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Signal Transduction
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ALX-270-348 Revised 07-Jul-08
LY-333,531 . hydrochloride
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SYNONYMS (S)-13-[(Dimethylamino)methyl-10,11,14,15-tetrahydro-4,9:16,21-dimetheno-1H-13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)dione . HCl
Ruboxistaurin . hydrochloride
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY PKC Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-348-M001   1 mg Inquire
ALX-270-348-M005   5 mg Inquire
Product Specification
FORMULA: C28H28N4O3 . HCl
MW: 468.6 . 36.5
CAS NUMBER: 169939-93-9
MERCK INDEX: 14: 8290
PURITY: ≥98% (1H-NMR)
APPEARANCE: Red solid
SOLUBILITY: Soluble in DMSO; slightly soluble in 100% ethanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Isozyme selective inhibitor of protein kinase Cβ (PKCβ). Inhibits both the PKCβI (IC50=4.7nM) and PKCβII (IC50=5.9nM) isozymes. 76- and 61-fold more selective for inhibition of PKCβI and PKCβII over PKCα.

Not offered in the US.
Product Specific Literature References
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase : M.R. Jirousek, et al.; J. Med. Chem. 39, 2664 (1996) Abstract
Effects of the protein kinase C beta inhibitor LY333531 on neural and vascular function in rats with streptozotocin-induced diabetes: M.A. Cotter, et al.; Clin Sci (Lond) 103, 311 (2002) Abstract
Protein kinase Cbeta selective inhibitor LY333531 attenuates diabetic hyperalgesia through ameliorating cGMP level of dorsal root ganglion neurons: H. Kim, et al.; Diabetes 52, 2102 (2003) Abstract; Full Text
Role of p90 ribosomal S6 kinase (p90RSK) in reactive oxygen species and protein kinase C beta (PKC-beta)-mediated cardiac troponin I phosphorylation: S. Itoh, et al.; J. Biol. Chem. 280, 24135 (2005) Abstract; Full Text
Protein kinase C beta inhibitor LY333531 attenuates intercellular adhesion molecule-1 and monocyte chemotactic protein-1 expression in the kidney in diabetic rats: Y. Wu, et al.; J. Pharmacol. Sci. 101, 335 (2006) Abstract; Full Text
Ruboxistaurin: C.A. Taulien & S.V. Joy; Drugs Today (Barc) 42, 577 (2006) Abstract
Ruboxistaurin: LY 333531: Drugs R. D. 8, 193 (2007), (Review) Abstract
Role of PKC and TGF-beta receptor in glucose-induced proliferation of smooth muscle cells: Y. Yasuda, et al; BBRC 281, 71 (2001) Abstract
General Literature References
Protein kinase C and the development of diabetic vascular complications: K.J. Way, et al.; Diabet. Med. 18, 945 (2001), Review Abstract
 
 
ALX-260-092 Revised 05-Jun-08
MG-132
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SYNONYMS Z-LLL-CHO
Z-Leu-Leu-Leu-CHO
PRODUCT LINE Ubiquitin & Proteasome
PRODUCT CATEGORY Proteasome / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-092-M001   1 mg 25.00 USD Add To Cart
ALX-260-092-M005   5 mg 60.00 USD Add To Cart
Product Specification
SEQUENCE: Z-Leu-Leu-Leu-CHO
FORMULA: C26H41N3O5
MW: 475.6
CAS NUMBER: 133407-82-6
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by MS.
Product Description
Potent, reversible and cell permeable proteasome inhibitor. Inhibits NF-κB activation.
Product Specific Literature References
Inhibitors of the proteasome block the degradation of most cell proteins and the generation of peptides presented on MHC class I molecules: K.L. Rock, et al.; Cell 78, 761 (1994) Abstract
Multiple proteolytic systems, including the proteasome, contribute to CFTR processing: T.J. Jensen, et al.; Cell 83, 129 (1995) Abstract
The proteasome pathway is required for cytokine-induced endothelial-leukocyte adhesion molecule expression: M.A. Read, et al.; Immunity 2, 493 (1995) Abstract
Selective inhibitors of the proteasome-dependent and vacuolar pathways of protein degradation in Saccharomyces cerevisiae: D.H. Lee and A.L. Goldberg; J. Biol. Chem. 271, 27280 (1996) Abstract; Full Text
The human cytomegalovirus US11 gene product dislocates MHC class I heavy chains from the endoplasmic reticulum to the cytosol: E.J. Wiertz, et al.; Cell 84, 769 (1996) Abstract
Proteasome inhibitors activate stress kinases and induce Hsp72. Diverse effects on apoptosis: A.B. Meriin, et al.; J. Biol. Chem. 273, 6373 (1998) Abstract; Full Text
Role of proteasomal degradation in the cell cycle-dependent regulation of DNA topoisomerase IIalpha expression: L. Salmena, et al.; Biochem. Pharmacol. 61, 795 (2001) Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors
 
 
ALX-340-020 Revised 01-Apr-05
Prostaglandin F2α
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SYNONYMS Dinoprost
9α,11α,15S-Trihydroxy-prosta-5Z,13E-dien-1-oic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Prostaglandins & Prostaglandin Analogs
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-340-020-M001   1 mg 36.00 USD Add To Cart
ALX-340-020-M005   5 mg 162.00 USD Add To Cart
Product Specification
FORMULA: C20H34O5
MW: 354.5
CAS NUMBER: 551-11-1
PURITY: ≥99%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide; also soluble in aqueous buffers.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at –20°C.

Product Description
Widely distributed prostaglandin occurring in many species.
 
 
ALX-270-361 Revised 28-Sep-07
Indirubin
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PRODUCT LINE Cell Cycle
PRODUCT CATEGORY CDK & Cyclin Inhibitors
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ALX-270-361-M001   1 mg 50.00 USD Add To Cart
ALX-270-361-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C16H10N2O2
MW: 262.3
CAS NUMBER: 479-41-4
SOURCE/HOST: Synthetic.
PURITY: ≥98% (1H-NMR, HPLC)
APPEARANCE: Purple powder.
SOLUBILITY: Soluble in DMSO (10mg/ml) or methanol (0.3mg/ml). Sparingly soluble in aqueous buffers (12.5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years when stored at +4°C in the dark. Stock solutions should be stored in the dark and used within 1 month.
HANDLING: Keep cool and dry. Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR, IR, ESI-MS and UV.

Product Description
Inhibitor of cyclin-dependent kinases (CDK1/cyclin B (IC50=10µM), CDK2/cyclin A (IC50=2.2µM), CDK2/cyclin E (IC50=7.5µM), CDK4/cyclin D1 (IC50=12µM), CDK5/p35 (IC50=5.5µM)) [1] and of GSK-3β (IC50=600nM) [2]. Inhibits inflammatory reaction in delayed-type hypersensitivity in mice [3]. Ligand of human aryl hydrocarbon receptor [4]. Exhibits anti-cancer activity [5] [6].
Product Specific Literature References
[1] Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases: R. Hoessel, et al.; Nature Cell Biol. 1, 60 (1999) Abstract
[2] Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors?: S. Leclerc, et al.; J. Biol. Chem. 276, 251 (2001) Abstract; Full Text
[3] Indirubin inhibits inflammatory reactions in delayed-type hypersensitivity: T. Kunikata, et al.; Eur. J. Pharmacol. 410, 93 (2000) Abstract
[4] Indirubin and indigo are potent aryl hydrocarbon receptor ligands present in human urine: J. Adachi, et al.; J. Biol. Chem. 276, 31475 (2001) Abstract; Full Text
[5] Molecular mechanisms of indirubin and its derivatives: novel anticancer molecules with their origin in traditional Chinese phytomedicine: G. Eisenbrand, et al.; J. Cancer Res. Clin. Oncol. 130, 627 (2004) Abstract
[6] Indirubin enhances tumor necrosis factor-induced apoptosis through modulation of nuclear factor-kappa B signaling pathway: G. Sethi, et al.; J. Biol. Chem. 281, 23425 (2006) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Indirubin is derived from various natural sources, such as Indigofera indica, Isatis tinctoria and I. indigotica by fermentation, oxidation and the presence of light as a by product of indigo formation. Indirubin is also present in human urine and fetal bovine serum [4]. Preclinical studies of indirubin its confirmed anti-tumor activity. Efficacy against chronic myelocytic leukemia was demonstrated in clinical trials in China [2].
Related Products
Further Categories Containing This Product:
Anti-inflammatory Agents Other Products • GSK-3 Inhibitors • Antitumor Reagents Other Products
 
 
ALX-270-360 Revised 21-May-08
Tryptanthrin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
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ALX-270-360-M001   1 mg 50.00 USD Add To Cart
ALX-270-360-M005   5 mg 200.00 USD Add To Cart
Product Specification
FORMULA: C15H8N2O2
MW: 248.2
CAS NUMBER: 13220-57-0
SOURCE/HOST: Synthetic.
PURITY: ≥98% (1H-NMR, HPLC)
APPEARANCE: Yellow needles.
SOLUBILITY: Soluble in DMSO (8mg/ml) or methanol (0.3mg/ml); sparingly soluble in water (2.5µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at +4°C in the dark. Stock solutions made in DMSO must be stored in the dark no longer than one month.
HANDLING: Protect from light and moisture.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR, IR, MS and UV.

Product Description
Potent inhibitor of prostaglandin and leukotriene synthesis in various cell lines. Selective inhibitor of cyclooxygenase 2 (COX-2). Inhibitor of inducible nitric oxide synsthase (iNOS; NOS II) expression. Inhibits the production of IFN-γ and IL-2 after stimulation of Peyer’s patch lymphocytes with staphylococcal enterotoxin B (SEB). Inhibits P-glycoprotein (Pgp) (expressed by the MDR1 gene) and reverses doxorubicin (Prod. No. ALX-380-042) resistance on breast cancer cells.
Product Specific Literature References
H. Danz, et al.; Arch. Pharm. Suppl. I 333, 11 (2000)
Identification and isolation of the cyclooxygenase-2 inhibitory principle in Isatis tinctoria: H. Danz, et al.; Planta Med. 67, 411 (2001) Abstract
Inhibitory activity of tryptanthrin on prostaglandin and leukotriene synthesis: H. Danz, et al.; Planta Med. 68, 875 (2002) Abstract
Tryptanthrin inhibits nitric oxide and prostaglandin E(2) synthesis by murine macrophages: T. Ishihara, et al.; Eur. J. Pharmacol. 407, 197 (2000) Abstract
Tryptanthrin inhibits interferon-gamma production by Peyer’s patch lymphocytes derived from mice that had been orally administered staphylococcal enterotoxin: Y. Takei, et al.; Biol. Pharm. Bull. 26, 365 (2003) Abstract
Tryptanthrin inhibits MDR1 and reverses doxorubicin resistance in breast cancer cells: S.T. Yu, et al.; BBRC 358, 79 (2007) Abstract
General Information
Tryptanthrin occurs as a natural product in various plants, including Isatis tinctoria, I. indigotica, Polygonum tinctorium, Couroupita guianensis, Wrightia tinctoria and Calanthe discolor.
Further Categories Containing This Product:
Leukotrienes Other Products • NOS Inhibitors (NOS Induction & Enzyme Activity) • MDR Inhibitors • Prostaglandins Other Products • P-glycoprotein [Pgp] / Related Products • Natural Products - Nitric Oxide Pathway Modulators • COX Inhibitors
 
 
ALX-350-109 Revised 29-Nov-07
Panepoxydone
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - NF-kB Pathway Inhibitors
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ALX-350-109-MC05   0.5 mg 390.00 USD Add To Cart
Product Specification
FORMULA: C11H14O4
MW: 210.2
SOURCE/HOST: Isolated from Lentinus crinitus.
PURITY: >95% (HPLC)
FORMULATION: Yellow oil
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: SHIPPED ON BLUE ICE
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -20°C
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Protect from light. Keep cool and dry.
HAZARD: TOXIC.

Product Description
Antibiotic. Inhibitor of NF-κB activation by preventing the phosphorylation of IκB protein and thereby interrupts the signalling pathway. Strongly inhibits the expression of several NF-κB dependent pro-inflammatory genes.
Product Specific Literature References
Inhibition of NF-kappa B activation by panepoxydone: G. Erkel, et al.; BBRC 226, 214 (1996) Abstract
Cytokine induction of NO synthase II in human DLD-1 cells: roles of the JAK-STAT, AP-1 and NF-kappaB-signaling pathways: H. Kleinert, et al.; Br. J. Pharmacol. 125, 193 (1998) Abstract
Naturally occurring and synthetic inhibitors of NF-kappaB functions: K. Umezawa, et al.; Anticancer Drug Des. 15, 239 (2000) Abstract
Inhibitors of NF-kappaB signaling: design and synthesis of a biotinylated isopanepoxydone affinity reagent: J.B. Shotwell, et al.; Bioorg. Med. Chem. Lett. 12, 3463 (2002) Abstract
Molecular design and biological activities of NF-kappaB inhibitors: K. Umezawa & C. Chaicharoenpong; Mol. Cells 14, 163 (2002) Abstract
Influence of the fungal NF-kappaB inhibitor panepoxydone on inflammatory gene expression in MonoMac6 cells: G. Erkel, et al.; Int. Immunopharmacol. 7, 612 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Anti-inflammatory Agents • Natural Products with Antibiotic Activity • NF-kB Pathway Inhibitors
 
 
ALX-260-095 Revised 04-Mar-05
α-MAPI
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Proteases Other Products
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ALX-260-095-M001   1 mg 80.00 USD Add To Cart
ALX-260-095-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C30H41N7O6
MW: 595.7
SOURCE/HOST: Synthetic.
PURITY: ≥95%
APPEARANCE: White powder.
SOLUBILITY: Soluble in methanol; soluble in water (2mg/ml) after sonification.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Microbial alkaline proteinase inhibitor (α-MAPI) binds strongly to the active site of the HIV protease.
Product Specific Literature References
Structural elucidation of alpha-MAPI, a novel microbial alkaline proteinase inhibitor, produced by Streptomyces nigrescens: T. Watanabe, et al.; THL 7, 625 (1979)
A high throughput assay for inhibitors of HIV-1 protease. Screening of microbial metabolites: E. Sarubbi, et al.; FEBS Lett. 279, 265 (1991) Abstract
First efficient synthesis of alpha-MAPI: R.J. Broadbridge, et al.; Chem. Commun. 1998, 1449
 
 
ALX-420-036 Revised 21-Jul-05
DICA
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SYNONYMS 2-(2,4-Dichlorophenoxy)-N-(2-mercaptoethyl)acetamide
PRODUCT LINE Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY Caspase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-420-036-M005   5 mg 40.00 USD Add To Cart
ALX-420-036-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C10H11Cl2NO2S
MW: 280.2
CAS NUMBER: 613665-26-2
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Do not store DMSO solutions for more than 1 day.
HANDLING: Keep under inert gas. Protect from oxygen.

Product Description
Inhibitor of caspase-3 and caspase-7 binding to an allosteric site and not to the active site.
Product Specific Literature References
Discovery of an allosteric site in the caspases: J.A. Hardy, et al.; PNAS 101, 12461 (2004) Abstract; Full Text
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-420-030 Revised 24-Sep-08
BAY 41-2272
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SYNONYMS 3-(4-Amino-5-cyclopropylpyrimidine-2-yl)-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY Guanylyl Cyclases, Guanosine Phosphate Metabolism / Related Products
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ALX-420-030-M005   5 mg 92.00 USD Add To Cart
ALX-420-030-M025   25 mg 358.00 USD Add To Cart
Product Specification
FORMULA: C20H17FN6
MW: 360.4
CAS NUMBER: