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Stress & Heat Shock Proteins
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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 • Antitumor Agents (Enzyme Inhibitors) • Antibiotics - Other Signal Transduction Pathway Modulators • HSP90 / HtpG / Related Products
 
 
ALX-151-026 Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-026-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C39H57N7O14S
MW: 880.0
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Peptide is very unstable.
Product Description
Peptide containing a phosphotyrosyl mimetic. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides: B. Ye, et al.; J. Med. Chem. 38, 4270 (1995) Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K] / Related Products • Peptides
 
 
ALX-151-027 Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-027-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C36H57N7O13SP
MW: 858.9
PURITY: ≥96%
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Phosphotyrosine containing peptide. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides: B. Ye, et al.; J. Med. Chem. 38, 4270 (1995) Abstract
Further Categories Containing This Product:
Phosphoinositide 3-kinase [PI(3)K] / Related Products • Peptides
 
 
ALX-201-275 Revised 18-Mar-08
Activator of HSP90 ATPase 1 (human) (recombinant)
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SYNONYMS AHA1 (human) (recombinant)
PRODUCT LINE Stress & Heat Shock Proteins
PRODUCT CATEGORY HSP90 / HtpG / Related Products
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ALX-201-275-C100   100 µg 320.00 USD Add To Cart
Product Specification
MW: ~36.1kDa
SOURCE/HOST: Produced in E.coli.
CONCENTRATION: 1mg/ml
PURITY: ≥95% (SDS-PAGE)
FORMULATION: Liquid. In 20mM TRIS, pH 8.0, containing 2mM EDTA.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
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General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link Q12449: Activator of HSP90 ATPase-1 (human)
Further Categories Containing This Product:
Co-Chaperones & HSP-interacting Proteins / Related Products • Recombinant Proteins / Fusion Proteins
 
 
ALX-270-385 Revised 17-Jul-07
Aloisine A
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SYNONYMS RP107
7-n-Butyl-6-(4-hydroxyphenyl)[5H]pyrrolo[2,3-b]pyrazine
PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-385-M001   1 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C16H17N3O
MW: 267.3
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Cell permeable, potent, selective, reversible and ATP-competitive inhibitor of CDK1/cyclin B (IC50=150nM), CDK2/cyclin A (IC50=120nM), CDK2/cyclin E (IC50=400nM), CDK5/p25
(IC50=200nM), CDK5/p35 (IC50=160nM) and GSK-3α (IC50=500nM). Also inhibits GSK-3β (IC50=650nM) and c-Jun N-terminal kinase (JNK) (IC50~3-10µM). Poor inhibitor of CK1, CK2, CDK4/cyclin D1, MAPKK, PKA, PKG, PKCs and c-raf (IC50≥100µM). Blocks cell cycle in both G1 and G2 phase.
Product Specific Literature References
Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects: Y. Mettey, et al.; J. Med. Chem. 46, 222 (2003) Abstract
Further Categories Containing This Product:
GSK-3 Inhibitors • JNK [SAPK1] / Related Products • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-380-051 Revised 20-Jun-08
Anisomycin
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SYNONYMS 2-(p-Methoxybenzyl)-3,4-pyrrolidinediol-3-acetate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Other Signal Transduction Pathway Modulators
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-380-051-M010   10 mg 35.00 USD Add To Cart
ALX-380-051-M050   50 mg 140.00 USD Add To Cart
ALX-380-051-M100   100 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C14H19NO4
MW: 265.3
CAS NUMBER: 22862-76-6
MERCK INDEX: 14: 670
RTECS: BZ9800000
SOURCE/HOST: Isolated from Streptomyces griseolus.
PURITY: ≥98% (HPLC)
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in DMSO (25mg/ml), 100% ethanol, methanol or ethyl acetate (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Antibiotic. Activator of p38 and MAP kinases. Synergistic with growth factors and phorbol esters to superinduce cFos and cJun, by acting as a potent signalling agonist. Induces apoptosis in the human monoblastoid cell line. Used in the eradication of bean mildew. Inhibits other pathogenic fungi in plants.
Product Specific Literature References
Anisomycin, a new anti-protozoan antibiotic: B. A. Sobin & F. W. Tanner; J. Am. Chem. Soc. 76, 4053 (1954)
DNA fragmentation and cytolysis in U937 cells treated with diphtheria toxin or other inhibitors of protein synthesis: S.K. Kochi & R.J. Collier; Exp. Cell. Res. 208, 296 (1993) Abstract
The stress-activated protein kinase subfamily of c-Jun kinases: J.M. Kyriakis, et al.; Nature 369, 156 (1994) Abstract
Role of SAPK/ERK kinase-1 in the stress-activated pathway regulating transcription factor c-Jun: I. Sanchez, et al.; Nature 372, 794 (1994) Abstract
Anisomycin and rapamycin define an area upstream of p70/85S6k containing a bifurcation to histone H3-HMG-like protein phosphorylation and c-fos-c-jun induction: E. Kardalinou, et al.; Mol. Cell. Biol. 14, 1066 (1994) Abstract
Protein synthesis inhibitor phase shifts vasopressin rhythms in long- term suprachiasmatic cultures: K. Shinohara & T. Oka; NeuroReport 5, 2201 (1994) Abstract
Anisomycin selectively desensitizes signalling components involved in stress kinase activation and fos and jun induction: C.A. Hazzalin, et al.; Mol Cell Biol 18, 1844 (1998) Abstract
Anisomycin treatment paradigm affects duration of long-term potentiation in slices of the amygdala: P. Okulski, et al.; Neuroscience 114, 1 (2002) Abstract
Downregulation of Ski and SnoN co-repressors by anisomycin: A. Vazquez-Macias, et al.; FEBS Lett. 579, 3701 (2005) Abstract
Anisomycin and the reconsolidation hypothesis: J.W. Rudy, et al.; Learn. Mem. 13, 1 (2006), Review Abstract
A chemical screen identifies anisomycin as an anoikis sensitizer that functions by decreasing FLIP protein synthesis: I.A. Mawji, et al.; Cancer Res. 67, 8307 (2007) Abstract
Anisomycin abrogates repression of protooncogene c-fos transcription in E1A + cHa-ras-transformed cells through activation of MEK/ERK kinase cascade: A. N. Kukushkin, et al.; J. Cell. Biochem. 103, 1005 (2008) Abstract
Further Categories Containing This Product:
MAPK Pathway Activators • Antibiotics - Apoptosis Inducers & Inhibitors • JNK [SAPK1] / Related Products
 
 
ALX-340-063 Revised 19-Apr-07
N-Arachidonoyl-L-serine
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SYNONYMS N-[(5Z,8Z,11Z,14Z)-1-Oxo-5,8,11,14-eicosatetraenyl)]-L-serine
ARA-S
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Endocannabinoids
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ALX-340-063-M010   10 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C23H37NO4
MW: 391.5
CAS NUMBER: 187224-29-9
PURITY: ≥98%
APPEARANCE: Waxy solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; sparingly soluble in water.
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -80°C

Product Description
Endocannabinoid-like brain constituent with similar biological profile like abnormal cannabidiol. Binds weakly to CB1 and CB2 receptors and TRPV1. Produces endothelium-dependent vasodilation. Increases phosphorylation of Akt and mitogen-activated protein kinase (MAPK) in HUVEC.
Product Specific Literature References
N-arachidonoyl L-serine, an endocannabinoid-like brain constituent with vasodilatory properties: G. Milman, et al.; PNAS 103, 2428 (2006) Abstract; Full Text
Further Categories Containing This Product:
MAPK Pathway Activators • Endovanilloids • PI(3)K-Akt-mTOR Pathway Other Products
 
 
ALX-270-465 Revised 22-May-07
AS-252424
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SYNONYMS 5-[5-(4-Fluoro-2-hydroxyphenyl)-furan-2-ylmethylene)]-thiazolidine-2,4-dione
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-465-M001   1 mg 30.00 USD Add To Cart
ALX-270-465-M005   5 mg 120.00 USD Add To Cart
ALX-270-465-M025   25 mg 480.00 USD Add To Cart
Product Specification
FORMULA: C14H8FNO4S
MW: 305.3
CAS NUMBER: 900515-16-4
PURITY: ≥98% (1H-NMR)
APPEARANCE: Yellow to brown crystalline solid.
SOLUBILITY: Soluble in 100% ethanol (10mg/ml), DMSO (20mg/ml) or dimethyl formamide; also soluble in a 1:1 solution of DMSO:PBS, pH 7.4, (0.5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 2 years after receip when stored at -20°C.

Product Description
Potent and selective phosphoinositide 3-kinase (PI(3)K) p110γ inhibitor shown to be selective for class IB PI(3)K-mediated cellular effects.
Product Specific Literature References
Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils: A.M. Condliffe, et al.; Blood 106, 1432 (2005) Abstract; Full Text
Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma: V. Pomel, et al.; J. Med. Chem. 49, 3857 (2006) Abstract; Full Text
 
 
ALX-270-443 Revised 05-May-08
AS601245
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SYNONYMS 1,3-Benzothiazol-2-yl-(2-{[2-(3-pyridinyl)ethyl]amino}-4-pyrimidinyl) acetonitrile
JNK Inhibitor V
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY JNK [SAPK1] / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-443-M001   1 mg 50.00 USD Add To Cart
ALX-270-443-M005   5 mg 150.00 USD Add To Cart
ALX-270-443-M025   25 mg 520.00 USD Add To Cart
Product Specification
FORMULA: C20H16N6S
MW: 372.5
CAS NUMBER: 345987-15-7
PURITY: ≥95% (HPLC)
APPEARANCE: White to yellow solid.
PURITY DETAIL: Sum of two isomers.
SOLUBILITY: Soluble in DMSO (10mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Hygroscopic. Packaged under inert gas. Protect from light.
HAZARD: HARMFUL.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Potent and cell permeable ATP competitive JNK inhibitor (hJNK1: IC50=150nM, hJNK2: IC50=220nM and hJNK3: IC50=70 nM). Displays anti-inflammatory properties and has been shown to reduce TNF-α plasma levels induced by LPS in mice.
Product Specific Literature References
AS601245 (1,3-benzothiazol-2-yl (2-[[2-(3-pyridinyl) ethyl] amino]-4 pyrimidinyl) acetonitrile): a c-Jun NH2-terminal protein kinase inhibitor with neuroprotective properties: S. Carboni, et al.; J. Pharmacol. Exp. Ther. 310, 25 (2004) Abstract; Full Text
Design and synthesis of the first generation of novel potent, selective, and in vivo active (benzothiazol-2-yl)acetonitrile inhibitors of the c-Jun N-terminal kinase: P. Gaillard, et al.; J. Med. Chem. 48, 4596 (2005) Abstract
Further Categories Containing This Product:
TNF-alpha & TNF Receptors Other Products • Anti-inflammatory Agents Other Products
 
 
ALX-270-461 Revised 25-May-07
AS-604850
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