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Signal Transduction
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ALX-380-091 Revised 03-Apr-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. Epub ahead of print, (2008) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Tyrosine Kinase Inhibitors • Antibiotics - Other Signal Transduction Pathway Modulators • HSP90/HtpG/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
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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 • Casein Kinase Inhibitors • PKG 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-450-002 Revised 14-Nov-07
A23187 (Mixed Calcium-Magnesium Salt)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-450-002-M005   5 mg 60.00 USD Add To Cart
ALX-450-002-M010   10 mg 110.00 USD Add To Cart
ALX-450-002-M050   50 mg 415.00 USD Add To Cart
Product Specification
MERCK INDEX: 13: 1639
SOURCE/HOST: Semisynthetic.
PURITY: ≥98% (molar ratio Ca:Mg ~1:1)
APPEARANCE: White solid.
SOLUBILITY: Soluble in methylene chloride, chloroform, acetone, ethyl acetate, or diethyl ketone; also soluble in DMSO, 100% ethanol, and ethanol. Solubilize in DMSO or ethanol prior to preparing aqueous solutions of very low concentrations.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. In aqueous systems, product may aggregate over time.
HAZARD: TOXIC.

Product Description
Salt form of A23187 (Prod. No. ALX-450-001). Used in cell activation experiments when calcium dose-response data are not required.
 
 
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:
Immunomodulators Other Products • COX Inhibitors • NF-kB Pathway Inhibitors
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
Alkaloids • Antitumor Agents (Anti-proliferative) • Adrenergics & Adrenergic Receptors/Related Products • Natural Products - Antitumor Reagents
 
 
ALX-550-221 Revised 17-Jan-05
ABHxD-I . hydrochloride
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SYNONYMS (1S,2S,4S,5S)-2-Aminobicyclo[2.1.1]hexene-2,5-dicarboxylic acid . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic)/Related Products
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ALX-550-221-MC05   0.5 mg 60.00 USD Add To Cart
ALX-550-221-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C8H11NO4 . HCl
MW: 185.2 . 36.5
PURITY: ≥96%
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Conformationally restricted ACPD analog. Potent mGluR ligand with similar selectivity and potency to glutamate but without ionotropic activity. Neuroprotective.
Product Specific Literature References
Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-I, a potent mGluR agonist: A.P. Kozikowski, et al.; J. Med. Chem. 41, 1641 (1998) Abstract
 
 
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 20-Sep-05
Ac-AAVALLPAVLLALLAPYVAD-CHO
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SYNONYMS Caspase-1 Inhibitor (Aldehyde)
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Inhibitors
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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: ≥99% (HPLC)
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO (0.25mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions should be divided into aliquots and stored at -20°C. Solution is stable for at least