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ALX-380-091
Revised 21-Aug-08
17-AAG
SYNONYMS
17-(Allylamino)-17-desmethoxygeldanamycin
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antitumor Antibiotics
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-380-091-C100
100 µg
65.00 USD
ALX-380-091-M001
1 mg
162.00 USD
Product Specification
FORMULA:
C
31
H
43
N
3
O
8
MW:
585.7
CAS NUMBER:
75747-14-7
SOURCE/HOST:
Semisynthetic derivative from geldanamycin.
PURITY:
≥97%
APPEARANCE:
Red to dark red powder.
SOLUBILITY:
Soluble in DMSO (10mg/ml) or methanol (10mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
Potent, less toxic derivative of geldanamycin (Prod. No.
ALX-380-054
). Inhibits the essential ATPase activity of HSP90. Inhibitor of telomerase activity. Inducer of apoptosis with antitumor activity.
Product Specific Literature References
Inhibition of the oncogene product p185erbB-2 in vitro and in vivo by geldanamycin and dihydrogeldanamycin derivatives:
R.C. Schnur, et al.; J. Med. Chem.
38
, 3806 (1995)
Abstract
The benzoquinone ansamycin 17-allylamino-17-demethoxygeldanamycin binds to HSP90 and shares important biologic activities with geldanamycin:
T.W. Schulte & L.M. Neckers; Cancer Chemother. Pharmacol.
42
, 273 (1998)
Abstract
Gene expression profiling of human colon cancer cells following inhibition of signal transduction by 17-allylamino-17-demethoxygeldanamycin, an inhibitor of the hsp90 molecular chaperone:
P.A. Clarke, et al.; Oncogene
19
, 4125 (2000)
Abstract
Geldanamycin and its analogue 17-allylamino-17-demethoxygeldanamycin lowers Bcr-Abl levels and induces apoptosis and differentiation of Bcr-Abl-positive human leukemic blasts:
R. Nimmanapalli, et al.; Cancer Res.
61
, 1799 (2001)
Abstract
;
Full Text
Inhibition of heat shock protein 90 function by ansamycins causes the morphological and functional differentiation of breast cancer cells:
P.N. Munster, et al.; Cancer Res.
61
, 2945 (2001)
Abstract
;
Full Text
Disruption of the EF-2 kinase/Hsp90 protein complex: a possible mechanism to inhibit glioblastoma by geldanamycin:
J. Yang, et al.; Cancer Res.
61
, 4010 (2001)
Abstract
;
Full Text
Enhancement of paclitaxel-mediated cytotoxicity in lung cancer cells by 17-allylamino geldanamycin: in vitro and in vivo analysis:
D.M. Nguyen, et al.; Ann. Thorac. Surg.
72
, 371 (2001)
Abstract
ErbB2 degradation mediated by the co-chaperone protein CHIP:
P. Zhou, et al.; J. Biol. Chem.
278
, 13829 (2003)
Abstract
Inhibition of telomerase activity by geldanamycin and 17-allylamino, 17-demethoxygeldanamycin in human melanoma cells:
R. Villa, et al.; Carcinogenesis
24
, 851 (2003)
Abstract
Geldanamycin and its 17-allylamino-17-demethoxy analogue antagonize the action of Cisplatin in human colon adenocarcinoma cells: differential caspase activation as a basis for interaction:
I.A. Vasilevskaya, et al.; Cancer Res.
63
, 3241 (2003)
Abstract
A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors:
A. Kamal, et al.; Nature
425
, 407 (2003)
Abstract
Chaperoning oncogenes: HSP90 as a target of geldanamycin:
L. Neckers; Handb. Exp. Pharmacol. 259 (2006)
Abstract
Drugging the cancer chaperone HSP90: Combinatorial therapeutic exploitation of oncogene addiction and tumor stress:
P. Workman, et al.; Ann. N.Y. Acad. Sci.
1113
, 202 (2007)
Abstract
Synergism between etoposide and 17-AAG in leukemia cells: critical roles for Hsp90, FLT3, topoisomerase II, Chk1, and Rad51:
Q. Yao, et al.; Clin. Cancer Res.
13
, 1591 (2007)
Abstract
;
Full Text
Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers:
R.K. Ramanathan, et al.; Clin. Cancer Res.
13
, 1769 (2007)
Abstract
HSP90 inhibitor 17AAG causes apoptosis in ATRA-resistant acute promyelocytic leukemia cells:
P.N. Meyer, et al.; Leuk. Res.
32
, 143 (2008)
Abstract
Intratumor injection of the Hsp90 inhibitor 17AAG decreases tumor growth and induces apoptosis in a prostate cancer xenograft model:
C.R. Williams, et al.; J. Urol.
178
, 1528 (2007)
Abstract
Rituximab and 17-allylamino-17-demethoxygeldanamycin induce synergistic apoptosis in B-cell chronic lymphocytic leukaemia:
A.J. Johnson, et al.; Br. J. Haematol.
139
, 837 (2007)
Abstract
An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models:
U. Banerji, et al.; Cancer Chemother. Pharmacol.
62
, 769 (2008)
Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors
•
Tyrosine Kinase Inhibitors
•
Antibiotics - Other Signal Transduction Pathway Modulators
•
Antitumor Agents (Enzyme Inhibitors)
•
HSP90 / HtpG / Related Products
ALX-430-156
Revised 21-Apr-08
6BIO
SYNONYMS
(2’Z,3’E)-6-Bromoindirubin-3’-oxime
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
GSK-3 Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-430-156-M001
1 mg
40.00 USD
Product Specification
FORMULA:
C
16
H
10
BrN
3
O
2
MW:
356.2
CAS NUMBER:
667463-62-9
PURITY:
≥98%
APPEARANCE:
Dark red solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
IRRITANT.
Product Description
Inhibitor of phosphoinositide-dependent kinase 1 (PDK1). Potent, reversible and ATP-competitive inhibitor of glycogen synthase kinase-3α/β (GSK-3α/β).
Product Specific Literature References
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases:
P. Polychronopoulos, et al.; J. Med. Chem.
47
, 935 (2004)
Abstract
7-Bromoindirubin-3’-oxime induces caspase-independent cell death:
J. Ribas, et al.; Oncogene
25
, 6304 (2006)
Abstract
Inverse in silico screening for identification of kinase inhibitor targets:
S. Zahler, et al.; Chem. Biol.
14
, 1207 (2007)
Abstract
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins:
V. Myrianthopoulos, et al.; J. Med. Chem.
50
, 4027 (2007)
Abstract
Related Products
ALX-270-271
Indirubin-3'-monoxime
ALX-430-149
7BIO
ALX-430-157
Me-7BIO
ALX-270-296
Indirubin-5-sulfonic acid . sodium salt
ALX-270-361
Indirubin
ALX-270-424
5-Iodo-indirubin-3'-monoxime
Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other Products
ALX-430-149
Revised 23-Jun-08
7BIO
SYNONYMS
(2’Z, 3’E)-7-Bromoindirubin-3’-monoxime
MLS2156
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
Non-apoptotic Cell Death / Necrosis
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-430-149-M005
5 mg
80.00 USD
ALX-430-149-M025
25 mg
320.00 USD
Product Specification
FORMULA:
C
16
H
10
BrN
3
O
2
MW:
356.2
PURITY:
≥95% (
1
H-NMR)
APPEARANCE:
Dark brown solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
IRRITANT.
Product Description
Induces a rapid caspase-independent cell death process distinct from apoptosis. Demonstrated selective inhibition of aurora kinase B (IC
50
=4.6µM) and aurora kinase C (IC
50
=0.7µM) whereas the homologeous aurora kinase A is poorly inhibited.
Product Specific Literature References
3’-Substituted 7-halogenoindirubins, a new class of cell death inducing agents:
Y. Ferandin, et al.; J. Med. Chem.
49
, 4638 (2006)
Abstract
7-Bromoindirubin-3’-oxime induces caspase-independent cell death:
J. Ribas, et al.; Oncogene
25
, 6304 (2006)
Abstract
An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins:
V. Myrianthopoulos, et al.; J. Med. Chem.
50
, 4027 (2007)
Abstract
7-Bromoindirubin-3’-oxime uncovers a serine protease-mediated paradigm of necrotic cell death:
J. Ribas, et al.; Biochem. Pharmacol.
76
, 39 (2008)
Abstract
Related Products
ALX-270-271
Indirubin-3'-monoxime
ALX-430-157
Me-7BIO
ALX-430-156
6BIO
ALX-270-296
Indirubin-5-sulfonic acid . sodium salt
ALX-270-361
Indirubin
ALX-270-424
5-Iodo-indirubin-3'-monoxime
Further Categories Containing This Product:
Aurora / Related Products
ALX-270-039
Revised 15-Nov-06
A-3 . hydrochloride
SYNONYMS
N-(2-Aminoethyl)-5-chloronaphthalene-1-sulfonamide . HCl
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PKA Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-039-M010
10 mg
65.00 USD
ALX-270-039-M050
50 mg
260.00 USD
Product Specification
FORMULA:
C
12
H
13
ClN
2
O
2
S . HCl
MW:
284.8 . 36.5
PURITY:
≥98%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Inhibitor of cAMP- and cGMP-dependent protein kinase (PKA and PKG), protein kinase C (PKC), casein kinase I and II, and myosin light chain kinase.
Product Specific Literature References
Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors:
M. Inagaki, et al.; Mol. Pharmacol.
29
, 577 (1986)
Abstract
Further Categories Containing This Product:
Myosin Light Chain Kinase Inhibitors
•
PKC Inhibitors
•
PKG Inhibitors
•
Casein Kinase Inhibitors
ALX-450-001
Revised 23-Jul-08
A23187 (free acid)
SYNONYMS
Calcium Ionophore A23187
Calcimycin
Antibiotic A23187
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics - Ionophores
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-450-001-M001
1 mg
28.00 USD
ALX-450-001-M005
5 mg
65.00 USD
ALX-450-001-5001
5x1 mg
80.00 USD
ALX-450-001-M010
10 mg
92.00 USD
ALX-450-001-M025
25 mg
195.00 USD
ALX-450-001-M050
50 mg
350.00 USD
Product Specification
FORMULA:
C
29
H
37
N
3
O
6
MW:
523.6
CAS NUMBER:
52665-69-7
MERCK INDEX:
14:
1639
RTECS:
DM4676000
SOURCE/HOST:
Isolated from
Streptomyces chartreusis
.
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO, 100% ethanol or methylene chloride; slightly soluble in water. Solubilize in DMSO or ethanol prior to preparing aqueous solutions of very low concentrations.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
In aqueous systems product may aggregate over time.
HANDLING:
Protect from light. In aqueous systems, the product aggregates over time.
HAZARD:
IRRITANT.
Product Description
Antibiotic possessing weak
in vitro
antimicrobial activity against gram positive bacteria and fungi. Divalent cation ionophore commonly used to increase intracellular Ca
2+
levels in intact cells.
Product Specific Literature References
A23187: a divalent cation ionophore:
P. W. Reed & H. A. Lardy; J. Biol. Chem.
247
, 6970 (1972)
Abstract
Effects of antibiotic ionophore, A23187, on oxidative phosphorylation and calcium transport of liver mitochondria:
D.T. Wong, et al.; Arch. Biochem. Biophys.
156
, 578 (1973)
Abstract
Biological applications of ionophores:
B.C. Pressman; Annu. Rev. Biochem.
45
, 501 (1976), (Review)
Abstract
Molecular mechanisms of endothelium-mediated vasodilation:
R.R. Fiscus; Semin. Thromb. Hemost.
14 Suppl
, 12 (1988), (Review)
Abstract
Calcium ionophore A23187 action on cardiac myocytes is accompanied by enhanced production of reactive oxygen species: 1740, 481 (2005):
T. Przygodzki, et al.; Biochim. Biophys. Acta
1740
, 481 (2005)
Abstract
Further Categories Containing This Product:
Nitric Oxide Pathway Other Products
•
Respiratory Chain Other Products
•
Antibiotics - ATPase Inhibitors
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:
Add To Cart
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:
Unit Price:
Quantity:
Add To Cart
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
