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ALX-380-091 Revised 21-Aug-08
17-AAG
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SYNONYMS 17-(Allylamino)-17-desmethoxygeldanamycin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-091-C100   100 µg 65.00 USD Add To Cart
ALX-380-091-M001   1 mg 162.00 USD Add To Cart
Product Specification
FORMULA: C31H43N3O8
MW: 585.7
CAS NUMBER: 75747-14-7
SOURCE/HOST: Semisynthetic derivative from geldanamycin.
PURITY: ≥97%
APPEARANCE: Red to dark red powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent, less toxic derivative of geldanamycin (Prod. No. ALX-380-054). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.
Product Specific Literature References
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives: R.C. Schnur, et al.; J. Med. Chem. 38, 3806 (1995) Abstract
The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin: T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol. 42, 273 (1998) Abstract
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone: P.A. Clarke, et al.; Oncogene 19, 4125 (2000) Abstract
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts: R. Nimmanapalli, et al.; Cancer Res. 61, 1799 (2001) Abstract; Full Text
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells: P.N. Munster, et al.; Cancer Res. 61, 2945 (2001) Abstract; Full Text
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin: J. Yang, et al.; Cancer Res. 61, 4010 (2001) Abstract; Full Text
Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis: D.M. Nguyen, et al.; Ann. Thorac. Surg. 72, 371 (2001) Abstract
ErbB2 degradation mediated by the co-chaperone protein CHIP: P. Zhou, et al.; J. Biol. Chem. 278, 13829 (2003) Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells: R. Villa, et al.; Carcinogenesis 24, 851 (2003) Abstract
Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction: I.A. Vasilevskaya, et al.; Cancer Res. 63, 3241 (2003) Abstract
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors: A. Kamal, et al.; Nature 425, 407 (2003) Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin: L. Neckers; Handb. Exp. Pharmacol. 259 (2006) Abstract
Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress: P. Workman, et al.; Ann. N.Y. Acad. Sci. 1113, 202 (2007) Abstract
Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51: Q. Yao, et al.; Clin. Cancer Res. 13, 1591 (2007) Abstract; Full Text
Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers: R.K. Ramanathan, et al.; Clin. Cancer Res. 13, 1769 (2007) Abstract
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells: P.N. Meyer, et al.; Leuk. Res. 32, 143 (2008) Abstract
Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model: C.R. Williams, et al.; J. Urol. 178, 1528 (2007) Abstract
Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia: A.J. Johnson, et al.; Br. J. Haematol. 139, 837 (2007) Abstract
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models: U. Banerji, et al.; Cancer Chemother. Pharmacol. 62, 769 (2008) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Tyrosine Kinase Inhibitors • Antibiotics - Other Signal Transduction Pathway Modulators • Antitumor Agents (Enzyme Inhibitors) • HSP90 / HtpG / Related Products
 
 
ALX-430-096 Revised 24-Feb-05
A77 1726
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SYNONYMS N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-430-096-M005   5 mg 45.00 USD Add To Cart
ALX-430-096-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C12H9F3N2O2
MW: 270.2
CAS NUMBER: 108605-62-5
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo.
Product Specific Literature References
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • COX Inhibitors • Immunomodulators Other Products
 
 
ALX-350-104 Revised 10-May-07
Aaptamine
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SYNONYMS 8,9-Dimethoxy-1H-benzo[de][1,6]naphtyridine
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Toxins
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ALX-350-104-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C13H12N2O2
MW: 228.3
CAS NUMBER: 85547-22-4
SOURCE/HOST: Isolated from the sponge Aaptos aaptos.
PURITY: ≥97%
APPEARANCE: Oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Competitive antagonist of α-adrenoceptors in vascular smooth muscle cells. Inhibits cancer cell growth.
Product Specific Literature References
Alpha-adrenoceptor blocking action of aaptamine, a novel marine natural product, in vascular smooth muscle: Y. Ohizumi, et al.; J. Pharm. Pharmacol. 36, 785 (1984) Abstract
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine: G.R. Pettit, et al.; J. Org. Chem. 69, 2251 (2004) Abstract
Aaptamine, a spongean alkaloid, activates p21 promoter in a p53-independent manner: S. Aoki, et al.; BBRC 342, 101 (2006) Abstract
Further Categories Containing This Product:
Adrenergics & Adrenergic Receptors / Related Products • Natural Products - Antitumor Reagents • Antitumor Agents (Anti-proliferative) • Alkaloids • Marine Natural Products
 
 
ALX-201-006 Revised 04-Sep-08
N-Acetyl-eglin C (recombinant)
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PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
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ALX-201-006-MC01   0.1 mg 95.00 USD Add To Cart
ALX-201-006-MC05   0.5 mg 380.00 USD Add To Cart
ALX-201-006-M001   1 mg 670.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Thr-Glu-Phe-Gly-Ser-Glu-Leu-Lys-Ser-Phe-Pro-Glu-Val-Val-Gly-Lys-Thr-Val-Asp-Gln-Ala-Arg-Glu-Tyr-Phe-Thr-Leu-His-Tyr-Pro-Gln-Tyr-Asn-Val-Tyr-Phe-Leu-Pro-Glu-Gly-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-Asp-Arg-Val-Arg-Val-Phe-Tyr-Asn-Pro-Gly-Thr-Asn-Val-Val-Asn-His-Val-Pro-His-Val-Gly-OH
FORMULA: C377H552N96O107
MW: 8141.1
CAS NUMBER: 96380-69-7
SOURCE/HOST: Produced in E. coli.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
Product Description
Eglin C was originally isolated from the leech Hirudo medicinalis [1]. Recombinant N-acetyl-eglin C is a 70 amino acid peptide with identical biological activity to native eglin C. An effective inhibitor of chymotrypsin and subtilisin as well as of leukocyte elastase and cathepsin G.
Product Specific Literature References
[1] Structure of the elastase-cathepsin G inhibitor of the leech Hirudo medicinalis: U. Seemüller, et al.; Hoppe-Seyler's Z. Physiol. Chem. 361, 1841 (1980) Abstract
[2] A large fragment approach to DNA synthesis: total synthesis of a gene for the protease inhibitor eglin c from the leech Hirudo medicinalis and its expression in E. coli: H. Rink, et al.; Nucl. Acids Res. 12, 6369 (1984) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link P01051: Eglin C (Hirudo medicinalis)
Further Categories Containing This Product:
Proteases Other Products • Recombinant Proteins / Fusion Proteins
 
 
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 • Natural Products - Topoisomerase Inhibitors • Lipoxygenases / Related Products • NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Antitumor Agents (Apoptosis Inducers) • 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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-380-082 Revised 30-Oct-07
Actinomycin C2
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-082-C500   500 µg 80.00 USD Add To Cart
Product Specification
FORMULA: C63H88N12O16
MW: 1269.5
MERCK INDEX: 14: 1606
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (contains traces of ethylacetate or cyclohexane)
APPEARANCE: Orange crystals.
SOLUBILITY: Soluble in methanol, acetone or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: TOXIC.
IDENTITY: Determined by 1H-NMR: Identical to standard reference.

Product Description
Antitumor antibiotic.
Product Specific Literature References
Nomenclature of the Actinomycins: S.A. Waksman, et al.; PNAS 44, 602 (1958) Abstract
Actinomycin D, C2 and VII, inhibitors of Grb2-SHC interaction produced by Streptomyces: J. Y. Nam, et al.; Bioorg. Med. Chem. Lett. 8, 2001 (1998) Abstract
Further Categories Containing This Product:
Transcription Inhibitors / Related Products
 
 
ALX-380-077 Revised 30-Oct-07
Actinomycin C3
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-077-M001   1 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C64H90N12O16
MW: 1283.5
MERCK INDEX: 14: 1606
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (solvent free)
APPEARANCE: Orange crystals.
SOLUBILITY: Soluble in methanol, acetone or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: TOXIC.
IDENTITY: Determined by 1H-NMR: Identical to standard reference.

Product Description
Antitumor antibiotic.
Product Specific Literature References
Nomenclature of the Actinomycins: S.A. Waksman, et al.; PNAS 44, 602 (1958) Abstract
Further Categories Containing This Product:
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-380-083 Revised 30-Oct-07
Actinomycin X0β
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antitumor Antibiotics
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ALX-380-083-C200   200 µg 70.00 USD Add To Cart
Product Specification
FORMULA: C62H86N12O17
MW: 1271.5
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥98% (contains traces of ethyl acetate or cyclohexane)
APPEARANCE: Orange crystals.