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Antitumor Agents (Apoptosis Inducers)
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ALX-350-310 Revised 03-Apr-08
3-O-Acetyl-11-keto-β-boswellic acid
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SYNONYMS AKβBA
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-310-M005   5 mg 130.00 USD Add To Cart
Product Specification
FORMULA: C32H48O5
MW: 512.7
CAS NUMBER: 67416-61-9
SOURCE/HOST: Isolated from Boswellia serrata.
PURITY: ≥99% (HPLC, NMR)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetone, dichloromethane, diethyl ether or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light.
HAZARD: MAY BE CARCINOGENIC. HARMFUL.

Product Description
Shows antitumor and anti-inflammatory activities. Potent non-redox, noncompetitive 5-lipoxygenase and topoisomerase I and IIa inhibitor leading to apoptosis. 10-times more potent than 3-O-acetyl-β-boswellic acid (Prod. No. ALX-350-308). Exhibits in vivo efficacy in tumor growth and inhibition.
Product Specific Literature References
Acetyl-11-keto-beta-boswellic acid induces apoptosis in HL-60 and CCRF-CEM cells and inhibits topoisomerase I: R.F. Hoernlein, et al.; J. Pharmacol. Exp. Ther. 288, 613 (1999) Abstract; Full Text
Boswellic acids activate p42(MAPK) and p38 MAPK and stimulate Ca(2+) mobilization: A. Altmann, et al.; BBRC 290, 185 (2002) Abstract
Coupling of boswellic acid-induced Ca2+ mobilisation and MAPK activation to lipid metabolism and peroxide formation in human leucocytes: A. Altmann, et al.; Br. J. Pharmacol. 141, 223 (2004) Abstract; Full Text
Inhibition of IkappaB kinase activity by acetyl-boswellic acids promotes apoptosis in androgen-independent PC-3 prostate cancer cells in vitro and in vivo: T. Syrovets, et al.; J. Biol. Chem. 280, 6170 (2005) Abstract; Full Text
Boswellic acids: biological actions and molecular targets: D. Poeckel & O. Werz; Curr. Med. Chem. 13, 3359 (2006), Review Abstract
Mechanisms underlying the anti-inflammatory actions of boswellic acid derivatives in experimental colitis: C. Anthoni, et al.; Am. J. Physiol. Gastrointest. Liver Physiol. 290, G1131 (2006) Abstract
Potentiation of antinociceptive effect of NSAIDs by a specific lipooxygenase inhibitor, acetyl 11-keto-beta boswellic acid: M. Bishnoi, et al.; Indian J. Exp. Biol. 44, 128 (2006) Abstract
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Further Categories Containing This Product:
Natural Products - Protein Kinase Inhibitors • Lipoxygenases / Related Products • NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Antitumor Agents (Apoptosis Inducers) • Natural Products - Topoisomerase Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-380-024 Revised 30-Oct-07
Actinomycin C
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SYNONYMS Cactinomycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-024-M005   5 mg 40.00 USD Add To Cart
ALX-380-024-M025   25 mg 140.00 USD Add To Cart
Product Specification
CAS NUMBER: 8052-16-2
MERCK INDEX: 14: 1606
SOURCE/HOST: Isolated from Streptomyces chrysomallus.
PURITY: ≥98%
APPEARANCE: Orange solid.
FORMULATION: Mixture of actinomycin C1(= actinomycin D) (R = R’ = D-Val)  ~3%, C2(R = D-Val, R’ = D-allo-Ile) ~45%, C3(R = R’ = D-allo-Ile) ~53%.
SOLUBILITY: Soluble in methanol. Sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Antibiotic complex with antitumor activity.
Product Specific Literature References
Nomenclature of the Actinomycins: S.A. Waksman, et al.; PNAS 44, 602 (1958) Abstract
General Information
For nomenclature see S.A. Waksman, E. Katz and L.C. Vining; PNAS 44, 602 (1958).
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Antibiotics - Apoptosis Inducers & Inhibitors • Transcription Inhibitors / Related Products
 
 
ALX-380-009 Revised 26-Jun-08
Actinomycin D
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SYNONYMS Actinomycin IV
Actinomycin C1
Dactinomycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-009-M005   5 mg 50.00 USD Add To Cart
ALX-380-009-M025   25 mg 200.00 USD Add To Cart
ALX-380-009-M100   100 mg 540.00 USD Add To Cart
Product Specification
FORMULA: C62H86N12O16
MW: 1255.5
CAS NUMBER: 50-76-0
MERCK INDEX: 14: 2800
RTECS: AU1575000
SOURCE/HOST: Isolated from Streptomyces parvulus.
PURITY: ≥98%
APPEARANCE: Red shiny crystals.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Sensitive to strong acids and bases.
HANDLING: Protect from light. Hygroscopic.
HAZARD: VERY TOXIC.

Product Description
Antitumor antibiotic. DNA intercalating agent. Cytotoxic inducer of apoptosis against tumor cells. Inhibitor of RNA synthesis.

For nomenclature see S.A. Waksman, E. Katz & L.C. Vining; PNAS 44, 602 (1958)
Product Specific Literature References
Apoptosis induced by Actinomycin D, Camptothecin or Aphidicolin can occur in all phases of the cell cycle: J.M. Glynn, et al.; Biochem. Soc. Trans. 20, 84S (1992) Abstract
Influence of DNA base sequence on the binding energetics of actinomycin D: S.A. Bailey, et al.; Biochemistry 32, 5881 (1993) Abstract
Nitric oxide ameliorates actinomycin D/endotoxin-induced apoptotic liver failure in mice: M. Akahori, et al.; J. Surg. Res. 85, 286 (1999) Abstract
Tumor necrosis factor-alpha plus actinomycin D-induced apoptosis of L929 cells is prevented by nitric oxide: S. Hakoda, et al.; Surg. Today 29, 1059 (1999) Abstract
Actinomycin D induces apoptosis and inhibits growth of pancreatic cancer cells: J. Kleeff, et al.; Int. J. Cancer 86, 399 (2000) Abstract
Actinomycin D inhibiting K562 cell apoptosis elicited by salvicine but not decreasing its cytotoxicity: C. Qing, et al.; Acta Pharmacol. Sin. 24, 415 (2003) Abstract; Full Text
Actinomycin D induces histone gamma-H2AX foci and complex formation of gamma-H2AX with Ku70 and nuclear DNA helicase II: H.E. Mischo, et al.; J. Biol. Chem. 280, 9586 (2005) Abstract
Actinomycin D upregulates proapoptotic protein Puma and downregulates Bcl-2 mRNA in normal peripheral blood lymphocytes: I. Kalousek, et al.; Anticancer Drugs 18, 763 (2007) Abstract
Actinomycin D enhances TRAIL-induced caspase-dependent and -independent apoptosis in SH-SY5Y neuroblastoma cells: M.J. Wang, et al.; Neurosci. Res. 59, 40 (2007) Abstract
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Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Antibiotics - Apoptosis Inducers & Inhibitors • Transcription Inhibitors / Related Products
 
 
ALX-380-283 Revised 21-May-08
7-Amino-actinomycin D
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SYNONYMS 7-AAD
7-Aminoactinomycin C1
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-283-M001   1 mg 90.00 USD Add To Cart
ALX-380-283-M005   5 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C62H87N13O16
MW: 1270.4
CAS NUMBER: 7240-37-1
RTECS: AU1579000
SOURCE/HOST: Semisynthetic from actinomycin D (Prod. No. ALX-380-009).
PURITY: ≥96% (HPLC)
APPEARANCE: Red to dark purple powder.
SOLUBILITY: Soluble in DMSO (20mg/ml), methanol or 100% ethanol; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Hygroscopic.
HAZARD: VERY TOXIC.

Product Description
Membrane impermeable fluorescent DNA intercalator. Used as a fluorescent DNA stain. Inhibitor of DNA-primed RNA polymerase and DNA polymerase. Induces apoptosis and is used as a tool to identify apoptotic cells. Cytochemical probe. Exhibits growth-inhibitory activity against certain leukemias and sarcomas. Has antibacterial properties.
Product Specific Literature References
7-Amino-actinomycin D as a cytochemical probe. I. Spectral properties: J.E. Gill, et al.; J. Histochem. Cytochem. 23, 793 (1975) Abstract; Full Text
7-substituted actinomycin D analogs. Chemical and growth-inhibitory studies: S.K. Sengupta, et al.; J. Med. Chem. 18, 1175 (1975) Abstract
Simultaneous cell cycle analysis and two-color surface immunofluorescence using 7-amino-actinomycin D and single laser excitation: applications to study of cell activation and the cell cycle of murine Ly-1 B cells: P.S. Rabinovitch, et al.; J. Immunol. 136, 2769 (1986) Abstract
Binding specificities of actinomycin D to non-self-complementary -XGCY-tetranucleotide sequences: F.M. Chen; Biochemistry 31, 6223 (1992) Abstract
Dead cell discrimination with 7-amino-actinomycin D in combination with dual color immunofluorescence in single laser flow cytometry: I. Schmid, et al.; Cytometry 13, 204 (1992) Abstract
Improved staining method for the simultaneous flow cytofluorometric analysis of DNA content, S-phase fraction, and surface phenotype using single laser instrumentation: K. Toba, et al.; Cytometry 13, 60 (1992) Abstract
Flow cytometric immunofluorescence assay for quantification of cyclobutyldithymine dimers in separate phases of the cell cycle: R.J. Berg, et al.; Carcinogenesis 14, 103 (1993) Abstract
Simultaneous three-color analysis of the surface phenotype and DNA-RNA quantitation using 7-amino-actinomycin D and pyronin Y: K. Toba, et al.; J. Immunol. Methods 182, 193 (1995) Abstract
Hematopoietic cell protein-tyrosine phosphatase-deficient motheaten mice exhibit T cell apoptosis defect: X. Su, et al.; J. Immunol. 156, 4198 (1996) Abstract
The use of 7-amino actinomycin D in identifying apoptosis: simplicity of use and broad spectrum of application compared with other techniques: N.J. Philpott, et al.; Blood 87, 2244 (1996) Abstract; Full Text
A rapid method for measuring apoptosis and dual-color immunofluorescence by single laser flow cytometry: I. Schmid, et al.; J. Immunol. Methods 170, 145 (1996) Abstract
Strategies for phenotyping apoptotic peripheral human lymphocytes comparing ISNT, annexin-V and 7-AAD cytofluorometric staining methods: H. Lecoeur, et al.; J. Immunol. Methods 209, 111 (1997) Abstract
Cell kinetic study of normal human bone marrow hematopoiesis and acute leukemia using 7AAD/PY: K. Toba, et al.; Eur. J. Haematol. 64, 10 (2000) Abstract
Live-cell assay for detection of apoptosis by dual-laser flow cytometry using Hoechst 33342 and 7-amino-actinomycin D: I. Schmid, et al.; Nat. Protoc. 2, 187 (2007) Abstract
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Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Apoptosis & Necrosis Detection Other Products • DNA Intercalators & Crosslinkers • Antitumor Agents (Apoptosis Inducers) • Transcription Inhibitors / Related Products • Dyes / Stains / Fluorescent Probes / Fluorescent Labels
 
 
ALX-380-207 Revised 03-Apr-08
Apoptolidin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-207-MC01   0.1 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C58H96O21
MW: 1129.4
CAS NUMBER: 194874-06-1
SOURCE/HOST: Isolated from Amicolatopsis sp. MST-AS5912.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, dimethyl formamide or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Originally isolated from Nocardiopsis sp. Antibiotic. Potent and highly selective apoptosis inducer in several cancer cell lines. F0F1-ATPase inhibitor.
Product Specific Literature References
Apoptolidin, a new apoptosis inducer in transformed cells from Nocardiopsis sp: J.W. Kim, et al.; J. Antibiot. (Tokyo) 50, 6628 (1997) Abstract
Understanding and exploiting the mechanistic basis for selectivity of polyketide inhibitors of F(0)F(1)-ATPase: A.R. Salomon, et al.; PNAS 97, 14766 (2000) Abstract; Full Text
Apoptolidin, a selective cytotoxic agent, is an inhibitor of F0F1-ATPase: A.R. Salomon, et al.; Chem. Biol. 8, 71 (2001) Abstract; Full Text
Apoptolidin: induction of apoptosis by a natural product: P.T. Daniel, et al.; Angew. Chem. Int. Ed. Engl. 45, 872 (2006) Abstract
Correlation of F0F1-ATPase inhibition and antiproliferative activity of apoptolidin analogues: P.A. Wender, et al.; Org. Lett. 8, 589 (2006) Abstract
Further Categories Containing This Product:
Antitumor Antibiotics • Natural Products - ATPase Inhibitors • Antitumor Agents (Apoptosis Inducers) • Respiratory Chain Other Products
 
 
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:
Antitumor Agents (Apoptosis Inducers) • Sirtuins / Related Products • Natural Products - Antitumor Reagents
 
 
ALX-350-361 Revised 17-Mar-08
Auraptene
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SYNONYMS 7-Geranyloxycoumarin
7-[(2E)-3,7-Dimethylocta-2,6-dienoxy]chromen-2-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-361-M005   5 mg 25.00 USD Add To Cart
ALX-350-361-M025   25 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C19H22O3
MW: 298.4
CAS NUMBER: 495-02-3
SOURCE/HOST: Isolated from citrus fruit.
PURITY: ≥98% (HPLC)
SOLUBILITY: Soluble in methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by NMR.

Product Description
Anti-inflammatory and chemopreventive compound. Exerts tumor preventive effects through apoptosis. Suppresses cell proliferation and lipid peroxidation. Acts as an agonist of PPARs. Induces phase II drug-metabolizing enzymes.
Product Specific Literature References
Citrus auraptene exerts dose-dependent chemopreventive activity in rat large bowel tumorigenesis: the inhibition correlates with suppression of cell proliferation and lipid peroxidation and with induction of phase II drug-metabolizing enzymes: T. Tanaka, et al.; Cancer Res. 58, 2550 (1998) Abstract; Full Text
Immunomodulatory action of citrus auraptene on macrophage functions and cytokine production of lymphocytes in female BALB/c mice: T. Tanaka, et al.; Carcinogenesis 20, 1471 (1999) Abstract; Full Text
Cell proliferation in cancer prevention; effects of preventive agents on estrogen-related endometrial carcinogenesis model and on an in vitro model in human colorectal cells: H. Mori, et al.; Mutat. Res. 480-481, 201 (2001) Abstract
Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins: M. Curini, et al.; Bioorg. Med. Chem. Lett. 14, 2241 (2004) Abstract
Citrus auraptene targets translation of MMP-7 (matrilysin) via ERK1/2-dependent and mTOR-independent mechanism: K. Kawabata, et al.; FEBS Lett. 580, 5288 (2006) Abstract
Citrus auraptene acts as an agonist for PPARs and enhances adiponectin production and MCP-1 reduction in 3T3-L1 adipocytes: K. Kuroyanagi, et al.; BBRC 366, 219 (2008) Abstract
Further Categories Containing This Product:
PPAR Agonists • Antitumor Agents (Apoptosis Inducers) • Natural Products - Anti-inflammatory Agents • Natural Products - Apoptosis Inducers & Inhibitors
 
 
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) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-ka