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ALX-260-005 Revised 03-Mar-05
Chymostatin
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SYNONYMS (S)-1-Carboxy-2-phenylethyl)-carbamoyl-α-[2-iminohexahydro-4(S)-pyrimidyl]-(S)-glycyl-X-phenylalaninal
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-005-M001   1 mg 22.00 USD Add To Cart
ALX-260-005-M005   5 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C21H38N4O8
MW: 605.0 (average)
CAS NUMBER: 9076-44-2
SOURCE/HOST: Microbial.
SOLUBILITY: Soluble in DMSO (20 mg/ml) or glacial acetic acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Inhibitor of serine proteinases having a chymotrypsin-like specificity like α-, β-, δ- and γ-chymotrypsin, chymases, cathepsin G, and most cysteine proteinases including papain and cathepsin A, B, H, and L. Mixture of type A (R=L-Leu), type B (R=L-Val), type C (R=L-Ile).
Product Specific Literature References
Chymostatin, a new chymotrypsin inhibitor produced by actinomycetes: H. Umezawa, et al.; J. Antibiot. 23, 425 (1970) Abstract
Further Categories Containing This Product:
Proteases Other Products
 
 
ALX-260-007 Revised 16-Feb-05
E-64
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SYNONYMS N-[N-(L-3-trans-Carboxyoxirane-2-carbonyl]-L-leucyl)-agmatine
L-trans-Epoxysuccinyl-leucylamide-(4-guanido)-butane
PRODUCT LINE Cancer
PRODUCT CATEGORY Cathepsin Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-260-007-M005   5 mg 55.00 USD Add To Cart
ALX-260-007-M025   25 mg 195.00 USD Add To Cart
Product Specification
FORMULA: C15H27N5O5
MW: 357.4
CAS NUMBER: 66701-25-5
SOURCE/HOST: Synthetic.
PURITY: ≥99%
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Irreversible inhibitor of cysteine proteinases like papain, cathepsin B and L. Acts by forming a thioether bond with the thiol of the active cysteine. Does not inhibit serine proteinases.
Product Specific Literature References
K. Hanada, et al.; Agric. Biol. Chem. 42, 529 (1978)
K. Hanada, et al.; Agric. Biol. Chem. 42, 523 (1978)
Further Categories Containing This Product:
Proteases Other Products
 
 
ALX-260-014 Revised 19-Aug-08
Calpeptin
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SYNONYMS Z-Leu-norleucinal
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-260-014-M005   5 mg 85.00 USD Add To Cart
ALX-260-014-M010   10 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H30N2O4
MW: 362.5
CAS NUMBER: 117591-20-5
PURITY: ≥94% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 5mg/ml soluble in DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stock solutions are stable for up to 2 months when stored at -20°C.
HANDLING: Packaged under inert gas. After reconstitution, prepare aliquots and store at -20°C. Protect from light and moisture.

Product Description
Membrane permeable inhibitor of calpain I and II and cathepsin L. Promotes neurite elongation in differentiating PC12 cells. Prevents Ca2+-ionophore induced degradation of actin binding protein and P235 in platelets. Inhibits myosin light chain phosphorylation in platelets stimulated by collagen, ionomycin (Prod. No. ALX-450-006) or thrombin.
Product Specific Literature References
Inhibitory effect of di- and tripeptidyl aldehydes on calpains and cathepsins: T. Sasaki, et al.; J. Enz. Inhib. 3, 195 (1990) Abstract
Cell-penetrating inhibitors of calpain: S. Mehdi; TIBS 16, 150 (1991) Abstract
Specificity of calcium-activated neutral proteinase (CANP) inhibitors for human mu CANP and mCANP: K. Saito and R.A. Nixon; Neurochem. Res. 18, 231 (1993) Abstract
Calpeptin, a calpain inhibitor, promotes neurite elongation in differentiating PC12 cells: M. Pinter, et al.; Neurosci. Lett. 170, 91 (1994) Abstract
Further Categories Containing This Product:
Cathepsin Inhibitors
 
 
ALX-270-103 Revised 28-Jan-05
NCO-700 . hemisulfate
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SYNONYMS Calpain Inhibitor
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Calpains / Related Products
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ALX-270-103-M001   1 mg 75.00 USD Add To Cart
ALX-270-103-M005   5 mg 300.00 USD Add To Cart
Product Specification
FORMULA: (C26H39N3O8)2 . H2SO4
MW: 1141.3 . 98.0
PURITY: ≥98%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in 100% ethanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: TOXIC.

Product Description
Specific thiol (cysteine) protease inhibitor. Active against calpains, cathepsin B and L and papain. Inhibits fMLP-stimulated PMN oxidant production; scavenges reactive oxygen species.
Product Specific Literature References
K. Hara & K. Takahashi; Biomed. Res. 4, 121 (1983)
Purification and characterization of cathepsin B from monkey skeletal muscle: T. Hirao, et al.; J. Biochem. 95, 871 (1984) Abstract
Ca overload and the action of calcium sensitive proteases, phospholipases and prostaglandin E2 in myocardial cell degradation: T. Toyo-oka, et al.; Basic Res. Cardiol. 80, 303 (1985) Abstract
Suppression of myocardial protein degradation by the protease inhibitor bis[ethyl(2R,3R)-3-[(S)-methyl-1-[4-(2,3,4-tri-methoxy-phenyl-methyl) piperazine-1-ylcarbonyl]butyl-carbonyl]oxiran-2-carboxylat e]sulfate under hypoxia: T. Toyo-oka, et al.; Drug Res. 36, 190 (1986) Abstract
Effect of NCO-700, an inhibitor of thiol protease, on reactive oxygen production by chemotactic peptide-stimulated rabbit peripheral granulocytes: K. Tawara, et al.; Experientia 44, 346 (1988) Abstract
A protease inhibitor, NCO-700, improves the contractile function in stunned canine myocardium: H. Ikeda, et al.; Jpn. Cir. J. 58, 713 (1994) Abstract
Further Categories Containing This Product:
Cathepsin InhibitorsProteases Other Products
 
 
ALX-270-280 Revised 07-Apr-08
clasto-Lactacystin β-lactone (synthetic)
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SYNONYMS Omuralide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Proteasome / Ubiquitin Modulators
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ALX-270-280-C200   200 µg 280.00 USD Add To Cart
ALX-270-280-M001   1 mg 1'295.00 USD Add To Cart
Product Specification
FORMULA: C10H15NO4
MW: 213.2
CAS NUMBER: 155975-72-7
SOURCE/HOST: Synthetic.
PURITY: ≥95% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: 20mg/ml soluble in DMSO or acetonitrile.
ACTIVITY: Kobs/[I]=20’000M-1s-1 versus 20S:PA28 complex.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Subject to hydrolysis in aqueous buffers. We do not recommend storing the aqueous solutions for more than one day.
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR.

Product Description
Highly specific, cell permeable, and irreversible 20S proteasome inhibitor. Inhibits ubiquitin proteasome pathway in cell culture (IC50=1µM). It has been suggested that the natural product lactacystin acts as a precursor for clasto-lactacystin β-lactone and that the latter is the sole species that interacts with the proteasome. Inhibits cathepsin A. Leads to a reduction of adipogenesis.
Product Specific Literature References
Inhibition of proteasome activities and subunit-specific amino-terminal threonine modification by lactacystin: G. Fenteany, et al.; Science 268, 726 (1995) Abstract
Mechanistic studies on the inactivation of the proteasome by lactacystin: a central role for clasto-lactacystin beta-lactone: L.R. Dick, et al.; J. Biol. Chem. 271, 7273 (1996) Abstract
Mechanistic studies on the inactivation of the proteasome by lactacystin in cultured cells: L.R. Dick, et al.; J. Biol. Chem. 272, 182 (1997) Abstract; Full Text
Lactacystin and clasto-lactacystin beta-lactone modify multiple proteasome beta-subunits and inhibit intracellular protein degradation and major histocompatibility complex class I antigen presentation: A. Craiu, et al.; J. Biol. Chem. 272, 13437 (1997) Abstract; Full Text
Lactacystin, proteasome function, and cell fate: G. Fenteany & S.L. Schreiber; J. Biol. Chem. 273, 8545 (1998) Abstract; Full Text
Total synthesis and biological activity of lactacystin, omuralide and analogs: E.J. Corey & W.D. Li; Chem. Pharm. Bull. 47, 1 (1999) Abstract
Lactacystin, a proteasome inhibitor: discovery and its application in cell biology: H. Tomoda & S. Omura; Yakugaku Zasshi 120, 935 (2000), Review Abstract
Lactacystin inhibits cathepsin A activity in melanoma cell lines: L. Kozlowski, et al.; Tumour Biol. 22, 211 (2001) Abstract
Inhibition of human preadipocyte proteasomal activity by HIV protease inhibitors or specific inhibitor lactacystin leads to a defect in adipogenesis, which involves matrix metalloproteinase-9: S. De Barros, et al.; J. Pharmacol. Exp. Ther. 320, 291 (2007) Abstract
Effect of proteasome inhibitor clasto-lactacystin-beta-lactone on the proteome of the haloarchaeon Haloferax volcanii: P.A. Kirkland, et al.; Microbiology 153, 2271 (2007) Abstract
Further Categories Containing This Product:
Cathepsin InhibitorsProteasome / Related ProductsMMP Inhibitors
 
 
ALX-620-080 Revised 23-May-06
bADA
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SYNONYMS Dibenzyl-1-[(R)-biotin-6-aminohexanoyl-aziridine]-2,3-(S,S+R,R)-dicarboxylate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Proteases Other Products
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ALX-620-080-M002   2 mg 540.00 USD Add To Cart
Product Specification
FORMULA: C34H42N4O7S
MW: 650.8
CAS NUMBER: 744207-03-02
PURITY: ≥98% (HPLC)
APPEARANCE: White to yellow solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Irreversible, cell permeable, biotin-labelled inhibitor of cysteine proteases.
Product Specific Literature References
Synthesis and antiplasmodial activity of a cysteine protease-inhibiting biotinylated aziridine-2,3-dicarboxylate: C. Gelhaus, et al.; Biol. Chem. 385, 435 (2004) Abstract
Blocking effect of a biotinylated protease inhibitor on the egress of Plasmodium falciparum merozoites from infected red blood cells: C. Gelhaus, et al.; Biol. Chem. 386, 499 (2005) Abstract
Further Categories Containing This Product:
Cathepsin Inhibitors
 
 
ALX-350-124 Revised 05-Apr-08
Ferulenol
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products with Antibiotic Activity
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ALX-350-124-M001   1 mg 45.00 USD Add To Cart
ALX-350-124-M005   5 mg 135.00 USD Add To Cart
ALX-350-124-M010   10 mg 230.00 USD Add To Cart
Product Specification
FORMULA: C24H30O3
MW: 366.5
CAS NUMBER: 6805-34-1
SOURCE/HOST: Isolated from Ferula communis.
PURITY: ≥96%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol and methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Prenylated 4-hydroxycoumarin. Antitubercular antibiotic with potent activity against Mycobacteria. Exerts taxol-like and dose-dependent cytotoxicity against various human tumor cell lines. Stimulator of tubulin polymerisation in vitro and inhibitor of colchicine binding to tubulin. Antithrombotic, depressing the activity of all vitamin K-dependent coagulation factors. Shows lower acute toxicity and higher activity than warfarin. Shows hepatocyte toxicity.
Product Specific Literature References
Experimental studies on the toxicity of some compounds isolated from Ferula communis in the rat: S. Tagliapietra, et al.; Res. Commun. Chem. Pathol. Pharmacol. 66, 333 (1989) Abstract
Plasma ferulenol concentration and activity of clotting factors in sheep with Ferula communis variety brevifolia intoxication: N. Tligui, et al.; Am. J. Vet. Res. 55, 1564 (1994) Abstract
Antibacterial constituents from the rhizomes of Ferula communis: M.A. Al-Yahya, et al.; Phytother. Res. 12, 335 (1998)
Microtubule-interacting activity and cytotoxicity of the prenylated coumarin ferulenol: C. Bocca, et al.; Planta Med. 68, 1135 (2002) Abstract
Acute toxicity of ferulenol, a 4-hydroxycoumarin isolated from Ferula communis L: O. Fraigui, et al.; Vet. Hum. Toxicol. 44, 5 (2002) Abstract
Characterization of anti-coagulant properties of prenylated coumarin ferulenol: M. Monti, et al.; Biochim. Biophys. Acta 1770, 1437 (2007) Abstract
 
 
ALX-351-001 Revised 08-Apr-08
Paclitaxel
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SYNONYMS Taxol®
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
Ordering Information
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ALX-351-001-M001   1 mg 20.00 USD Add To Cart
ALX-351-001-M005   5 mg 50.00 USD Add To Cart
ALX-351-001-M025   25 mg 150.00 USD Add To Cart
Product Specification
FORMULA: C47H51NO14
MW: 853.9
CAS NUMBER: 33069-62-4
MERCK INDEX: 14: 6982
RTECS: DA8340700
SOURCE/HOST: Isolated from Taxus brevifolia.
PURITY: ≥98%
APPEARANCE: Off-white crystalline powder.
SOLUBILITY: Soluble in acetonitrile, DMSO or methanol; sparingly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep cool and dry.
HAZARD: MAY BE MUTAGENIC. HARMFUL. MAY BE TERATOGENIC.
IDENTITY: Determined by IR.

Product Description

Antitumor agent. Binds to tubulin. Promotes assembly and inhibits disassembly of microtubules. Blocks the cell cycle at the mitotic phase and induces apoptosis. The checkpoint of mitotic spindle assembly, aberrant activation of cyclin-dependent kinases (CDKs) and the c-Jun N-terminal kinase/stress-activated protein kinase (JNK/SAPK) are involved in paclitaxel-induced apoptosis.

Product Specific Literature References
CDK4 down-regulation induced by paclitaxel is associated with G1 arrest in gastric cancer cells: Y.D. Yoo, et al.; Clin Cancer Res 4, 3063 (1998) Abstract
Molecular effects of paclitaxel: myths and reality (a critical review): M.V. Blagosklonny & T. Fojo; Int. J. Cancer 83, 151 (1999) Abstract
Paclitaxel-induced cell death: where the cell cycle and apoptosis come together: T.H. Wang, et al.; Cancer 88, 2619 (2000) Abstract
Disruption of Cell Adhesion and Caspase-Mediated Proteolysis of beta- and gamma-Catenins and APC Protein in Paclitaxel-Induced Apoptosis:: Y.H. Ling, et al.; Mol. Pharmaco. 59, 593 (2001) Abstract; Full Text
Taxol: biosynthesis, molecular genetics, and biotechnological applications: S. Jennewein and R. Croteau; Appl. Microbiol. Biotechnol. 57, 13 (2001) Abstract
Chemistry and chemical biology of taxane anticancer agents: M.L. Miller and I. Ojima; Chem. Rec. 1, 195 (2001) Abstract
Paclitaxel and its formulations: A.K. Singla, et al.; Int. J. Pharm. 235, 179 (2002) Abstract
Paclitaxel in cancer therapy: T.M. Mekhail and M. Markman; Expert. Opin. Pharmacother. 3, 755 (2002) Abstract
Taxol reactions: K.S. Price and M.C. Castells; Allergy Asthma Proc. 23, 205 (2002) Abstract
The chemistry of taxol and related taxoids: D.G. Kingston, et al.; Fortschr. Chem. Org. Naturst. 84, 53 (2002) Abstract
Overcoming multidrug resistance in taxane chemotherapy: R. Geney, et al.; Clin. Chem. Lab. Med. 40, 918 (2002) Abstract
Taxanes: microtubule and centrosome targets, and cell cycle dependent mechanisms of action: M. Abal, et al.; Curr. Cancer Drug Targets 300, 193 (2003) Abstract
Paclitaxel: as adjuvant or neoadjuvant therapy in early breast cancer: D. Simpson & G.L. Plosker; Drugs 64, 1839 (2004), Review Abstract
Paclitaxel for AIDS-associated Kaposi’s sarcoma: T. Dhillon, et al.; Expert Rev. Anticancer Ther. 5, 215 (2005), Review Abstract
Microtubule Associated Protein (MAP)-Tau: a novel mediator of paclitaxel sensitivity in vitro and in vivo: P. Wagner, et al.; Cell Cycle 4, 1149 (2005), Review Abstract
 
 
ALX-351-005 Revised 07-Jan-08
Baccatin III
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antitumor Reagents
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-351-005-M005   5 mg 85.00 USD Add To Cart
ALX-351-005-M025   25 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C31H38O11
MW: 586.6
CAS NUMBER: 27548-93-2
SOURCE/HOST: Semisynthetic.
PURITY: ≥95%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or 100 % ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light and moisture. Avoid strong oxidizing agents, acids and bases.