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Antitumor Agents (Apoptosis Inducers)
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ALX-350-113 Revised 28-May-08
Gossypol
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SYNONYMS 2,2’-bis[8-Formyl-1,6,7-trihydroxy-5-isopropyl-3-
methylnaphthalene]
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-113-M100   100 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C30H30O8
MW: 518.6
CAS NUMBER: 303-45-7
MERCK INDEX: 14: 4528
RTECS: DU3100000
SOURCE/HOST: Isolated from Gossypium genus, Malvaceae.
PURITY: ≥90%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in acetone or DMSO; sparingly soluble in 100% ethanol (2mg/ml) or methanol (2mg/ml). Insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Mixture of ~65% (+)- and ~35% (-)-enantiomers. Male antifertility agent. Shows antitumor, antiviral and antioxidant actions. Small molecule inhibitor of Bcl-2/Bcl-XL. Induces apoptosis. Synergizes with radiation and chemotherapy in vitro. Reversible inhibitor of protein phosphatase 2B (PP2B; calcineurin). Protein kinase C (PKC) inhibitor.
Product Specific Literature References
Binding of gossypol to purified tubulin and inhibition of its assembly into microtubules: F.J. Medrano and J.M. Andreu; Eur. J. Biochem. 158, 63 (1986) Abstract
Differential inhibition of protein kinase C subtypes: J.M. Pelosin, et al.; BBRC 169, 1040 (1990) Abstract
Induction of apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells by pharmacological inhibitors of protein kinase C: W.D. Jarvis, et al.; Cancer Res. 54, 1707 (1994) Abstract
Gossypol arrests human benign prostatic hyperplastic cell growth at G0/G1 phase of the cell cycle: F. Shidaifat, et al.; Anticancer Res. 17, 1003 (1997) Abstract
Inhibition of huntingtin fibrillogenesis by specific antibodies and small molecules: implications for Huntington’s disease therapy: V. Heiser, et al.; PNAS 97, 6739 (2000) Abstract; Full Text
Cytotoxic effect of gossypol on colon carcinoma cells: X. Wang, et al.; Life Sci. 67, 2663 (2000) Abstract
Reversible inhibition of calcineurin by the polyphenolic aldehyde gossypol: R. Baumgrass, et al.; J. Biol. Chem. 276, 47914 (2001) Abstract; Full Text
Toxicity of (+)- and (-)-gossypol to the plant pathogen, Rhizoctonia solani: L.S. Puckhaber, et al.; J. Agric. Food Chem. 50, 7017 (2002) Abstract
Telomerase inhibitors in anticancer therapy: gossypol as a potential telomerase inhibitor: M. Mego; Bratisl. Lek. Listy 103, 378 (2002) Abstract
An in vitro study of inhibitory activity of gossypol, a cottonseed extract, in human carcinoma cell lines: M. Le Blanc, et al.; Pharmacol. Res. 46, 551 (2002) Abstract
Gossypol induces chloride secretion in rat proximal colon: G. Kuhn, et al.; Eur. J. Pharmacol. 457, 187 (2002) Abstract
Determination of the absolute configuration and solution conformation of gossypol by vibrational circular dichroism: T.B. Freedman, et al.; Chirality 15, 196 (2003) Abstract
In vitro effects of the BH3 mimetic, (-)-gossypol, on head and neck squamous cell carcinoma cells: C.L. Oliver, et al.; Clin. Cancer Res. 10, 7757 (2004) Abstract; Full Text
The inhibitory effects of gossypol on human prostate cancer cells-PC3 are associated with transforming growth factor beta1 (TGFbeta1) signal transduction pathway: J. Jiang, et al.; Anticancer Res. 24, 19 (2004) Abstract
(-)-Gossypol enhances response to radiation therapy and results in tumor regression of human prostate cancer: L. Xu, et al.; Mol. Cancer Ther. 4, 197 (2005) Abstract; Full Text
Investigations on gossypol: past and present developments: K. Dodou; Expert Opin. Investig. Drugs 14, 1419 (2005) Abstract
An in vitro study of cytotoxic effects of gossypol on human epidermoid larynx carcinoma cell line (HEp-2): E. Konac, et al.; Exp. Oncol. 27, 81 (2005) Abstract; Full Text
Further Categories Containing This Product:
Bcl-2 Family Modulators • Natural Products - Protein Kinase Inhibitors • PKC Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • PP2B [Calcineurin] / Related Products • Natural Products - Antioxidants • Polyphenols Other Products • Natural Products - Antiviral / anti-HIV Agents • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-118 Revised 22-Sep-08
Deguelin
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SYNONYMS [-]-Deguelin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-118-M005   5 mg 60.00 USD Add To Cart
ALX-350-118-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C23H22O6
MW: 394.4
CAS NUMBER: 522-17-8
MERCK INDEX: 14: 2863
RTECS: DX1500000
PURITY: ≥95%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in acetone, acetonitrile or DMSO. Slightly soluble in 100% ethanol. Insoluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of Akt (protein kinase B; PKB) in an in vitro lung carcinogenesis progression model. Inhibits cell proliferation - cells accumulate in the G2-M phase of the cell cycle. Induces apoptosis. Exhibits a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. Inhibits cyclooxygenase-2 (COX-2) expression.
Product Specific Literature References
Deguelin inhibits the growth of colon cancer cells through the induction of apoptosis and cell cycle arrest: G. Murillo, et al.; Eur. J. Cancer 38, 2446 (2002) Abstract
Effects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells: K.H. Chun, et al.; J. Natl. Cancer Inst. 95, 291 (2003) Abstract; Full Text
Cancer Chemopreventive Activity of Rotenoids from Derris trifoliata: C. Ito, et al.; Planta Med. 70, 8 (2004) Abstract
Apoptosis induction by the natural product cancer chemopreventive agent deguelin is mediated through the inhibition of mitochondrial bioenergetics.: N. Hail, et al.; Apoptosis 9, 437 (2004) Abstract
Deguelin-induced inhibition of cyclooxygenase-2 expression in human bronchial epithelial cells: H.Y. Lee, et al.; Clin. Cancer Res. 10, 1074 (2004) Abstract
Further Categories Containing This Product:
Natural Products - Apoptosis Inducers & Inhibitors • Phosphoinositide 3-kinase [PI(3)K] / Related Products • COX Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Anti-proliferative) • Natural Products - Antitumor Reagents • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-120 Revised 01-Apr-08
Helenalin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-350-120-MC05   0.5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C15H18O4
MW: 262.3
CAS NUMBER: 6754-13-8
SOURCE/HOST: Isolated from Arnica chamissonis.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (10mg/ml) or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Potent anti-inflammatory and antineoplastic agent. Induces a CD95 death receptor-independent apoptosis even when the mitochondria protecting proteins Bcl-XLor Bcl-2 are overexpressed. Also an inhibitor of NF-κB.
Product Specific Literature References
Helenalin, an anti-inflammatory sesquiterpene lactone from Arnica, selectively inhibits transcription factor NF-kappaB: G. Lyss, et al.; J. Biol. Chem. 378, 951 (1997) Abstract
The anti-inflammatory sesquiterpene lactone helenalin inhibits the transcription factor NF-kappaB by directly targeting p65: G. Lyss, et al; J. Biol. Chem. 273, 33508 (1998) Abstract
Constituents of Helenium species.XIII. The structure of Helenalin and Mexicanin A: W. Herz, et al.; JACS 85, 19 (1963)
Further Categories Containing This Product:
Bcl-2 Family Modulators • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - NF-kB Pathway Inhibitors • NF-kB Pathway Inhibitors • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-129 Revised 04-Dec-07
Aristoforin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Apoptosis Inducers & Inhibitors
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ALX-350-129-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C37H54O6
MW: 594.8
CAS NUMBER: 849215-53-8
PURITY: ≥95%
APPEARANCE: White to yellow oil.
SOLUBILITY: Soluble in DMSO or 100mM sodium hydrogen carbonate/2% DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Stable and water-soluble derivative of hyperforin (Prod. No. ALX-350-097) inducing apoptosis. Antitumor agent. Inhibits sirtuins.
Product Specific Literature References
Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent: M. Gartner, et al.; Chembiochem. 6, 171 (2005) Abstract
Phloroglucinol Derivatives Guttiferone G, Aristoforin, and Hyperforin: Inhibitors of Human Sirtuins SIRT1 and SIRT2: C. Gey, et al.; Angew. Chem. Int. Ed. Engl. 46, 5219 (2007) Abstract
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Further Categories Containing This Product:
Sirtuins / Related Products • Natural Products - Antitumor Reagents • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-153 Revised 28-Jul-08
Withaferin A
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SYNONYMS 5,6-Epoxy-4,27-dihydroxy-1-oxowitha-2,24-dienolide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-153-M001   1 mg 60.00 USD Add To Cart
ALX-350-153-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C28H38O6
MW: 470.6
CAS NUMBER: 5119-48-2
MERCK INDEX: 14: 10048
RTECS: KE7288500
SOURCE/HOST: Isolated from Withania somnifera.
PURITY: ≥94% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (20 mg/ml), methanol (10 mg/ml) or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: MAY BE MUTAGENIC. MAY BE CARCINOGENIC. HARMFUL.

Product Description
Cell permeable and potent angiogenesis inhibitor from the family of withanolides. Inhibits endothelial cells (HUVEC) sprouting in vitro (IC50=12nM) and in vivo. Exhibits antitumor, anti-inflammatory, radiosensitizing, and immunosuppressive properties. Potently inhibits NF-κB activation by preventing the TNF-induced activation of IκB kinase β (IKKβ). Affects AP1 transcription and induces cell death. Alters cytoskeletal architecture by covalently binding annexin II and stimulating its basal F-actin cross-linking activity which inhibits the migratory and invasive capability of endothelial cells. Displays neuronal regenerative properties. Targets the intermediate filament protein vimentin.
Product Specific Literature References
Tumor inhibitors. XXXIX. Active principles of Acnistus arborescens. Isolation and structural and spectral studies of withaferin A and withacnistin: S.M. Kupchan, et al.; J. Org. Chem. 34, 3858 (1969) Abstract
In vivo growth inhibitory and radiosensitizing effects of withaferin A on mouse Ehrlich ascites carcinoma: P.U. Devi, et al.; Cancer Lett. 95, 189 (1995) Abstract
Growth inhibition of human tumor cell lines by withanolides from Withania somnifera leaves: B. Jayaprakasam, et al.; Life Sci. 74, 125 (2003) Abstract
Withaferin A is a potent inhibitor of angiogenesis: R. Mohan, et al.; Angiogenesis 7, 115 (2004) Abstract
Neuritic regeneration and synaptic reconstruction induced by withanolide: A: T. Kuboyama, et al.; Br. J. Pharmacol. 144, 961 (2005) Abstract; Full Text
Actin microfilament aggregation induced by withaferin A is mediated by annexin II: R.R. Falsey, et al.; Nat. Chem. Biol. 2, 33 (2006) Abstract
Withaferin a strongly elicits IkappaB kinase beta hyperphosphorylation concomitant with potent inhibition of its kinase activity: M. Kaileh, et al.; J. Biol. Chem. 282, 4253 (2007) Abstract; Full Text
The tumor inhibitor and antiangiogenic agent withaferin A targets the intermediate filament protein vimentin: P. Bargagna-Mohan, et al.; Chem. Biol. 14, 623 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Immunomodulators • Natural Products for Angiogenesis Research • Natural Products - NF-kB Pathway Inhibitors • Natural Products for Cytoskeletal Research • Vimentin / Related Products • Natural Products - Anti-inflammatory Agents • NF-kB Pathway Inhibitors • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-257 Revised 08-Oct-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: TOXIC. MAY BE CARCINOGENIC.

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
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Further Categories Containing This Product:
Cell Cycle Blockers & Inhibitors / Related Products • Alkaloids • Natural Products for Cytoskeletal Research • Microtubule Modulators • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-259 Revised 17-Dec-07
Triptolide
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SYNONYMS PG490
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Immunomodulators
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ALX-350-259-M001   1 mg 70.00 USD Add To Cart
ALX-350-259-M005   5 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C20H24O6
MW: 360.4
CAS NUMBER: 38748-32-2
SOURCE/HOST: Isolated from Tripterygium wilfordii.
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Immunosuppressive agent with anti-inflammatory and antitumor properties. More effective in preventing T cell proliferation and interferon-γ production than FK506 (Prod. No. ALX-380-008). Induces apoptosis in T cells by activating DEVD cleaving caspases. Blocks TNF-α mediated induction of c-IAP1 and c-IAP2 and NF-κB activation.
Product Specific Literature References
Triptolide induces apoptotic death of T lymphocyte: Y. Yang, et al.; Immunopharmacology 40, 139 (1998) Abstract
Triptolide is more effective in preventing T cell proliferation and interferon-gamma production than is FK506: M.A. Chan, et al.; Phytother. Res. 13, 464 (1999) Abstract
Immunosuppressant PG490 (triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T- cells and NF-kappaB transcriptional activation: D. Qiu, et al.; J. Biol. Chem. 274, 13443 (1999) Abstract; Full Text
PG490 (triptolide) cooperates with tumor necrosis factor-alpha to induce apoptosis in tumor cells: K.Y. Lee, et al.; J. Biol. Chem. 274, 13451 (1999) Abstract; Full Text
Immunosuppressive and anti-inflammatory mechanisms of triptolide, the principal active diterpenoid from the Chinese medicinal herb Tripterygium wilfordii Hook. f:: D. Qiu & P.N. Kao; Drugs R. D. 4, 1 (2003), (Review) Abstract
Triptolide, a diterpenoid triepoxide, induces antitumor proliferation via activation of c-Jun NH2-terminal kinase 1 by decreasing phosphatidylinositol 3-kinase activity in human tumor cells: Y. Miyata, et al.; BBRC 336, 1081 (2005) Abstract
Triptolide, an inhibitor of the human heat shock response that enhances stress-induced cell death: S.D. Westerheide, et al.; J. Biol. Chem. 281, 9616 (2006) Abstract
Triptolide induces caspase-dependent cell death mediated via the mitochondrial pathway in leukemic cells: B.Z. Carter, et al.; Blood 108, 630 (2006) Abstract
Further Categories Containing This Product:
Natural Products - Anti-inflammatory Agents • Natural Products - NF-kB Pathway Inhibitors • NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-277 Revised 03-Apr-08
Betulinic acid (high purity)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-277-M005   5 mg 32.00 USD Add To Cart
ALX-350-277-M025   25 mg 95.00 USD Add To Cart
ALX-350-277-M100   100 mg 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane) tree bark.
PURITY: ≥99%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: IRRITANT.

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995)