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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:
Immunomodulators Other Products • COX Inhibitors • NF-kB Pathway Inhibitors
 
 
ALX-270-444 Revised 07-Apr-08 New product
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
Related Products
Further Categories Containing This Product:
Natural Products - NF-kB Pathway Inhibitors • Antitumor Agents (Apoptosis Inducers) • Natural Products - Protein Kinase Inhibitors • Natural Products - Topoisomerase Inhibitors • Natural Products - Anti-inflammatory Agents • NF-kB Pathway Inhibitors • Natural Products - Apoptosis Inducers & Inhibitors • Lipoxygenases/Related Products
 
 
ALX-280-016 Revised 13-Feb-08
Acrolein
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY NF-kB Pathway Inhibitors
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ALX-280-016-L010   10 ml 110.00 USD Add To Cart
Product Specification
FORMULA: C3H4O
MW: 56.1
CAS NUMBER: 107-02-8
MERCK INDEX: 14: 128
RTECS: AS1050000
PURITY: ≥95% (GC)
APPEARANCE: Clear to yellow liquid.
PURITY DETAIL: ≥99% (as anhydrous). Stabilized with ~0.2% hydroquinone and ~3% water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Unstable. Very reactive with acids, amines, alkalis, sulfur dioxide, metal salts, oxidants, thiourea, dimethylamine, or weak acid conditions such as nitrogen or carbon oxide gases. Reactions may be very rapid and violent.
HANDLING: Keep away from heat, sources of ignition and incompatibles such as oxidizing agents.
HAZARD: FLAMMABLE VERY TOXIC.
IDENTITY: Determined by 1H-NMR.

Product Description
Highly electrophilic α,β-unsaturated aldehyde to which humans are exposed in a variety of environmental situations (particularly as a component of smoke). As a metabolite of cyclophosphamide, acrolein is a major factor in the toxicity and perhaps the therapeutic activity of this important anticancer agent. Reduces NF-κB activation through the formation of conjugates with NF-κB.
Product Specific Literature References
Acrolein causes inhibitor kappaB-independent decreases in nuclear factor kappaB activation in human lung adenocarcinoma (A549) cells: N.D. Horton, et al.; J. Biol. Chem. 274, 9200 (1999) Abstract; Full Text
General Literature References
The molecular effects of acrolein: J.P. Kehrer & S.S. Biswal; Toxicol. Sci. 57, 6 (2000) Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme 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) • Transcription Inhibitors/Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
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
Related Products
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Transcription Inhibitors/Related Products • Antibiotics - Apoptosis Inducers & Inhibitors
 
 
ALX-380-083 Revised 30-Oct-07
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