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Bcl-2 Family Modulators
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ALX-380-075 Revised 03-Apr-08
Antimycin A
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SYNONYMS Antipiricullin
Virosin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-075-M005   5 mg 20.00 USD Add To Cart
ALX-380-075-M010   10 mg 33.00 USD Add To Cart
Product Specification
CAS NUMBER: 1397-94-0
MERCK INDEX: 14: 714 (A1) & 715 (A3)
RTECS: CD0350000
SOURCE/HOST: Isolated from Streptomyces sp. Mixture of antimycin A's.
APPEARANCE: White to faint yellow powder.
SOLUBILITY: Soluble in 100% ethanol (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Antibiotic. Induces apoptosis, which is not prevented by the presence of Bcl-2. Inhibits mitochondrial electron transport specifically between cytochromes b and c1.
Product Specific Literature References
The isolation and properties of antimycin A: B. R. Dunshee, et al.; J. Am. Chem. Soc. 71, 2436 (1949)
The effect of antimycin A on mouse liver inner mitochondrial membrane channel activity: M.L. Campo, et al.; J. Biol. Chem. 267, 8123 (1992) Abstract; Full Text
Antimycin A mimics a cell-death-inducing Bcl-2 homology domain 3: S.P. Tzung, et al.; Nat. Cell Biol. 3, 183 (2001) Abstract
Biophysical characterization of recombinant human Bcl-2 and its interactions with an inhibitory ligand, antimycin A: K.M. Kim, et al.; Biochemistry 40, 4911 (2001) Abstract
Synthetic peptides and non-peptidic molecules as probes of structure and function of Bcl-2 family proteins and modulators of apoptosis: D. Liu & Z. Huang; Apoptosis 6, 453 (2001) Abstract
Antimycin A mimics a cell-death-inducing Bcl-2 homology domain 3: S.P. Tzung, et al.; Nat. Cell. Biol. 3, 183 (2001) Abstract
Oligomycin and antimycin A prevent nitric oxide-induced apoptosis by blocking cytochrome C leakage: N. Dairaku, et al.; J. Lab. Clin. Med. 143, 143 (2004) Abstract
An ROS generator, antimycin A, inhibits the growth of HeLa cells via apoptosis: W.H. Park, et al.; J. Cell. Biochem. 102, 98 (2007) Abstract
Further Categories Containing This Product:
Bcl-2 Family Modulators • Respiratory Chain Other Products
 
 
ALX-350-312 Revised 28-May-08
(-)-Arctigenin
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SYNONYMS (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]dihydro-3-[(4-hydroxy-3-methoxyphenyl)methyl]-2-(3H)-furanone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-312-M025   25 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C21H24O6
MW: 372.4
CAS NUMBER: 7770-78-7
SOURCE/HOST: Isolated from Arctium lappa.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (34mg/ml, heating, sonication); sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Lignan derivative, which shows antitumor, anti-inflammatory, immunomodulatory and neuroprotective activities. Down-regulates anti-apoptotic protein Bcl-XL. Potent inhibitor of HIV type-I integrase and DNA topoisomerase II. Shows phytoestrogenic and cytotoxic properties against Hep62 cells.  Antagonist for platelet activating factor and Ca2+. Blocks the activation of Akt (protein kinase B; PKB) induced by glucose starvation.
Product Specific Literature References
Antiproliferative effect of Arctigenin and Arctiin: S.Y. Ryu, et al.; Arch. Pharm. Res. 18, 462 (1995)
(-)-Arctigenin as a lead structure for inhibitors of human immunodeficiency virus type-1 integrase: E. Eich, et al.; J. Med. Chem 39, 86 (1996) Abstract
Immunomodulatory effect of arctigenin, a lignan compound, on tumour necrosis factor-alpha and nitric oxide production, and lymphocyte proliferation: J.Y. Cho, et al.; J. Pharm. Pharmacol. 51, 1267 (1999) Abstract
Arctigenin protects cultured cortical neurons from glutamate-induced neurodegeneration by binding to kainate receptor: Y.P. Jang, et al.; J. Neurosci. Res. 68, 233 (2002) 68, 233 (2002) Abstract
A phytochemical study of lignans in whole plants and cell suspension cultures of Anthriscus sylvestris: A. Koulman, et al.; Planta Med. 69, 733 (2003) Abstract
Naturally occurring lignans efficiently induce apoptosis in colorectal tumor cells: B. Hausott, et al.; J. Cancer Res. Clin. Oncol. 129, 569 (2003) Abstract
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition: M.K. Cho, et al.; Int. Immunopharmacol. 4, 1419 (2004) Abstract
Arctigenin, a phenylpropanoid dibenzylbutyrolactone lignan, inhibits MAP kinases and AP-1 activation via potent MKK inhibition: the role in TNF-alpha inhibition: M.K. Cho, et al.; Int. Immunopharmacol. 4, 1419 (2004) Abstract
Identification of arctigenin as an antitumor agent having the ability to eliminate the tolerance of cancer cells to nutrient starvation: S. Awale, et al.; Cancer Res. 66, 1751 (2006) Abstract
The chemopreventive effects of Saussurea salicifolia through induction of apoptosis and phase II detoxification enzyme: K. Kang, et al.; Biol. Pharm. Bull. 30, 2352 (2007) Abstract
Further Categories Containing This Product:
Bcl-2 Family Modulators • Platelet Activating Factors [PAF] & Receptors / Related Products • Natural Products - Topoisomerase Inhibitors • Natural Products - Anti-inflammatory Agents • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Immunomodulators • Natural Products - Nitric Oxide Pathway Modulators • HIV / AIDS / Related Products
 
 
ALX-350-318 Revised 17-Jun-08
(-)-Arctiin
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SYNONYMS (3R,4R)-4-[(3,4-Dimethoxyphenyl)methyl]-3-[[4-(β-D-glucopyranosyloxy)-3-methoxyphenyl]methyl]dihydro-2(3H)-furanone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-318-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C27H34O11
MW: 534.6
CAS NUMBER: 20362-31-6
SOURCE/HOST: Isolated from Arctium lappa.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (5mg/ml); sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description

Lignan derivative with antitumor activities. Down-regulates anti-apoptotic protein Bcl-XL. Potent inhibitor of HIV type-I integrase and DNA topoisomerase II. Shows phytoestrogenic activity and is an antagonist for platelet activating factor and Ca2+.
Product Specific Literature References
Platelet activating factor (PAF) antagonists contained in medicinal plants: lignans and sesquiterpenes: S. Iwakami, et al.; Chem. Pharm. Bull. (Tokyo) 40, 1196 (1992) Abstract
Antiproliferative effect of Arctigenin and Arctiin: S.Y. Ryu, et al.; Arch. Pharm. Res. 18, 462 (1995)
Cytotoxic components of bardanae fructus (goboshi): S. Moritani, et al.; Biol. Pharm. Bull. 19, 1515 (1996) Abstract
Plant-derived leading compounds for chemotherapy of human immunodeficiency virus (HIV) infection: A.J. Vlietinck, et al.; Planta Med. 64, 97 (1998) Abstract
Anti-tumor-promoting activity of lignans from the aerial part of Saussurea medusa: M. Takasaki, et al.; Cancer Lett. 158, 53 (2000) Abstract
Isolation and identification of arctiin and arctigenin in leaves of burdock (Arctium lappa L.) by polyamide column chromatography in combination with HPLC-ESI/MS: S. Liu, et al.; Phytochem. Anal. 16, 86 (2005) Abstract
Application of preparative high-speed counter-current chromatography for separation and purification of arctiin from Fructus Arctii: X. Wang, et al.; J. Chromatogr. A. 1063, 247 (2005) Abstract
The chemopreventive effects of Saussurea salicifolia through induction of apoptosis and phase II detoxification enzyme: K. Kang, et al.; Biol. Pharm. Bull. 30, 2352 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Immunomodulators • Bcl-2 Family Modulators • Antitumor Agents (Anti-proliferative) • Platelet Activating Factors [PAF] & Receptors / Related Products • Natural Products - Topoisomerase Inhibitors • Natural Products - Antiviral / anti-HIV Agents • HIV / AIDS / Related Products
 
 
ALX-430-122 Revised 23-Feb-05
BH3I-1
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SYNONYMS 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Bcl-2 Family Modulators
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ALX-430-122-M005   5 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C15H14BrNO3S2
MW: 400.3
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at –20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas. Protect from light.
HAZARD: HARMFUL.

Product Description
Cell permeable BH3 mimetic. Binds to Bcl-XL.
 
 
ALX-430-123 Revised 24-Feb-05
BH3I-1"
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SYNONYMS 5-Benzylidine-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Bcl-2 Family Modulators
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ALX-430-123-M005   5 mg 125.00 USD Add To Cart
Product Specification
FORMULA: C15H15NO3S2
MW: 321.4
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for 2 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at –20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas. Protect from light.
HAZARD: HARMFUL.

Product Description
Cell permeable BH3 mimetic. Binds to Bcl-XL.
 
 
ALX-350-008 Revised 02-Oct-07
Chelerythrine chloride
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SYNONYMS 1,2-Dimethoxy-N-methyl-[1,3]benzodioxolo[5,6-c]phenanthridinium chloride
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-350-008-M001   1 mg 25.00 USD Add To Cart
ALX-350-008-M005   5 mg 75.00 USD Add To Cart
ALX-350-008-M025   25 mg 300.00 USD Add To Cart
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Product Specification
FORMULA: C21H18NO4Cl
MW: 383.8
CAS NUMBER: 3895-92-9
MERCK INDEX: 14: 2051
RTECS: FL9200000
SOURCE/HOST: Synthetic.
PURITY: ≥97% (completely free of biologically active impurities, such as sanguinarine)
APPEARANCE: Yellow to orange solid.
SOLUBILITY: Soluble in DMSO, water, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Heating to 40-50°C with gentle agitation may support complete solubilization. Further dilute with buffer just prior to use. Stock solutions should be refrigerated or frozen between for storage.
HAZARD: HARMFUL.

Product Description
Potent, selective and cell permeable protein kinase C (PKC) inhibitor. Induces apoptosis. BH3 mimetic which inhibits Bcl-XL function.
Product Specific Literature References
Antiplatelet effects of chelerythrine chloride isolated from Zanthoxylum simulans: F.-N. Ko, et al.; Biochim. Biophys. Acta 1052, 360 (1990) Abstract
Chelerythrine is a potent and specific inhibitor of protein kinase C: J.M. Herbert, et al.; BBRC 172, 993 (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
Identification of chelerythrine as an inhibitor of BclXL function: S.L. Chan, et al.; J. Biol. Chem. 278, 20453 (2003) Abstract
Chelerythrine and sanguinarine dock at distinct sites on BclXL that are not the classic BH3 binding cleft: Y.H. Zhang, et al.; J. Mol. Biol. 364, 536 (2006) Abstract
The effect of chelerythrine on cell growth, apoptosis, and cell cycle in human normal and cancer cells in comparison with sanguinarine: J. Malikova, et al.; Cell Biol. Toxicol. 22, 439 (2006) Abstract
Further Categories Containing This Product:
Bcl-2 Family Modulators • PKC Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Alkaloids
 
 
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 • PKC Inhibitors • Natural Products - Protein Kinase Inhibitors • PP2B [Calcineurin] / Related Products • Antitumor Agents (Apoptosis Inducers) • Natural Products - Antioxidants • Polyphenols Other Products • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antiviral / anti-HIV Agents
 
 
ALX-430-101 Revised 08-Aug-08
HA14-1
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SYNONYMS Ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Bcl-2 Family Modulators
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ALX-430-101-M005   5 mg 40.00 USD Add To Cart
ALX-430-101-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C17H17N2O5Br
MW: 409.2
CAS NUMBER: 65673-63-4
PURITY: ≥95% (1H-NMR)
APPEARANCE: Off-white to light yellow powder.
SOLUBILITY: Soluble in DMSO, dimethyl formamide or halogenated solvents; also soluble in 100% ethanol (hot).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Unstable in solution. Prepare fresh solution for each application.
HANDLING: Keep cool and dry.
IDENTITY: Identity determined by IR, 1H-NMR.

Product Description

Cell permeable Bcl-2 ligand.
Product Specific Literature References
Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells: J.L. Wang, et al.; PNAS 97, 7124 (2000) Abstract
Synthetic peptides and non-peptidic molecules as probes of structure and function of Bcl-2 family proteins and modulators of apoptosis: D. Liu & Z. Huang; Apoptosis 6, 453 (2001) Abstract
Synergistic induction of apoptosis by simultaneous disruption of the Bcl-2 and MEK/MAPK pathways in acute myelogenous leukemia: M. Milella, et al.; Blood 99, 3461 (2002) Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
 
 
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 • Antitumor Agents (Apoptosis Inducers) • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors
 
 
ALX-430-124 Revised 23-Feb-05
Licochalcone A (synthetic)
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SYNONYMS (E)-3-[5-(1,1-Dimethyl-2-propenyl)-4-hydroxy-2-methoxyphenyl]-1-(4-hydroxyphenyl)-2-propen-1-one
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Bcl-2 Family Modulators
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ALX-430-124-M005   5 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C21H22O4
MW: 338.4
CAS NUMBER: 58749-22-7
PURITY: ≥96% (HPLC)
APPEARANCE: Yellow crystalline solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 6 months when stored at –20°C. Dilute stock solution 1:10 with aqueous buffer or medium just prior to use.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas. Protect from light.
HAZARD: HARMFUL.

Product Description
Reduces Bcl-2 protein expression.
Further Categories Containing This Product:
Chalcones
 
 
ALX-350-076 Revised 16-Jun-08
Sanguinarine chloride
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SYNONYMS Pseudochelerythrine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - ATPase Inhibitors
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