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ALX-430-096
Revised 24-Feb-05
A77 1726
SYNONYMS
N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-430-096-M005
5 mg
45.00 USD
ALX-430-096-M025
25 mg
180.00 USD
Product Specification
FORMULA:
C
12
H
9
F
3
N
2
O
2
MW:
270.2
CAS NUMBER:
108605-62-5
PURITY:
≥98%
APPEARANCE:
White solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light. Keep under inert gas.
Product Description
Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No.
ALX-430-095
). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2)
in vitro
and
in vivo
.
Product Specific Literature References
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide:
T. Mattar, et al.; FEBS Lett.
334
, 161 (1993)
Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide:
X. Xu, et al.; J. Biol. Chem.
270
, 12398 (1995)
Abstract
;
Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase:
J.P. Davis, et al.; Biochemistry
35
, 1270 (1996)
Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation:
X. Xu, et al.; Biochem. Pharmacol.
52
, 527 (1996)
Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms:
R.T. Elder, et al.; J. Immunol.
159
, 22 (1997)
Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice:
X. Xu, et al.; J. Immunol.
159
, 167 (1997)
Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression:
S.K. Manna & B.B. Aggarwal; J. Immunol.
162
, 2095 (1999)
Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner:
L.C. Hamilton, et al.; Br. J. Pharmacol.
127
, 1589 (1999)
Abstract
Further Categories Containing This Product:
NF-kB Pathway Inhibitors
•
COX Inhibitors
•
Immunomodulators Other Products
ALX-260-046
Revised 06-Jun-08
Ac-AAVALLPAVLLALLAPDEVD-CHO
SYNONYMS
Caspase-3 Inhibitor (Aldehyde)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-260-046-M001
1 mg
70.00 USD
ALX-260-046-M005
5 mg
290.00 USD
Product Specification
SEQUENCE:
Ac-Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Asp-Glu-Val-Asp-CHO
FORMULA:
C
94
H
158
N
20
O
27
MW:
2000.4
PEPTIDE CONTENT:
65-95%.
PURITY:
≥95% (HPLC)
APPEARANCE:
White to off-white powder.
FORMULATION:
Lyophilized. TFA salt.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry. After dissolving, prepare aliquots and store at -20°C
Product Description
Reversible, cell permeable inhibitor of caspase-3. Also inhibits caspase-6, -7, -8 and -10.
Product Specific Literature References
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis:
W. Nicholson, et al.; Nature
376
, 37 (1995)
Abstract
Yama/CPP32 beta, a mammalian homolog of CED-3, is a CrmA-inhibitable protease that cleaves the death substrate poly(ADP-ribose) polymerase:
M. Tewari, et al.; Cell
81
, 801 (1995)
Abstract
Activation of CPP32-like proteases is not sufficient to trigger apoptosis: inhibition of apoptosis by agents that suppress activation of AP24, but not CPP32-like activity:
S.C. Wright, et al.; J. Exp. Med.
186
, 1107 (1997)
Abstract
ALX-260-047
Revised 27-Aug-08
Ac-AAVALLPAVLLALLAPYVAD-CHO
SYNONYMS
Caspase-1 Inhibitor (Aldehyde)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-047-M001
1 mg
170.00 USD
ALX-260-047-M005
5 mg
680.00 USD
Product Specification
SEQUENCE:
Ac-Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Tyr-Val-Ala-Asp-CHO
FORMULA:
C
97
H
160
N
20
O
24
MW:
1990.5
PEPTIDE CONTENT:
78-98%
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO (0.25mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry. After reconstitution, prepare aliquots and store at -20°C.
Product Description
Reversible, cell permeable inhibitor of caspase-1.
ALX-260-158
Revised 16-Feb-05
Ac-AEVD-CHO
SYNONYMS
Caspase-10 Inhibitor (Aldehyde)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
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ALX-260-158-M001
1 mg
60.00 USD
ALX-260-158-M005
5 mg
240.00 USD
Product Specification
SEQUENCE:
Z-Ala-Glu-Val-Asp-aldehyde
FORMULA:
C
19
H
30
N
4
O
9
MW:
458.5
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
Product Description
Inhibitor of caspase-10. Also inhibits caspase-6 and -8.
ALX-260-114
Revised 24-Feb-05
Ac-AEVD-AFC
SYNONYMS
Caspase-6 Substrate (Fluorogenic)
Caspase-8 Substrate (Fluorogenic)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Substrates
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-114-M005
5 mg
157.00 USD
ALX-260-114-M010
10 mg
295.00 USD
Product Specification
SEQUENCE:
Ac-Ala-Glu-Val-Asp-AFC (AFC=7-Amino-4-trifluoromethylcoumarin)
FORMULA:
C
29
H
34
F
3
N
5
O
11
MW:
685.6
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry.
Product Description
Fluorogenic substrate for caspase-6 and -8.
General Information
BACKGROUND/TECHNICAL INFORMATION
AFC has an excitation maximum of 400nm and an emission maximum of 505nm.
ALX-260-032
Revised 27-Apr-05
Ac-DEVD-AFC
SYNONYMS
Caspase-3 Substrate (Fluorogenic)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Substrates
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-032-M001
1 mg
47.00 USD
ALX-260-032-M005
5 mg
138.00 USD
Product Specification
SEQUENCE:
Ac-Asp-Glu-Val-Asp-AFC (AFC = 7-Amino-4-trifluoromethylcoumarin)
FORMULA:
C
30
H
34
F
3
N
5
O
13
MW:
729.6
PEPTIDE CONTENT:
65-95%
PURITY:
≥96% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in dimethyl formamide, DMSO or methanol; slightly soluble in water (0.4mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry.
Product Description
Fluorogenic substrate for caspase-3. Also a substrate for caspase-1, -4 and -7. This product is similar to Ac-DEVD-AMC (Prod. No.
ALX-260-031
) but the AFC fluorophore has a greater Stokes’ shift upon cleavage. The peptide sequence is based on the PARP cleavage site Asp
216
for caspase-3.
Product Specific Literature References
BAX-induced cell death may not require interleukin 1 β-converting enzyme-like proteases:
J. Xiang, et al.; Proc. Natl. Acad. Sci. USA
93
, 14559 (1996)
Abstract
Different subcellular distribution of caspase-3 and caspase-7 following Fas-induced apoptosis in mouse liver:
J.M. Chandler, et al.; J. Biol. Chem.
273
, 10815 (1998)
Abstract
;
Full Text
Caspase-7 is activated during lovastatin-induced apoptosis of the prostate cancer cell line LNCaP:
M. Marcelli, et al.; Cancer Res.
58
, 76 (1998)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
AFC has an excitation maximum of 400nm and an emission maximum of 505nm.
ALX-260-031
Revised 02-Mar-06
Ac-DEVD-AMC
SYNONYMS
Caspase-3 Substrate (Fluorogenic)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Substrates
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-031-M001
1 mg
40.00 USD
ALX-260-031-M005
5 mg
115.00 USD
Product Specification
SEQUENCE:
Ac-Asp-Glu-Val-Asp-AMC (AMC = 7-Amino-4-methylcoumarin)
FORMULA:
C
30
H
37
N
5
O
13
MW:
675.7
PEPTIDE CONTENT:
70-95%
PURITY:
≥97% (HPLC)
FORMULATION:
Lyophilized.
SOLUBILITY:
Soluble in DMSO. Dilute with buffer, pH 7.5.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Fluorogenic substrate for caspase-3. Also a substrate for caspase-1, -4, -7 and -8. The peptide sequence is based on the PARP cleavage site Asp
216
for caspase-3.
Product Specific Literature References
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis:
D.W. Nicholson, et al.; Nature
376
, 37 (1995)
Abstract
Purification and catalytic properties of human caspase family members:
M. Garcia-Calvo, et al.; Cell Death Differ.
6
, 362 (1999)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
AMC has an excitation maximum of 380nm and an emission maximum of 460nm.
ALX-260-030
Revised 05-Jun-08
Ac-DEVD-CHO
SYNONYMS
Caspase-3 Inhibitor (Aldehyde)
Caspase-7 Inhibitor (Aldehyde)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-030-M001
1 mg
47.00 USD
ALX-260-030-M005
5 mg
183.00 USD
Product Specification
SEQUENCE:
Ac-Asp-Glu-Val-Asp-CHO
FORMULA:
C
20
H
30
N
4
O
11
MW:
502.5
PEPTIDE CONTENT:
70-90%.
PURITY:
≥95% (HPLC)
FORMULATION:
Lyophilized.
SOLUBILITY:
Soluble in distilled water or DMSO.
RECONSTITUTION:
Add 0.2ml DMSO per 1mg peptide. Shake well until all the contents are dissolved. This furnishes a 10mM solution of this material.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions should be divided into aliquots and stored at -20°C. Solutions are stable for at least 1 month when stored at -20°C in the dark and protected from moisture.
HANDLING:
Keep cool and dry. Keep under nitrogen.
Product Description
Reversible inhibitor of caspase-3 and -7.
Product Specific Literature References
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis:
D.W. Nicholson, et al.; Nature
376
, 37 (1995)
Abstract
Sequential activation of ICE-like and CPP32-like proteases during Fas- mediated apoptosis:
M. Enari, et al.; Nature
380
, 723 (1996)
Abstract
ICE/CED3-like proteases as therapeutic targets for the control of inappropriate apoptosis:
D.W. Nicholson; Nature Biotechnol.
14
, 297 (1996)
Abstract
CPP32/apopain is a key interleukin 1 beta converting enzyme-like protease involved in Fas-mediated apoptosis:
J. Schlegel, et al.; J. Biol. Chem.
271
, 1841 (1996)
Abstract
;
Full Text
A sequential two-step mechanism for the production of the mature p17:p12 form of caspase-3 in vitro:
Z. Han, et al.; J. Biol. Chem.
272
, 13432 (1997)
Abstract
;
Full Text
Inhibition of human caspases by peptide-based and macromolecular inhibitors:
M. Garcia-Calvo, et al.; J. Biol. Chem.
273
, 32608 (1998)
Abstract
;
Full Text
Inhibition of ubiquitin-proteasome pathway activates a caspase-3-like protease and induces Bcl-2 cleavage in human M-07e leukaemic cells:
X.M. Zhang, et al.; Biochem. J.
340
, 127 (1999)
Abstract
;
Full Text
ALX-260-033
Revised 10-Sep-08
Ac-DEVD-pNA
SYNONYMS
Caspase-3 Substrate (Chromogenic)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Substrates
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-033-M001
1 mg
27.00 USD
ALX-260-033-M005
5 mg
73.00 USD
Product Specification
SEQUENCE:
Ac-Asp-Glu-Val-Asp-pNA (pNA = p-Nitroaniline)
FORMULA:
C
26
H
34
N
6
O
13
MW:
638.6
PEPTIDE CONTENT:
70-95%
PURITY:
≥97% (HPLC)
APPEARANCE:
White to off-white powder.
FORMULATION:
Lyophilized.
SOLUBILITY:
Soluble in DMSO or buffer, pH 7.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Always use fresh solutions.
HANDLING:
Keep cool and dry.
Product Description
Chromogenic substrate for caspase-3. Also a substrate for caspase-1, -4 and -7.
Product Specific Literature References
Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis:
D.W. Nicholson, et al.; Nature
376
, 37 (1995)
Abstract
Activation of the CPP32 protease in apoptosis induced by 1-beta-D- arabinofuranosylcytosine and other DNA-damaging agents:
R. Datta, et al.; Blood
88
, 1936 (1996)
Abstract
Substrate specificities of caspase family proteases:
R.V. Talanian, et al.; J. Biol. Chem.
272
, 9677 (1997)
Abstract
;
Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION
λmax of pNA is 400nm.
ALX-260-078
Revised 17-Jan-06
Ac-DMQD-AMC
SYNONYMS
Caspase-3 Substrate (Fluorogenic)
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Caspase Substrates
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-260-078-M001
1 mg
42.00 USD
ALX-260-078-M005
5 mg
163.00 USD
Product Specification
SEQUENCE:
Ac-Asp-Met-Gln-Asp-AMC (AMC=7-Amino-4-methylcoumarin)
FORMULA:
C
30
H
38
N
6
O
12
S
MW:
706.7
PEPTIDE CONTENT:
75-95%.
PURITY:
≥98% (HPLC)
APPEARANCE:
White powder.
SOLUBILITY:
Soluble in DMSO. Dilute with distilled water or buffer. Also soluble in phosphate buffer, pH 7.5
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry.
Product Description
Fluorogenic substrate for caspase-3.
Product Specific Literature References
Bid truncation, bid/bax targeting to the mitochondria, and caspase activation associated with neutrophil apoptosis are inhibited by granulocyte colony-stimulating factor
:
N.A. Maianski, et al.; J. Immunol.
172
, 7024 (2004)
Abstract
The effects of TNF-alpha and inhibitors of arachidonic acid metabolism on human colon HT-29 cells depend on differentiation status
:
M. Kovarikova, et al.; Differentiation
72
, 23 (2004)
Abstract
Interaction of polyunsaturated fatty acids and sodium butyrate during apoptosis in HT-29 human colon adenocarcinoma cells
:
J. Hofmanova; Eur. J. Nutrition
44
, 40 (2005)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
AMC has an excitation maximum of 380nm and an emission maximum of 460nm.
ALX-260-077
Revised 10-Feb-05
Ac-DMQD-CHO
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