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DNA Regulation / Transcription
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ALX-430-155 Revised 16-Nov-07
4EGI-1
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SYNONYMS α-[2-[4-(3,4-Dichlorophenyl)-2-thiazolyl]hydrazinylidene]-2-nitro-benzenepropanoic acid
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Translation Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-155-M002   2 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C18H12Cl2N4O4S
MW: 451.3
CAS NUMBER: 315706-13-9
PURITY: ≥95%
APPEARANCE: Brown solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Selective and cell permeable inhibitor of the interaction between the human eukaryotic translation initiation factors 4E (eIF4E) and 4G (eIF4G).
Product Specific Literature References
Small-molecule inhibition of the interaction between the translation initiation factors eIF4E and eIF4G: N.J. Moerke, et al.; Cell 128, 257 (2007) Abstract
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-270-444 Revised 07-Apr-08
ABT-888
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SYNONYMS 2-[(2R)-2-Methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide . dihydrochloride
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PARP Inhibitors
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ALX-270-444-M001   1 mg 50.00 USD Add To Cart
ALX-270-444-M005   5 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C13H16N4O . 2HCl
MW: 244.3 . 73.0
CAS NUMBER: 912445-05-7
PURITY: ≥98% (HPLC)
APPEARANCE: Colorless to white crystalline solid.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by 1H-NMR.

Product Description

Potent inhibitor of PARP-1 and PARP-2 (potency ≤5nM in vitro). Does not inhibit other NAD-binding enzymes. Has minimal CYP450 inhibition and induction. Shows broad spectrum of chemo- and radiopotentiation. Enantiomeric purity ≥97% suitable for in vivo studies. Does not show inherent cytotoxicity and shows no single agent activity in tumor models. Has excellent bioavailability and good blood-brain permeation. Increases tumor growth delay resulting from radiation and DNA-damaging agents.
Product Specific Literature References
Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models: J.M. Albert, et al.; Clin. Cancer Res. 13, 3033 (2007) Abstract
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models: C.K. Donawho, et al.; Clin. Cancer Res. 13, 2728 (2007) Abstract
 
 
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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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
Ordering Information
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
Related Products
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.
SOLUBILITY: Soluble in methanol, acetone or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Keep cool and dry.
HAZARD: TOXIC.
IDENTITY: Detemined 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
Identification of actinomycins by high performance liquid chromatography and fast atom bombardment mass spectrometry: S. Cho, et al.; Arch. Pharm. Res. 17, 424 (1994) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Transcription Inhibitors / Related Products
 
 
ALX-380-084 Revised 30-Oct-07
Actinomycin X0δ
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY