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Signal Transduction Enzymes / Related Products
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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
Ordering Information
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-430-156 Revised 21-Apr-08
6BIO
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SYNONYMS (2’Z,3’E)-6-Bromoindirubin-3’-oxime
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY GSK-3 Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-156-M001   1 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C16H10BrN3O2
MW: 356.2
CAS NUMBER: 667463-62-9
PURITY: ≥98%
APPEARANCE: Dark red solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Inhibitor of phosphoinositide-dependent kinase 1 (PDK1). Potent, reversible and ATP-competitive inhibitor of glycogen synthase kinase-3α/β (GSK-3α/β).
Product Specific Literature References
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases: P. Polychronopoulos, et al.; J. Med. Chem. 47, 935 (2004) Abstract
7-Bromoindirubin-3’-oxime induces caspase-independent cell death: J. Ribas, et al.; Oncogene 25, 6304 (2006) Abstract
Inverse in silico screening for identification of kinase inhibitor targets: S. Zahler, et al.; Chem. Biol. 14, 1207 (2007) Abstract
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins: V. Myrianthopoulos, et al.; J. Med. Chem. 50, 4027 (2007) Abstract
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Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other Products
 
 
ALX-430-149 Revised 23-Jun-08
7BIO
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SYNONYMS (2’Z, 3’E)-7-Bromoindirubin-3’-monoxime
MLS2156
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Non-apoptotic Cell Death / Necrosis
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-149-M005   5 mg 80.00 USD Add To Cart
ALX-430-149-M025   25 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C16H10BrN3O2
MW: 356.2
PURITY: ≥95% (1H-NMR)
APPEARANCE: Dark brown solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Induces a rapid caspase-independent cell death process distinct from apoptosis. Demonstrated selective inhibition of aurora kinase B (IC50=4.6µM) and aurora kinase C (IC50=0.7µM) whereas the homologeous aurora kinase A is poorly inhibited.
Product Specific Literature References
3’-Substituted 7-halogenoindirubins, a new class of cell death inducing agents: Y. Ferandin, et al.; J. Med. Chem. 49, 4638 (2006) Abstract
7-Bromoindirubin-3’-oxime induces caspase-independent cell death: J. Ribas, et al.; Oncogene 25, 6304 (2006) Abstract
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins: V. Myrianthopoulos, et al.; J. Med. Chem. 50, 4027 (2007) Abstract
7-Bromoindirubin-3’-oxime uncovers a serine protease-mediated paradigm of necrotic cell death: J. Ribas, et al.; Biochem. Pharmacol. 76, 39 (2008) Abstract
Related Products
Further Categories Containing This Product:
Aurora / Related Products
 
 
ALX-270-039 Revised 15-Nov-06
A-3 . hydrochloride
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SYNONYMS N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKA Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-039-M010   10 mg 65.00 USD Add To Cart
ALX-270-039-M050   50 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C12H13ClN2O2S . HCl
MW: 284.8 . 36.5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.
Product Specific Literature References
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors: M. Inagaki, et al.; Mol. Pharmacol. 29, 577 (1986) Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors • PKC Inhibitors • PKG Inhibitors • Casein Kinase Inhibitors
 
 
ALX-450-001 Revised 23-Jul-08
A23187 (free acid)
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SYNONYMS Calcium Ionophore A23187
Calcimycin
Antibiotic A23187
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-450-001-M001   1 mg 28.00 USD Add To Cart
ALX-450-001-M005   5 mg 65.00 USD Add To Cart
ALX-450-001-5001   5x1 mg 80.00 USD Add To Cart
ALX-450-001-M010   10 mg 92.00 USD Add To Cart
ALX-450-001-M025   25 mg 195.00 USD Add To Cart
ALX-450-001-M050   50 mg 350.00 USD Add To Cart
Product Specification
FORMULA: C29H37N3O6
MW: 523.6
CAS NUMBER: 52665-69-7
MERCK INDEX: 14: 1639
RTECS: DM4676000
SOURCE/HOST: Isolated from Streptomyces chartreusis.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methylene chloride; slightly soluble in water. Solubilize in DMSO or ethanol prior to preparing aqueous solutions of very low concentrations.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: In aqueous systems product may aggregate over time.
HANDLING: Protect from light. In aqueous systems, the product aggregates over time.
HAZARD: IRRITANT.

Product Description
Antibiotic possessing weak in vitro antimicrobial activity against gram positive bacteria and fungi. Divalent cation ionophore commonly used to increase intracellular Ca2+ levels in intact cells.
Product Specific Literature References
A23187: a divalent cation ionophore: P. W. Reed & H. A. Lardy; J. Biol. Chem. 247, 6970 (1972) Abstract
Effects of antibiotic ionophore, A23187, on oxidative phosphorylation and calcium transport of liver mitochondria: D.T. Wong, et al.; Arch. Biochem. Biophys. 156, 578 (1973) Abstract
Biological applications of ionophores: B.C. Pressman; Annu. Rev. Biochem. 45, 501 (1976), (Review) Abstract
Molecular mechanisms of endothelium-mediated vasodilation: R.R. Fiscus; Semin. Thromb. Hemost. 14 Suppl, 12 (1988), (Review) Abstract
Calcium ionophore A23187 action on cardiac myocytes is accompanied by enhanced production of reactive oxygen species: 1740, 481 (2005): T. Przygodzki, et al.; Biochim. Biophys. Acta 1740, 481 (2005) Abstract
Further Categories Containing This Product:
Nitric Oxide Pathway Other Products • Respiratory Chain Other Products • Antibiotics - ATPase Inhibitors
 
 
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
Ordering Information
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-260-046 Revised 06-Jun-08
Ac-AAVALLPAVLLALLAPDEVD-CHO
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SYNONYMS Caspase-3 Inhibitor (Aldehyde)
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-046-M001   1 mg 70.00 USD Add To Cart
ALX-260-046-M005   5 mg 290.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Asp-Glu-Val-Asp-CHO
FORMULA: C94H158N20O27
MW: 2000.4
PEPTIDE CONTENT: 65-95%.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
FORMULATION: Lyophilized. TFA salt.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry. After dissolving, prepare aliquots and store at -20°C
Product Description
Reversible, cell permeable inhibitor of caspase-3. Also inhibits caspase-6, -7, -8 and -10.
Product Specific Literature References
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis: W. Nicholson, et al.; Nature 376, 37 (1995) Abstract
Yama/CPP32 beta, a mammalian homolog of CED-3, is a CrmA-inhibitable protease that cleaves the death substrate poly(ADP-ribose) polymerase: M. Tewari, et al.; Cell 81, 801 (1995) Abstract
Activation of CPP32-like proteases is not sufficient to trigger apoptosis: inhibition of apoptosis by agents that suppress activation of AP24, but not CPP32-like activity: S.C. Wright, et al.; J. Exp. Med. 186, 1107 (1997) Abstract
 
 
ALX-260-047 Revised 27-Aug-08
Ac-AAVALLPAVLLALLAPYVAD-CHO
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SYNONYMS Caspase-1 Inhibitor (Aldehyde)
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-047-M001   1 mg 170.00 USD Add To Cart
ALX-260-047-M005   5 mg 680.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Tyr-Val-Ala-Asp-CHO
FORMULA: C97H160N20O24
MW: 1990.5
PEPTIDE CONTENT: 78-98%
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (0.25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry. After reconstitution, prepare aliquots and store at -20°C.
Product Description
Reversible, cell permeable inhibitor of caspase-1.
 
 
ALX-260-158 Revised 16-Feb-05
Ac-AEVD-CHO
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SYNONYMS Caspase-10 Inhibitor (Aldehyde)
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY