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Ubiquitin & Proteasome
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ALX-350-298 Revised 03-Apr-08
Betulinic acid (~95%)
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SYNONYMS 3β-Hydroxy-20(29)-lupaene-28-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
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ALX-350-298-M100   100 mg 55.00 USD Add To Cart
ALX-350-298-M500   500 mg 180.00 USD Add To Cart
ALX-350-298-G001   1 g 290.00 USD Add To Cart
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Product Specification
FORMULA: C30H48O3
MW: 456.7
CAS NUMBER: 472-15-1
SOURCE/HOST: Isolated from Platanus acerifolia (plane tree) bark.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Antitumor and anti-HIV agent. Induces apoptosis by activating mitochondrial permeability transition (MPT). Inhibits NF-κB activation and NF-κB-regulated gene expression induced by carcinogens and inflammatory stimuli. Decreases expression of Bcl-2 and cyclin D1. Potent proteasome activator.
Product Specific Literature References
Anti-AIDS agents, 11. Betulinic acid and platanic acid as anti-HIV principles from Syzigium claviflorum, and the anti-HIV activity of structurally related triterpenoids: T. Fujioka, et al.; J. Nat. Prod. 57, 243 (1994) Abstract
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis: E. Pisha, et al.; Nat. Med. 1, 1046 (1995) Abstract
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents: Y. Kashiwada, et al.; J. Med. Chem. 39, 1016 (1996) Abstract
Betulinic acid triggers CD95 (APO-1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors: S. Fulda, et al.; Cancer Res. 57, 4956 (1997) Abstract
Anti-AIDS agents--XXVII. Synthesis and anti-HIV activity of betulinic acid and dihydrobetulinic acid derivatives: F. Hashimoto, et al.; Bioorg. Med. Chem. 5, 2133 (1997) Abstract
Betulinic acid induces apoptosis in human neuroblastoma cell lines: M.L. Schmidt, et al.; Eur. J. Cancer 33, 2007 (1997) Abstract
Induction of p53 without increase in p21WAF1 in betulinic acid-mediated cell death is preferential for human metastatic melanoma: M. Rieber & M. Strasberg Rieber; DNA Cell Biol. 17, 399 (1998) Abstract
Activation of mitochondria and release of mitochondrial apoptogenic factors by betulinic acid: S. Fulda, et al.; J. Biol. Chem. 273, 33942 (1998) Abstract; Full Text
Betulinic acid inhibits aminopeptidase N activity: M.F. Melzig & H. Bormann; Planta Med. 64, 655 (1998) Abstract
Correspondence re: S. Fulda et al., Betulinic acid triggers CD95 (Apo1/Fas)- and p53-independent apoptosis via activation of caspases in neuroectodermal tumors. Cancer Res., 57: 4956, 1997: M. Rieber & M. Strasberg Rieber; Cancer. Res. 58, 5876 (1998) Abstract
Betulinic acid: a new cytotoxic agent against malignant brain-tumor cells: S. Fulda, et al.; Int. J. Cancer 82, 435 (1999) Abstract
Betulinic acid-induced apoptosis in glioma cells: A sequential requirement for new protein synthesis, formation of reactive oxygen species, and caspase processing: W. Wick, et al.; J Pharmacol. Exp. Ther. 289, 1306 (1999) Abstract; Full Text
Effects of betulinic acid alone and in combination with irradiation in human melanoma cells: E. Selzer, et al.; J. Invest. Dermatol. 114, 935 (2000) Abstract
Betulinic acid suppresses carcinogen-induced NF-kappa B activation through inhibition of I kappa B alpha kinase and p65 phosphorylation: abrogation of cyclooxygenase-2 and matrix metalloprotease-9: Y. Takada & B.B. Aggarwal; J. Immunol. 171, 3278 (2003) Abstract
Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection: R.H. Cichewicz & S.A. Kouzi; Med. Res. Rev. 24, 90 (2004), Review Abstract
Betulinic acid-induced apoptosis in leukemia cells: H. Ehrhardt, et al.; Leukemia 18, 1406 (2004) Abstract
Betulinic acid and its derivatives: a review on their biological properties: P. Yogeeswari & D. Sriram; Curr. Med. Chem. 12, 657 (2005), Review Abstract
Betulinic acid decreases expression of bcl-2 and cyclin D1, inhibits proliferation, migration and induces apoptosis in cancer cells: W. Rzeski, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 374, 11 (2006) Abstract
Activation and inhibition of the proteasome by betulinic acid and its derivatives: L. Huang, et al.; FEBS Lett. 581, 4955 (2007) Abstract
 
 
ALX-260-037 Revised 30-May-07
Calpain Inhibitor I
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SYNONYMS Ac-LL-Norleucinal
Ac-Leu-Leu-Nle-CHO
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-260-037-M010   10 mg 80.00 USD Add To Cart
ALX-260-037-M050   50 mg 310.00 USD Add To Cart
Product Specification
FORMULA: C20H37N3O4
MW: 383.5
CAS NUMBER: 110044-82-1
SOURCE/HOST: Synthetic.
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and moisture.
Product Description
Inhibits calpain I (Ki=190nM), calpain II (Ki=220nM), cathepsin B (Ki=150nM) and cathepsin L (Ki=0.5nM). Inhibits neutral cysteine proteases and the proteasome. Protects against neuronal damage caused by hypoxia and ischemia. Inhibits apoptosis in thymocytes and metamyelocytes. Inhibits cell cycle progression at the G1/S border and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation. Also prevents nitric oxide production by activated macrophages by interfering with the transcription of inducible nitric oxide synthase (iNOS; NOS II). Inhibits the proteolysis of IκB-α and IκB-β by the ubiquitin-proteasome complex.
Product Specific Literature References
Serine and cysteine proteinase inhibitors prevent nitric oxide production by activated macrophages by interfering with transcription of the inducible NO synthase gene: J.M. Griscavage, et al.; BBRC 215, 721 (1995) Abstract
Further Categories Containing This Product:
Proteasome / Related ProductsCathepsin InhibitorsProteases Other Products
 
 
ALX-350-332 Revised 20-Oct-08
Celastrol
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SYNONYMS Tripterine
3-Hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-350-332-M005   5 mg 65.00 USD Add To Cart
ALX-350-332-M025   25 mg 260.00 USD Add To Cart
Product Specification
FORMULA: C29H38O4
MW: 450.6
CAS NUMBER: 34157-83-0
SOURCE/HOST: Isolated from the root of Tripterygium sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Red cubic crystals.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Cell permeable triterpenoid; anti-inflammatory and immunosuppressive compound. Antioxidant. Suppresses LPS-induced cytokine release in macrophages and monocytes (IC50=40nM for IL-1β and IL-1α, 80nM for IL-6, 110nM for prostaglandin E2 and 210nM for IL-8 and TNF-α). Suppresses nitric oxide (NO) production (IC50=230nM) and LPS-induced NF-κB activation (IC50=270nM). Inhibits chymotrypsin-like activity of 20S proteasome (IC50=2.5µM). Inhibits lipid peroxidation induced by ADP and Fe2+ in rat liver mitochondria (IC50=7µM). Induces expression of a wider set of heat shock proteins. Inhibits topoisomerse II.
Product Specific Literature References
The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria: H. Sassa, et al.; BBRC 172, 890 (1990) Abstract
Structural basis of potent antiperoxidation activity of the triterpene celastrol in mitochondria: effect of negative membrane surface charge on lipid peroxidation: H. Sassa, et al.; Free Radic. Biol. Med. 17, 201 (1994) Abstract
Novel cytokine release inhibitors. Part III: Truncated analogs of tripterine: W. He, et al.; Bioorg. Med. Chem. Lett. 8, 3659 (1998) Abstract
Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer’s disease: A.C. Allison, et al.; Prog. Neuropsychopharmacol. Biol. Psychiatry 25, 1341 (2001) Abstract
Antiinflammatory constituents of Celastrus orbiculatus inhibit the NF-kappaB activation and NO production: H.Z. Jin, et al.; J. Nat. Prod. 65, 89 (2002) Abstract
Apoptosis induction in HL-60 cells and inhibition of topoisomerase II by triterpene celastrol: M. Nagase, et al.; Biosci. Biotechnol. Biochem. 67, 1883 (2003) Abstract; Full Text
Celastrol inhibits pro-inflammatory cytokine secretion in Crohn’s disease biopsies: G.F. Pinna, et al.; BBRC 322, 778 (2004) Abstract
Celastrols as inducers of the heat shock response and cytoprotection: S.D. Westerheide, et al.; J. Biol. Chem. 279, 56053 (2004) Abstract; Full Text
Celastrol protects against MPTP- and 3-nitropropionic acid-induced neurotoxicity: C. Cleren, et al.; J. Neurochem. 94, 995 (2005) Abstract
Celastrol blocks neuronal cell death and extends life in transgenic mouse model of amyotrophic lateral sclerosis: M. Kiaei, et al.; Neurodegener. Dis. 2, 246 (2005) Abstract
Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice: H. Yang, et al.; Cancer Res. 66, 4758 (2006) Abstract; Full Text
Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation: G. Sethi, et al.; Blood 109, 2727 (2007) Abstract
Induction of heat shock proteins in differentiated human and rodent neurons by celastrol: A.M. Chow & I.R. Brown; Cell Stress Chaperones 12, 237 (2007) Abstract
 
 
ALX-201-215 Revised 02-Apr-08
CHIP (human) (recombinant)
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SYNONYMS C-terminus of HSC70 Interacting Protein
PRODUCT LINE Stress & Heat Shock Proteins
PRODUCT CATEGORY Co-Chaperones & HSP-interacting Proteins / Related Products
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ALX-201-215-C025   25 µg 160.00 USD Add To Cart
Product Specification
SOURCE/HOST: Produced in E. coli.
CONCENTRATION: 1mg/ml
PURITY: ≥99%
FORMULATION: Liquid. In 50mM HEPES/KOH, pH 7.0, containing 50mM potassium chloride, 5mM DTT and 10% (v/v) glycerol.
SHIPPING: SHIPPED ON DRY ICE
LONG TERM STORAGE: -80°C
HANDLING: Avoid freeze/thaw cycles.
Product Specific Literature References
Dimerization of the human E3 ligase CHIP via a coiled-coil domain is essential for its activity: R. Nikolay, et al.; J. Biol. Chem. 279, 2673 (2004) Abstract; Full Text
 
 
ALX-350-254 Revised 10-Mar-08
Epoxomicin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-350-254-C050   50 µg 132.00 USD Add To Cart
Product Specification
FORMULA: C28H50N4O7
MW: 554.7
CAS NUMBER: 134381-21-8
MERCK INDEX: 14: 3630
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (15mg/ml); insoluble in water.
ACTIVITY: kobs/[I] = 25’000M-1s-1 versus 20S proteasome.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles. Protect from light.
IDENTITY: Identity determined by 1H-NMR.

Product Description
Cell permeable, potent and selective proteasome inhibitor originally isolated from Actinomycetes strain based on its potent in vivo antitumor activity. More potent inhibitor of the chymotrypsin-like activity of the proteasome than lactacystin. Effectively inhibits NF-κB activation in vitro and potently blocks inflammation in vivo in the mouse ear edema assay.
Product Specific Literature References
Epoxomicin, a new antitumor agent of microbial origin: M. Hanada, et al.; J. Antibiot. (Tokyo) 45, 1746 (1992) Abstract
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency: K.B. Kim, et al.; Bioorg. Med. Chem. Lett. 9, 3335 (1999) Abstract
Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity: L. Meng, et al.; PNAS 96, 10403 (1999) Abstract
Total synthesis of the potent proteasome inhibitor epoxomicin: a useful tool for understanding proteasome biology: N. Sin, et al.; Bioorg. Med. Chem. Lett. 9, 2283 (1999) Abstract
The selective proteasome inhibitors lactacystin and epoxomicin can be used to either up- or down-regulate antigen presentation at nontoxic doses: K. Schwarz, et al.; J. Immunol. 164, 6147 (2000) Abstract
Establishment and some characteristics of epoxomicin (a proteasome inhibitor) resistant variants of the human squamous cell carcinoma cell line, A431: K. Ohkawa, et al.; Int. J. Oncol. 24, 425 (2004) Abstract
 
 
ALX-201-146 Revised 12-Nov-08
HtpG (E. coli) (recombinant)
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SYNONYMS Heat Shock Protein 90 (E. coli) (recombinant)
HSP90 (E. coli) (recombinant)
PRODUCT LINE Stress & Heat Shock Proteins
PRODUCT CATEGORY HSP90 / HtpG / Related Products
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ALX-201-146-C025   25 µg 155.00 USD Add To Cart
Product Specification
SOURCE/HOST: Produced in E. coli.
CONCENTRATION: 4mg/ml
PURITY: ≥99%
FORMULATION: Liquid. In 40mM HEPES/KOH, pH 7.5, containing 20mM KCl and 5% glycerol.
APPLICATION: Western blot
SHIPPING: SHIPPED ON DRY ICE
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -80°C
HANDLING: For maximum product recovery after thawing, centrifuge the vial before opening the cap. Avoid freeze/thaw cycles.
Product Specific Literature References
Eukaryotic Mr 83,000 heat shock protein has a homologue in Escherichia coli: J.C. Bardwell & E.A. Craig; PNAS 84, 5177 (1987) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Swiss-Prot link P10413: Chaperone protein htpG (E. coli)
General Literature References
Heat-shock protein 90, a chaperone for folding and regulation: D. Picard; Cell. Mol. Life Sci. 59, 1640 (2002), (Review) Abstract
Further Categories Containing This Product:
Ubiquitin-conjugating Enzymes [E2]Recombinant Proteins / Fusion Proteins
 
 
ALX-380-116 Revised 07-Apr-08
Hypothemycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-116-C250   250 µg 140.00 USD Add To Cart
ALX-380-116-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C19H22O8
MW: 378.4
CAS NUMBER: 76958-67-3
SOURCE/HOST: Isolated from Phoma sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.
Product Specific Literature References
Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract
 
 
ALX-350-245 Revised 07-Apr-08
Lactacystin (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-350-245-MC01   0.1 mg 60.00 USD Add To Cart
ALX-350-245-MC05   0.5 mg 250.00 USD Add To Cart
ALX-350-245-M001   1 mg 445.00 USD Add To Cart
Product Specification
FORMULA: C15H24N2O7S
MW: 376.4
CAS NUMBER: 133343-34-7
SOURCE/HOST: Isolated from Streptomyces sp.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetonitrile (20mg/ml), 100% ethanol (1mg/ml), methanol, DMSO (20mg/ml), dimethyl formamide (20mg/ml) or water (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Organic stock solutions are stable for 3 months when stored at -20°C. Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING: Protect from light.

Product Description

Cell permeable and irreversible proteasome inhibitor. Specifically inhibits 26S proteasome (MCP; multicatalytic proteinase complex). Blocks proteasome activity by targeting the catalytic β-subunit. Has no effect on serine or cysteine proteases. Induces apoptosis in human monoblast U937 cells. Also inhibits NF-κB activation by inhibiting IκB degradation. Inhibits the ubiquitin proteasome pathway in cell culture (IC50=10µM). Inhibits cathepsin A. Upregulates HSP70 and HSP22, suggesting an initial neuroprotective pathway.

Product Specific Literature References
Lactacystin, a novel microbial metabolite, induces neuritogenesis of neuroblastoma cells: S. Omura, et al.; J. Antibiot. 44, 116 (1991) Abstract
A beta-lactone related to lactacystin induces neurite outgrowth in a neuroblastoma cell line and inhibits cell cycle progression in an osteosarcoma cell line: G. Fenteany, et al.; PNAS 91, 3358 (1994) Abstract
Lactacystin, a specific inhibitor of the proteasome, induces apoptosis in human monoblast U937 cells: S. Imajo-Ohmi, et al.; BBRC 217, 1070 (1995) Abstract
The neuritogenesis inducer lactacystin arrests cell cycle at both G0/G1 and G2 phases in neuro 2a cells: M. Katagiri, et al.; J. Antibiotics (Tokyo) 48, 344 (1995) Abstract
Degradation process of ligand-stimulated platelet-derived growth factor beta-receptor involves ubiquitin-proteasome proteolytic pathway: S. Mori, et al.; J. Biol. Chem. 270, 29447 (1995) Abstract; Full Text
Structure-activity relationships of lactacystin, the first non-protein neurotrophic factor: T. Nagamitsu, et al.; J. Antibiotics (Tokyo) 48, 747 (1995) Abstract
Neuronal differentiation of Neuro 2a cells by lactacystin and its partial inhibition by the protein phosphatase inhibitors calyculin A and okadaic acid: H. Tanaka, et al.; BBRC 216, 291 (1995) Abstract
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Proteasome-dependent regulation of p21WAF1/CIP1 expression: M.V. Blagosklonny, et al.; BBRC 227, 564 (1996) Abstract
Enhancement of CPP32-like activity in the TNF-treated U937 cells by the proteasome inhibitors: E. Fujita, et al.; BBRC 224, 74 (1996) Abstract
Degradation of 3-hydroxy-3-methylglutaryl-CoA reductase in endoplasmic reticulum membranes is accelerated as a result of increased susceptibility to proteolysis: T.P. McGee, et al.; J.Biol. Chem. 271, 25630 (1996) Abstract; Full Text
Lactacystin increases LDL receptor level on HepG2 cells: H. Miura, et al.; BBRC 227, 684 (1996) Abstract
Proteasome pathway operates for the degradation of ornithine decarboxylase in intact cells: Y. Murakami, et al.; Biochem. J. 317, 77 (1996) Abstract; Full Text
Lactacystin, an inhibitor of the proteasome, blocks the degradation of a mutant precursor of glycosylphosphatidylinositol-linked protein in a pre-Golgi compartment: K. Oda, et al.; BBRC 219, 800 (1996) Abstract
Degradation of a mutant secretory protein, alpha1-antitrypsin Z, in the endoplasmic reticulum requires proteasome activity: D. Qu, et al.; J. Biol. Chem. 271, 22791 (1996) Abstract; Full Text
Accelerated degradatio