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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-850-043
Revised 27-Jul-05
ABSOLUTE-S™ Kit
PRODUCT LINE
Cell Death / Apoptosis / Autophagy
PRODUCT CATEGORY
DNA-based Apoptosis Detection
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-850-043-KI01
1 Kit
540.00 USD
Product Specification
QUANTITY:
50 assays.
KIT/SET CONTAINS:
Contains all the reagents necessary, including positive and negative control cells.
SHIPPING:
SHIPPED ON DRY ICE
LONG TERM STORAGE:
-20°C
POSITIVE CONTROL INCLUDED:
yes
Product Description
The kit utilizes the SBIP™ (strand break induced photolysis) methodology in which cells are irradiated with UV light to induce strand breaks. Does not require DNA denaturation and, therefore, is applicable in studies where preservation of antigens or other features of the cells is desired.
Product Specific Literature References
Detection of 5-bromo-2-deoxyuridine incorporated into DNA by labeling strand breaks induced by photolysis (
SBIP
):
X. Li, et al.; Int. J. Oncol.
4
, 1157 (1994)
Detection of apoptosis and DNA replication by differential labeling of DNA strand breaks with fluorochromes of different color:
X. Li, et al.; Exp. Cell. Res.
222
, 28 (1996)
Abstract
General Information
MANUFACTURER
Manufactured by Phoenix Flow Systems.
Further Categories Containing This Product:
Detection Kits
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
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 (1