Akinaga, et al.; Anticancer Drug Des. 15, 43 (2000) Abstract
UCN-01-induced cell cycle arrest requires the transcriptional induction of p21(waf1/cip1) by activation of mitogen-activated protein/extracellular signal-regulated kinase kinase/extracellular signal-regulated kinase pathway: M.M. Facchinetti, et al.; Cancer Res. 64, 3629 (2004) Abstract; Full Text
 
 
ALX-380-206 Revised 13-Nov-07
UCN-02
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Staurosporine/Related Products
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ALX-380-206-M001   1 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C28H26N4O4
MW: 482.5
CAS NUMBER: 121569-61-7
RTECS: KC6600000
SOURCE/HOST: Isolated from Streptomyces sp. MST-AS5346.
PURITY: ≥95% (HPLC)
APPEARANCE: White to pale yellow solid.
SOLUBILITY: Soluble in ethyl acetate, 100% ethanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of protein kinase C (PKC) and protein kinase A (PKA). Although less selective than its isomer UCN-01 (Prod. No. ALX-380-222), UCN-02 exhibits comparable activity and probably acts by similar mechanisms.
Product Specific Literature References
[1] UCN-01 and UCN-02, new selective inhibitors of protein kinase C. II. Purification, physico-chemical properties, structural determination and biological activities: I. Takahashi, et al.; J. Antibiot. (Tokyo) 42, 571 (1989) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Note: Some interconversion of UCN-02 to UCN-01 may occur under acidic HPLC conditions (see [1]).
 
 
ALX-380-056 Revised 10-May-07
Verruculogen
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-056-M001   1 mg 60.00 USD Add To Cart
ALX-380-056-M005   5 mg 225.00 USD Add To Cart
Product Specification
FORMULA: C27H33N3O7
MW: 511.2
CAS NUMBER: 12771-72-1
RTECS: JH4920000
SOURCE/HOST: Isolated from Penicillium verruculosum.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in ethyl acetate, DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
Neurotoxin that acts as an inhibitor of the M phase of the mammalian cell cycle. Inhibits Ca2+-activated K+ channels. Decreases GABA levels in CNS.
Product Specific Literature References
Tremorgenic indole alkaloids potently inhibit smooth muscle high- conductance calcium-activated potassium channels: H.H. Knaus, et al.; Biochemistry 33, 5819 (1994) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. II. Physico- chemical properties and structures: C.B. Cui, et al.; J. Antibiot. (Tokyo) 49, 534 (1996) Abstract
Verruculogen production in airborne and clinical isolates of Aspergillus fumigatus Fres.: I. Kosalec, et al.; Acta Pharm. 55, 357 (2005) Abstract
 
 
ALX-350-257 Revised 08-Apr-08
Vinblastine . sulfate
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SYNONYMS Vincaleukoblastine . sulfate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-257-M005   5 mg 45.00 USD Add To Cart
ALX-350-257-M025   25 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C46H58N4O9 . H2SO4
MW: 811.0 . 98.1
CAS NUMBER: 143-67-9
MERCK INDEX: 14: 9982
SOURCE/HOST: Semisynthetic from catharanthine or vindoline.
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO, methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: CARCINOGENIC. TOXIC.

Product Description
Plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Depolymerizes microtubules and blocks binding of tubulin to microtubule proteins. Induces apoptosis. Triggers Raf-1 activation, phosphorylation of Bcl-2 family proteins and induction of p53 expression.
Product Specific Literature References
Microtubule antagonists activate programmed cell death (apoptosis) in cultured rat hepatocytes: K. Tsukidate, et al.; Am. J. Pathol. 143, 918 (1993) Abstract
Resistance of Ehrlich tumor cells to apoptosis can be due to accumulation of heat shock proteins: V.L. Gabai, et al.; FEBS Lett. 375, 21 (1995) Abstract
The interaction of taxol and vinblastine with radiation induction of p53 and p21 WAF1/CIP1: R.B. Tishler & D.M. Lamppu; Br. J. Cancer. Suppl. 27, S82 (1996) Abstract
Raf-1/bcl-2 phosphorylation: a step from microtubule damage to cell death: M.V. Blagosklonny, et al.; Cancer Res. 57, 130 (1997) Abstract
Tubulin as a target for anticancer drugs: agents which interact with the mitotic spindle: A. Jordan, et al.; Med. Res. Rev. 18, 259 (1998) Abstract
The C terminus of beta-tubulin regulates vinblastine-induced tubulin polymerization: S.S. Rai & J. Wolff; PNAS 95, 4253 (1998) Abstract; Full Text
Caspase-3 activation is not responsible for vinblastine-induced Bcl-2 phosphorylation and G2/M arrest in human small cell lung carcinoma Ms-1 cells: E. Tashiro, et al.; Jpn. J. Cancer Res. 89, 940 (1998) Abstract
Use of drugs to study role of microtubule assembly dynamics in living cells: A. Jordan & L. Wilson; Meth. Enzymol. 298, 252 (1998) Abstract
Vinblastine-induced phosphorylation of Bcl-2 and Bcl-XL is mediated by JNK and occurs in parallel with inactivation of the Raf-1/MEK/ERK cascade: M. Fan, et al.; J. Biol. Chem. 275, 29980 (2000) Abstract; Full Text
Vinblastine, a chemotherapeutic drug, inhibits palmitoylation of tubulin in human leukemic lymphocytes: J.M. Caron & M. Herwood; Chemotherapy 53, 51 (2007) Abstract
 
 
ALX-350-069 Revised 15-Jul-08
Vincristine . sulfate
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SYNONYMS VCR . sulfate
Leukocristine . sulfate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Cell Cycle Research
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ALX-350-069-M001   1 mg 35.00 USD Add To Cart
ALX-350-069-M005   5 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C46H56N4O10 . H2SO4
MW: 825.0 . 98.1
CAS NUMBER: 2068-78-2
MERCK INDEX: 14: 9986
RTECS: OH6340000
SOURCE/HOST: Semisynthetic from catharanthine or vindoline.
PURITY: ≥95%
APPEARANCE: White to off-white powder.
SOLUBILITY: