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Items 17 of 17
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:
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ALX-260-005-M001
1 mg
22.00 USD
ALX-260-005-M005
5 mg
75.00 USD
Product Specification
FORMULA:
C
21
H
38
N
4
O
8
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
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
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ALX-260-007-M005
5 mg
55.00 USD
ALX-260-007-M025
25 mg
195.00 USD
Product Specification
FORMULA:
C
15
H
27
N
5
O
5
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
SYNONYMS
Z-Leu-norleucinal
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains/Related Products
Ordering Information
Product Numbers:
Format:
Size:
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ALX-260-014-M005
5 mg
85.00 USD
ALX-260-014-M010
10 mg
160.00 USD
Product Specification
FORMULA:
C
20
H
30
N
2
O
4
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 Ca
2+
-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
SYNONYMS
Calpain Inhibitor
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains/Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-103-M001
1 mg
75.00 USD
ALX-270-103-M005
5 mg
300.00 USD
Product Specification
FORMULA:
(C
26
H
39
N
3
O
8
)
2
. H
2
SO
4
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-270-280
Revised 07-Apr-08
clasto-Lactacystin β-lactone (synthetic)
SYNONYMS
Omuralide
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics - Proteasome/Ubiquitin Modulators
Ordering Information
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Format:
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ALX-270-280-C200
200 µg
280.00 USD
ALX-270-280-M001
1 mg
1'295.00 USD
Product Specification
FORMULA:
C
10
H
15
NO
4
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:
K
obs
/[I]=20’000M
-1
s
-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
1
H-NMR.
Product Description
Highly specific, cell permeable, and irreversible 20S proteasome inhibitor. Inhibits ubiquitin proteasome pathway in cell culture (IC
50
=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 Inhibitors
•
Proteasome/Related Products
•
MMP Inhibitors
ALX-620-080
Revised 23-May-06
bADA
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
Product Specification
FORMULA:
C
34
H
42
N
4
O
7
S
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-260-009
Revised 19-Dec-07
Leupeptin (synthetic)
SYNONYMS
Acetyl-L-leucyl-L-leucyl-L-argininal . sulfate
PRODUCT LINE
Cancer
PRODUCT CATEGORY
Cathepsin Inhibitors
Ordering Information
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ALX-260-009-M005
5 mg
40.00 USD
ALX-260-009-M025
25 mg
95.00 USD
ALX-260-009-M100
100 mg
320.00 USD
Product Specification
FORMULA:
C
20
H
38
N
6
O
4
. 0.5 H
2
SO
4
MW:
426.6 . 49.0
CAS NUMBER:
103476-89-7
MERCK INDEX:
14:
5456
SOURCE/HOST:
Synthetic.
PURITY:
≥95%
APPEARANCE:
Lyophilized.
SOLUBILITY:
Soluble in water, methanol and 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Competitive and reversible inhibitor of serine and cysteine proteinases like calpain, porcine kallikrein, trypsin, plasmin, papain and cathepsin B. Does not inhibit chymotrypsin and thrombin. Also known to inhibit activation-induced programmed cell death and restoration of defective immune responses of HIV
+
donors.
Product Specific Literature References
Isolation and characterization of leupeptins produced by Actinomycetes:
S. Kondo, et al.; Chem. Pharm. Bull.
17
, 1896 (1969)
Abstract
Leupeptin and E-64, inhibitors of cysteine proteinases, prevent gentamicin-induced lysosomal phospholipidosis in cultured rat fibroblasts:
J.P. Montenez, et al.; Toxicol. Lett.
73
, 201 (1994)
Abstract
Inhibition of activation-induced programmed cell death and restoration of defective immune responses of HIV+ donors by cysteine protease inhibitors:
A. Sarin, et al.; J. Immunol.
153
, 862 (1994)
Abstract
Ceramide-induced apoptosis occurs independently of caspases and is decreased by leupeptin:
M.A. Belaud-Rotureau, et al.; Cell Death Differ.
6
, 788 (1999)
Abstract
Further Categories Containing This Product:
Calpains/Related Products
•
Proteases Other Products
ALX-260-017
Revised 07-Jul-08
CA-074
SYNONYMS
N-[L-3-
trans
-Propylcarbamoyloxirane-2-carbonyl]-Ile-Pro-OH
PRODUCT LINE
Cancer
PRODUCT CATEGORY
Cathepsin Inhibitors
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ALX-260-017-M001
1 mg
210.00 USD
Product Specification
FORMULA:
C
18
H
29
N
3
O
6
MW:
383.5
CAS NUMBER:
134448-10-5
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in ethyl acetate (50mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Potent and specific inhibitor of cathepsin B
in vitro
and
in vivo
.
Product Specific Literature References
Novel epoxysuccinyl peptides. Selective inhibitors of cathepsin B, in vitro:
M. Murata, et al.; FEBS Lett.
280
, 307 (1991)
Abstract
Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo:
T. Towatari, et al.; FEBS Lett.
280
, 311 (1991)
Abstract
Specific assay method for the activities of cathepsin L-type cysteine proteinases:
T. Inubushi, et al.; J. Biochem.
116
, 282 (1994)
Abstract
ALX-260-037
Revised 30-May-07
Calpain Inhibitor I
SYNONYMS
Ac-LL-Norleucinal
Ac-Leu-Leu-Nle-CHO
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains/Related Products
Ordering Information
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ALX-260-037-M010
10 mg
80.00 USD
ALX-260-037-M050
50 mg
310.00 USD
Product Specification
FORMULA:
C
20
H
37
N
3
O
4
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 (K
i
=190nM), calpain II (K
i
=220nM), cathepsin B (K
i
=150nM) and cathepsin L (K
i
=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 Products
•
Cathepsin Inhibitors
•
Proteases Other Products
ALX-260-038
Revised 15-Nov-05
Calpain Inhibitor II
SYNONYMS
Ac-LLM-CHO
Ac-Leu-Leu-Met-CHO
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains/Related Products
Ordering Information
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ALX-260-038-M010
10 mg
75.00 USD
ALX-260-038-M050
50 mg
290.00 USD
Product Specification
FORMULA:
C
19
H
35
N
3
O
4
S
MW:
401.6
CAS NUMBER:
110115-07-6
PURITY:
≥96%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in 100% ethanol, methanol or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:
Protect from light and moisture.
Product Description
Inhibitor of calpain I, calpain II, cathepsin B and cathepsin L.
Further Categories Containing This Product:
Cathepsin Inhibitors
ALX-260-085
Revised 23-Jan-07
Pepstatin A (synthetic)
