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Items 12 of 12
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
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
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-260-014
Revised 19-Aug-08
Calpeptin
SYNONYMS
Z-Leu-norleucinal
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains / Related Products
Ordering Information
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Format:
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Quantity:
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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-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
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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
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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-260-070
Revised 24-Apr-08
Proteasome Substrate III (Fluorogenic)
SYNONYMS
Calpain Substrate (Fluorogenic)
Suc-LLVY-AMC
Suc-Leu-Leu-Val-Tyr-AMC
PRODUCT LINE
Ubiquitin & Proteasome
PRODUCT CATEGORY
Proteasome / Related Products
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ALX-260-070-M001
1 mg
25.00 USD
ALX-260-070-M005
5 mg
60.00 USD
Product Specification
SEQUENCE:
Suc-Leu-Leu-Val-Tyr-AMC (AMC=7-Amino-4-methylcoumarin)
FORMULA:
C
40
H
52
N
5
O
10
MW:
762.9
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white lyophilized powder.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Fluorogenic proteasome substrate. Also acts as a substrate for many other proteinases.
Product Specific Literature References
Comparative specificity and kinetic studies on porcine calpain I and calpain II with naturally occurring peptides and synthetic fluorogenic substrates:
T. Sasaki, et al.; J. Biol. Chem.
259
, 12489 (1984)
Abstract
;
Full Text
Purification and characterization of a Z-Leu-Leu-Leu-MCA degrading protease expected to regulate neurite formation: a novel catalytic activity in proteasome:
S. Tsubuki, et al.; BBRC
196
, 1195 (1993)
Abstract
Modulation of hypoxia-induced calpain activity in rat renal proximal tubules:
C.L. Edelstein, et al.; Kidney Int.
50
, 1150 (1996)
Abstract
Kinetic characterization of the chymotryptic activity of the 20S proteasome:
R.L. Stein, et al.; Biochemistry
35
, 3899 (1996)
Abstract
An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective:
K.K.W. Wang, et al.; PNAS
93
, 6687 (1996)
Abstract
Reovirus-Induced Apoptosis Is Preceded by Increased Cellular Calpain Activity and Is Blocked by Calpain Inhibitors
:
R.L. Debiasi, et al.; J. Virology
73
, 695 (1999)
Abstract
;
Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION
AMC has an excitation maximum of 380nm and an emission maximum of 460nm.
Further Categories Containing This Product:
Calpains / 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:
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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-270-234
Revised 29-Jan-05
PD 150,606
SYNONYMS
3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic acid
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains / Related Products
Ordering Information
Product Numbers:
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ALX-270-234-M005
5 mg
65.00 USD
Product Specification
FORMULA:
C
9
H
7
IO
2
S
MW:
306.1
PURITY:
≥95%
APPEARANCE:
Off-white solid.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Cell permeable, selective, and non-peptide calpain inhibitor directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases such as cathepsin B and cathepsin L. Prevents dexamethasone-induced apoptosis in thymocytes.
Product Specific Literature References
Modulation of hypoxia-induced calpain activity in rat renal proximal tubules:
C.L. Edelstein, et al.; Kidney Int.
50
, 1150 (1996)
Abstract
An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective:
K.K. Wang, et al.; PNAS
93
, 6687 (1996)
Abstract
Alpha-mercaptoacrylic acid derivatives as novel selective calpain inhibitors:
K.K. Wang, et al.; Adv. Exp. Med. Biol.
389
, 95 (1996)
Abstract
Crystal structure of calcium bound domain VI of calpain at 1.9A resolution and its role in enzyme assembly, regulation, and inhibitor binding:
G.D. Lin, et al.; Nat. Struct. Biol.
4
, 539 (1997)
Abstract
Calpains mediate calcium and chloride influx during the late phase of cell injury:
S.L. Waters, et al.; J. Pharmacol. Exp. Ther.
283
, 1177 (1997)
Abstract
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
ALX-804-050
Revised 10-Nov-08
Monoclonal Antibody to µ-Calpain (Domain III) (9A4H8D3)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains / Related Products
Ordering Information
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ALX-804-050-R100
100 µl
379.00 USD
Product Specification
SPECIES CROSSREACTIVITY:
Human
Mouse
Rat
Pig
Others
CLONE:
9A4H8D3
ISOTYPE:
Mouse IgG1
FORMULATION:
Liquid. Ascites containing 0.05% sodium azide.
IMMUNOGEN:
Purified bovine µ-calpain.
SPECIFICITY:
Recognizes an epitope in domain III (aa 465-520) of µ-calpain from several mammalian sources (e.g. human, mouse, rat, pig, bovine, hamster, rabbit). Detects a band of ~80kDa by Western blot. Does not cross-react with m-calpain, n-calpain, calmodulin or calpastatin.
APPLICATION:
Immunocytochemistry (1:100)
Immunohistochemistry (frozen sections)
Western Blot (1:2’000)
Note:
Not recommended for immunoprecipitation.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Avoid freeze/thaw cycles.
Product Description
This antibody has been successfully used in Western blot procedures to detect µ-calpain from human platelets and erythrocytes, bovine platelets, heart and skeletal muscle, and rat myoblasts, kidney, liver and spleen. Immunofluorescence staining of µ-calpain in porcine LLC-PK1 cells with 804-050 results in diffuse cytoplasmic staining.
Product Specific Literature References
A comparison of the intracellular distribution of mu-calpain, m-calpain, and calpastatin in proliferating human A431 cells:
R.D. Lane, et al.; Exp. Cell Res.
203
, 5 (1992)
Abstract
Effect of monoclonal antibodies specific for the 28-kDa subunit on catalytic properties of the calpains:
J. Cong, et al.; J. Biol. Chem.
268
, 25740 (1993)
Abstract
;
Full Text
Calpain-dependent proteolytic cleavage of the p35 cyclin-dependent kinase 5 activator to p25:
G. Kusakawa, et al.; J. Biol. Chem.
275
, 17166 (2000)
Abstract
;
Full Text
Calpain is a major cell death effector in selective striatal degeneration induced in vivo by 3-nitropropionate: implications for Huntington’s disease:
N. Bizat, et al.; J. Neurosci.
23
, 5020 (2003)
Abstract
;
Full Text
Further Categories Containing This Product:
Monoclonal Antibodies
ALX-804-051
Revised 09-Oct-08
Monoclonal Antibody to µ-Calpain (Domain II) (2H2A7C2)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains / Related Products
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ALX-804-051-R100
100 µl
379.00 USD
Product Specification
SPECIES CROSSREACTIVITY:
Human
Rat
Pig
Others
CLONE:
2H2A7C2
ISOTYPE:
Mouse IgG1
FORMULATION:
Liquid. Ascites containing 0.05% sodium azide.
IMMUNOGEN:
Purified bovine µ-calpain.
SPECIFICITY:
Recognizes an epitope in domain II (aa 245-265) of µ-calpain from several mammalian sources (e.g. human, rat, pig, bovine). Detects aband of ~80kDa by Western blot. Does not cross-react withm-calpain, n-calpain, calmodulin or calpastatin.
APPLICATION:
Immunocytochemistry (1:25)
Western Blot (1:1'000)
Note:
Not recommended for immunoprecipitation.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Avoid freeze/thaw cycles.
General Information
The calpain (Ca
2+
-dependent proteinase or Ca
2+
-activated neutral protease) system consists of two ubiquitous forms of calpain (m-calpain and µ-calpain), a tissue specific calpain (n-calpain), and a calpain inhibitory protein (calpastatin). The calpain system has been detected in every vertebrate tissue examined, and has been suggested to play a regulatory role in cellular protein metabolism. This regulatory role may have important implications in platelet aggregation and pathologies associated with altered Ca
2+
homeostasis and protein metabolism such as ischemic cell injury and degenerative diseases. Inhibitors of calpain have been shown to block dexamethasone and low-level irradiation induced apoptosis in thymocytes suggesting that calpain has a regulatory or mechanistic role in apoptotic cell death.
m- and µ-calpains are heterodimers consisting of 28 kDa and 80 kDa subunits. The 28 kDa subunit is identical in the two isoforms, but the 80 kDa subunits differ with ~50% sequence similarity. 28 kDa/80 kDa complexes are thought to be inactive proenzymes which, upon binding of Ca
2+
, undergo conformational changes that promotes cleavage of the 28 kDa subunit and results in enzyme activation.
BACKGROUND/TECHNICAL INFORMATION
Immunocytochemical staining of µ-calpain in pig LLC-PK1 cells with Prod. No. ALX-804-051 results in diffuse cytoplasmic staining.
Further Categories Containing This Product:
Monoclonal Antibodies
ALX-804-053
Revised 11-Jan-05
Monoclonal Antibody to Calpain (156)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Calpains / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-804-053-R100
100 µl
379.00 USD
Product Specification
SPECIES CROSSREACTIVITY:
Human
Others
CLONE:
156
ISOTYPE:
Mouse IgG1
FORMULATION:
Liquid. Ascites diluted in PBS containing 0.05% sodium azide.
IMMUNOGEN:
Purified 28kDa calpain subunit from bovine skeletal muscle.
SPECIFICITY:
Recognizes human and bovine 28kDa calpain subunit. Detects a band of ~28kDa by Western blot. Does not cross-react with the human 80kDa m-calpain subunit.
APPLICATION:
Western Blot (1:1'000)
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Avoid freeze/thaw cycles.
Product Description
The calpain (calcium-dependent protease or calcium-activated neutral protease) system consists of two ubiquitous forms of calpain (µ-calpain and m-calpain), a tissue specific calpain (n-calpain), and a calpain inhibitory protein (calpastatin). The calpain system has been detected in every vertebrate tissue examined, and has been suggested to play a regulatory role in cellular protein metabolism. This regulatory role may have important implications in platelet aggregation and pathologies associated with altered calcium homeostasis and protein metabolism such as ischemic cell injury and degenerative diseases. Inhibitors of calpain have been shown to block dexamethasone and low-level irradiation induced apoptosis in thymocytes suggesting that calpain has a regulatory or mechanistic role in apoptotic cell death.
µ- and m-calpains are heterodimers consisting of 28 kDa and 80 kDa subunits. The 28 kDa subunit is identical in the two isoforms, but the 80 kDa subunits differ with ~50% sequence similarity. 28 kDa/80 kDa complexes are thought to be inactive proenzymes which, upon binding of calcium, undergo conformational changes that promotes cleavage of the 28 kDa subunit and results in enzyme activation.
Product Specific Literature References
Effect of monoclonal antibodies specific for the 28-kDa subunit on catalytic properties of the calpains:
J. Cong, et al.; J. Biol. Chem.
268
, 25740 (1993)