ALEXIS Biochemicals: Matriptase (human) (recombinant)

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ALX-260-005

Revised 03-Mar-05

Chymostatin
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
ALX-260-005-M005		5 mg	75.00 USD

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

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Proteases Other Products

ALX-260-007

Revised 16-Feb-05

E-64
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
ALX-260-007-M025		25 mg	195.00 USD

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)

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Proteases Other Products

ALX-260-093

Revised 22-May-06

Antipain
SYNONYMS	[(S)-1-Carboxy-2-phenylethyl]-carbamoyl-Arg-Val-arginal . 2HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Proteases Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-260-093-M005		5 mg	35.00 USD
ALX-260-093-M025		25 mg	130.00 USD

Product Specification

SEQUENCE:	[(S)-1-Carboxy-2-phenylethyl]-carbamoyl-Arg-Val-arginal
FORMULA:	C₂₇H₄₄N₁₀O₆ . 2HCl
MW:	604.7 . 73.0
CAS NUMBER:	37682-72-7
SOURCE/HOST:	Synthetic.
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in water, methanol, 100 % ethanol or acetonitrile.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Inhibits papain and trypsin and to a small extent plasmin. Antipain is more specific for papain and trypsin than is leupeptin (Prod. No. ALX-260-009). The inhibitory potency of antipain is 100-fold higher than that of elastatinal. Acts by forming a hemiacetal adduct between its aldehyde group and the active serine of the proteinase.

Product Specific Literature References

Antipain, a new protease inhibitor isolated from actinomycetes: H. Suda, et al.; J. Antibiot. 25, 263 (1972) Abstract
Structures and activities of protease inhibitors of microbial origin: H. Umezawa; Meth. Enzymol. 45, 678 (1976) Abstract

ALX-260-095

Revised 04-Mar-05

α-MAPI
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Proteases Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-260-095-M001		1 mg	80.00 USD
ALX-260-095-M005		5 mg	240.00 USD

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-270-014

Revised 17-Jul-06

Ebelactone B
SYNONYMS	2-Ethyl-3,11-dihydroxy-4,6,8,10,12-pentamethyl-9-oxo-6-tetradecenoic 1,3-lactone
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Aminopeptidases / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-014-M001		1 mg	95.00 USD
ALX-270-014-M005		5 mg	380.00 USD

Product Specification

FORMULA:	C₂₁H₃₆O₄
MW:	352.5
CAS NUMBER:	76808-15-6
SOURCE/HOST:	Microbial.
PURITY:	≥99%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Inhibitor of esterases, lipases, N-formylmethionine aminopeptidase and carboxypeptidase Y-like kinase (CPY).

Product Specific Literature References

Ebelactone, an inhibitor of esterase, produced by actinomycetes: H. Umezawa, et al.; J. Antibiot. (Tokyo) 33, 1594 (1980) Abstract
Identification of an isoprenylated cysteine methyl ester hydrolase activity in bovine rod outer segment membranes: E.W. Tan & R.R. Rando; Biochemistry 31, 5572 (1992) Abstract
Structural studies on ebelactone A and B, esterase inhibitors produced by actinomycetes: K. Uotani, et al.; J. Antibiot. (Tokyo) 35, 1495 (1982) Abstract
Biosynthetic studies of ebelactone A and B by 13C NMR spectrometry: K. Uotani, et al.; J. Antibiot. (Tokyo) 35, 1670 (1982) Abstract
Diuretic and natriuretic effect of ebelactone B in anesthetized rats by inhibition of a urinary carboxypeptidase Y-like kininase: M. Majima, et al.; Jpn. J. Pharmacol. 65, 79 (1994) Abstract
Inhibition of kinin degradation on the luminal side of renal tubules reduces high blood pressure in deoxycorticosterone acetate salt-treated rats: S. Nakajima, et al.; Clin. Exp. Pharmacol. Physiol. 27, 80 (2000) Abstract

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Proteases Other Products

ALX-270-022

Revised 09-Jan-08

AEBSF . hydrochloride
SYNONYMS	4-(2-Aminoethyl)benzenesulfonylfluoride . HCl Pefabloc^®SC
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Proteases Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-022-M050		50 mg	40.00 USD
ALX-270-022-M250		250 mg	145.00 USD
ALX-270-022-G001		1 g	360.00 USD

Product Specification

FORMULA:	C₈H₁₀FNO₂S . HCl
MW:	203.2 . 36.5
CAS NUMBER:	30827-99-7
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in water or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from moisture.

Product Description

Specific irreversible inhibitor of serine proteases including trypsin, chymotrypsin, plasmin, plasma kallikrein, and thrombin. Stable, non-toxic alternative to PMSF (Prod. No. ALX-270-184). Inhibitor of NAD(P)H oxidase. Activator of MAP kinases JNK and p38.

Product Specific Literature References

Irreversible enzyme inhibitors. 180. Irreversible inhibitors of the C'la component of complement derived from m-(phenoxypropoxy)benzamidine and phenoxyacetamide: B.R. Baker & H.J. Cory; J. Med. Chem. 14, 119 (1971) Abstract
Serine protease inhibitors block priming of monocytes for enhanced release of superoxide: P. Megyeri, et al.; Immunology 86, 629 (1995) Abstract; Full Text
Inhibition of amyloid beta-protein production in neural cells by the serine protease inhibitor AEBSF: M. Citron, et al.; Neuron 17, 171 (1996) Abstract
Lysis of leukemic cells by human macrophages: inhibition by 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), a serine protease inhibitor: Y. Nakabo & M.J. Pabst; J. Leukoc. Biol. 60, 328 (1996) Abstract; Full Text
Inhibition of NADPH oxidase activation by 4-(2-aminoethyl)-benzenesulfonyl fluoride and related compounds: V. Diatchuk, et al.; J. Biol. Chem. 272, 13292 (1997) Abstract; Full Text
4-(2-Aminoethyl)benzenesulfonyl fluoride attenuates tumor-necrosis-factor-alpha-induced blood-brain barrier opening: P. Megyeri, et al.; Eur. J. Pharmacol. 374, 207 (1999) Abstract
Evaluation of two inhibitors of invasion: LY311727 [3-(3-acetamide-1-benzyl-2-ethyl-indolyl-5-oxy)propane phosphonic acid] and AEBSF [4-(2-aminoethyl)-benzenesulphonyl fluoride] in acute murine toxoplasmosis: R. Buitrago-Rey, et al.; J. Antimicrob. Chemother. 49, 871 (2002) Abstract; Full Text
Heme oxygenase-1 gene activation by the NAD(P)H oxidase inhibitor 4-(2-aminoethyl) benzenesulfonyl fluoride via a protein kinase B, p38-dependent signaling pathway in monocytes: N. Wijayanti, et al.; J. Biol. Chem. 280, 21820 (2005) Abstract; Full Text
Inhibitory effect of 4-(2-aminoethyl)-benzenesulfonyl fluoride, a serine protease inhibitor, on PI3K inhibitor-induced CHOP expression: T. Hosoi, et al.; Eur. J. Pharmacol. 554, 8 (2007) Abstract

Further Categories Containing This Product:

Heme Oxygenase / Related Products • Cell Stress, Oxidative Stress & Redox Signalling Other Products • MAPK Pathway Activators • Fatty Acid Amide Hydrolase [FAAH] / Related Products

ALX-270-103

Revised 28-Jan-05

NCO-700 . hemisulfate
SYNONYMS	Calpain Inhibitor
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Calpains / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-103-M001		1 mg	75.00 USD
ALX-270-103-M005		5 mg	300.00 USD

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 Inhibitors • Proteases Other Products

ALX-270-184

Revised 26-May-08

Phenylmethylsulfonyl fluoride
SYNONYMS	PMSF Benzylsulfonyl fluoride
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Proteases Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-184-G001		1 g	25.00 USD
ALX-270-184-G005		5 g	50.00 USD
ALX-270-184-G025		25 g	135.00 USD

Product Specification

FORMULA:	C₇H₇FO₂S
MW:	174.2
CAS NUMBER:	329-98-6
RTECS:	XT8040000
PURITY:	≥99% (HPLC)
APPEARANCE:	White to off-white needle crystals.
SOLUBILITY:	Soluble in 100% ethanol, methanol or isopropanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
HAZARD:	CORROSIVE. HARMFUL.

Product Description

Irreversible inhibitor of serine proteases. Widely used fatty acid amid hydrolase (FAAH) inhibitor for pretreatment of brain membrane preparations when testing CB₁ receptor activity. Spleen membranes used for CB₂ studies do not require this pretreatment, as FAAH activity is absent in these cells. Inhibits also cysteine proteases like papain (reversible by DTT treatment, Prod. No. ALX-280-001), as well as internucleosomal DNA fragmentation in immature thymocytes. For a related, more stable inhibitor see AEBSF (Prod. No. ALX-270-022).

Product Specific Literature References

Kinetic analysis of differences in brain acetylcholinesterase from fish or mammalian sources: D.E. Moss & D.E. Fahrney; Biochem. Pharmacol. 27, 2693 (1978) Abstract
Inactivation of the protease inhibitor phenylmethylsulfonyl fluoride in buffers: G.T. James; Anal. Biochem. 86, 574 (1978) Abstract
Enzymatic synthesis and degradation of anandamide, a cannabinoid receptor agonist: D.G. Deutsch & S.A. Chin; Biochem. Pharmacol. 46, 791 (1993) Abstract

Further Categories Containing This Product:

Acetylcholine Esterase / Related Products • Fatty Acid Amide Hydrolase [FAAH] / Related Products

ALX-350-044

Revised 06-Jun-08

Microcystin-YR
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Microcystins

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-044-C025		25 µg	140.00 USD
ALX-350-044-C100		100 µg	210.00 USD

Product Specification

FORMULA:	C₅₂H₇₂N₁₀O₁₃
MW:	1045.2
CAS NUMBER:	101064-48-6
SOURCE/HOST:	Isolated from Microcystis aeruginosa.
PURITY:	≥95% (HPLC)
APPEARANCE:	Whitish film adhered to inside of the vial.
SOLUBILITY:	Soluble in 100% ethanol, methanol or DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	For maximum product recovery after thawing, centrifuge the vial before opening the cap.
HAZARD:	MAY BE CARCINOGENIC. HIGHLY IRRITANT. VERY TOXIC.
IDENTITY:	Identity determined by MS.

Product Description

Analog of microcystin-LR (Prod. No. ALX-350-012) with Tyr substituted in place of Leu. As for all microcystins the conjugated double bonds in the ADDA moiety cause a characteristic absorption maximum at 238nm. The Tyr residue in position 2 of microcystin-YR confers an absorption maximum at 232nm. Potent inhibitor of eukaryotic protein phosphatases 1 and 2A. Useful as a reference compound in environmental analysis. The hydroxyl group of the Tyr residue may prove useful for linking microcystin-YR via conjugation to other chemicals. Inhibits the synthesis of proteases such as cathepsin D and L, and arginine aminopeptidase.

Product Specific Literature References

Structural studies on cyanoginosins-LR, -YR, -YA, and -YM, peptide toxins from Microcystis aeruginosa: D.P. Botes, et al.; JCS Perkin Trans. I, 2747 (1985)
Cyanobacteria secondary metabolites - the cyanotoxins: W.W. Carmichael; J. Appl. Bacteriol. 72, 445 (1992) Abstract
Extraction and high-performance liquid chromatographic method for the determination of microcystins in raw and treated waters: L.A. Lawton, et al.; Analyst 119, 1525 (1994) Abstract
Characterization of natural toxins with inhibitory activity against serine/threonine protein phosphatases: R.E. Honkanen, et al.; Toxicon 32, 339 (1994) Abstract
Isolation and characterization of microcystins from laboratory cultures and environmental samples of Microcystis aeruginosa and from an associated animal toxicosis: L.A. Lawton, et al.; Nat. Toxins 3, 50 (1995) Abstract
The cyanotoxins: W.W. Carmichael; Adv. Bot. Res. 27, 211 (1997)
The toxicology of microcystins: R.M. Dawson; Toxicon 36, 953 (1998) Abstract
Molecular mechanisms underlying inhibition of protein phosphatases by marine toxins: J.F. Dawson and C.F. Holmes; Front. Biosci. 4, D646 (1999) Abstract
Isolation and detection of microcystins and nodularins, cyanobacterial peptide hepatotoxins: J. Meriluoto, et al.; Methods Mol. Biol. 145, 65 (2000) Abstract
Toxicology and evaluation of microcystins: P.K. Lam, et al.; Ther. Drug. Monit. 22, 69 (2000) Abstract
Influence of microcystin-YR and nodularin on the activity of some proteolytic enzymes in mouse liver: A. Lankoff & A. Kolataj; Toxicon. 39, 419 (2001) Abstract
Molecular enzymology underlying regulation of protein phosphatase-1 by natural toxins: C.F. Holmes, et al.; Curr. Med. Chem. 9, 1981 (2002) Abstract
The microcystins and nodularins: cyclic polypeptide inhibitors of PP1 and PP2A: B.M. Gulledgea, et al.; Curr. Med. Chem. 9, 1991 (2002) Abstract
Production of secondary metabolites by freshwater cyanobacteria: K. Harada; Pharm. Bull. 52, 889 (2004) Abstract
Genetic contributions to the risk assessment of microcystin in the environment: E. Dittmann and T. Borner; Toxicol. Appl. Pharmacol. 203, 192 (2005) Abstract
Detection of the cyanobacterial hepatotoxins microcystins: J. McElhiney and L.A. Lawton; Toxicol. Appl. Pharmacol. 203, 219 (2005) Abstract
Guidance values for microcystins in water and cyanobacterial supplement products (blue-green algal supplements): a reasonable or misguided approach?: D. Dietrich and S. Hoeger; Toxicol. Appl. Pharmacol. 203, 273 (2005) Abstract
Acute and subacute toxic effects produced by microcystin-YR on the fish cell lines RTG-2 and PLHC-1: S. Pichardo, et al.; Toxicol. In Vitro 21, 1460 (2007) Abstract

ALX-350-148	Microcystin-LY
ALX-350-080	Microcystin-LW
ALX-350-012	Microcystin-LR
ALX-350-081	Microcystin-LF
ALX-350-096	Microcystin-LA
ALX-350-043