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ALX-151-026
Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
Ordering Information
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ALX-151-026-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
39
H
57
N
7
O
14
S
MW:
880.0
PURITY:
≥96% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water (1mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Peptide is very unstable.
Product Description
Peptide containing a phosphotyrosyl mimetic. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides:
B. Ye, et al.; J. Med. Chem.
38
, 4270 (1995)
Abstract
Further Categories Containing This Product:
Peptides
•
Phosphoinositide 3-kinase [PI(3)K] / Related Products
ALX-151-027
Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Tyrosine Kinase Inhibitors
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ALX-151-027-M001
1 mg
90.00 USD
Product Specification
FORMULA:
C
36
H
57
N
7
O
13
SP
MW:
858.9
PURITY:
≥96%
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Phosphotyrosine containing peptide. Effective protein tyrosine kinase inhibitor. Inhibits the phosphoinositide 3-kinase (PI(3)K) C-terminal p85 SH2 domain.
Product Specific Literature References
L-O-(2-malonyl)tyrosine: a new phosphotyrosyl mimetic for the preparation of Src homology 2 domain inhibitory peptides:
B. Ye, et al.; J. Med. Chem.
38
, 4270 (1995)
Abstract
Further Categories Containing This Product:
Peptides
•
Phosphoinositide 3-kinase [PI(3)K] / Related Products
ALX-201-055
Revised 17-Apr-07
Phosphoinositide 3-kinase p110γ (human) (recombinant)
SYNONYMS
PI(3)K p110γ (human) (recombinant)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-201-055-C010
10 µg
330.00 USD
Product Specification
EC:
2.7.1.137
SOURCE/HOST:
Produced in Sf9 cells. Full length PI(3)K p110γ (human phosphoinositide-3-kinase p110γ) is fused at the N-terminus to a His-tag.
CONCENTRATION:
1mg/ml
PURITY:
≥95% (SDS-PAGE)
FORMULATION:
Liquid. In 10mM HEPES, pH 7.5, containing 100mM sodium chloride, 0.5mM magnesium chloride and 50% glycerol.
SPECIFIC ACTIVITY:
~4.5nmol/mg/min using phosphatidylinositol as the substrate (lipid kinase activity test).
SHIPPING:
SHIPPED ON DRY ICE
LONG TERM STORAGE:
-20°C
Product Specific Literature References
Cloning and characterization of a G protein-activated human phosphoinositide-3 kinase:
B. Stoyanov, et al.; Science
269
, 690 (1995)
Abstract
Linkage of G protein-coupled receptors to the MAPK signaling pathway through PI 3-kinase gamma:
M. Lopez-Ilasaca, et al.; Science
275
, 394 (1997)
Abstract
Lipid kinase and protein kinase activities of G-protein-coupled phosphoinositide 3-kinase gamma: structure-activity analysis and interactions with wortmannin:
S. Stoyanova, et al.; Biochem. J.
324
, 489 (1997)
Abstract
;
Full Text
Gbetagamma stimulates phosphoinositide 3-kinase-gamma by direct interaction with two domains of the catalytic p110 subuni:
D. Leopoldt, et al.; J. Biol. Chem.
273
, 7024 (1998)
Abstract
;
Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION
Swiss-Prot link P48736:
PI(3)K p110γ (human)
Lipid kinase activity test
:
Kinase reaction buffer: 20mM TRIS-HCl, pH 7.4; 4mM MgCl
2
; 100mM sodium chloride.
- Reaction mixture in total volume of 100ml was:
1x reaction buffer (final concentration), enzyme (4 reactions with 1, 2, 3 or 4µg were performed), 10µg phosphatidylinositol, 20µM cold ATP and 10µCi
32
P-ATP.
- Reaction was started by addition of the
32
P-ATP and incubate for 10 minutes at 37°C.
- Reaction was stopped by adding 150µl 1M HCl.
- L
ipids were extracted with 400µl chloroform:methanol (1:1) by vortexing.
- Extracts were washed
three times with 200µl 1M HCl.
- Incorporation of
32
P in the extracted lipids was measured by mixing extract with 3ml scintillation cocktail (ROTH) and counting in a liquid scintillation analyzer.
- To determine specific activity of PI3K p110γ the assay was performed under the same conditions stated above by using 10µCi
32
P-ATP with a value of 10'000 units.
- Average value of measurements of the lipid extracts of the performed 4 reactions was 227 units for 1µg.
Dividing 10’000 by 227 a factor of 44 times less for the incorporation was determined.
-Total ATP (20µM) was divided by 44 giving 0.454µM for 10 minutes reaction time or 45.4M/min/µg. Recalculation of this value for a 1 liter solution results in
4.5 nmoles/min/mg
.
Further Categories Containing This Product:
Enzymes
•
Recombinant Proteins / Fusion Proteins
ALX-201-119
Revised 01-Mar-05
Phosphoinositide 3-kinase p110α/p85 (bovine) (recombinant)
SYNONYMS
PI(3)K p110α/p85 (bovine) (recombinant)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
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ALX-201-119-C005
5 µg
440.00 USD
Product Specification
MW:
p110α: ~124.3kDa; p85: ~83.5kDa.
SOURCE/HOST:
Produced in Sf9 cells. Bovine PI(3)K p110α/p85 dimer untagged.
CONCENTRATION:
0.1mg/ml
PURITY:
≥90% (SDS-PAGE)
FORMULATION:
Liquid. Recombinant protein in 25mM HEPES, pH 8.0, 25mM sodium chloride, 2.5mM magnesium dichloride and 50% glycerol.
SPECIFIC ACTIVITY:
~1nmol/mg/min using phosphatidyl-inositol as the substrate.
SHIPPING:
SHIPPED ON DRY ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Avoid freeze/thaw cycles.
General Information
Phosphoinositide 3- kinases (PI(3)Ks) phosphorylate the 3'-OH position of inositol phospholipids. The heterodimeric complex consists of a catalytic subunit (p110α) and a regulatory adaptor subunit (p85). The PI(3)K regulates the MAP kinase and the Akt/PKB signalling pathway that is involved in pivotal cellular processes such as mitogenesis, apoptosis and cytoskeletal functions, and also plays an important role in the development of human cancer.
Further Categories Containing This Product:
Enzymes
•
Recombinant Proteins / Fusion Proteins
ALX-210-747
Revised 18-Sep-08
Polyclonal Antibody to Phosphoinositide 3-kinase p110δ (human)
SYNONYMS
anti-PI(3)K p110δ (human) PAb
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-210-747-C200
200 µg
340.00 USD
Product Specification
SPECIES CROSSREACTIVITY:
Human
SOURCE/HOST:
From rabbit.
CONCENTRATION:
1mg/ml
PURITY DETAIL:
Epitope-affinity purified IgG.
FORMULATION:
Liquid. In PBS containing 1mg/ml BSA and 0.1% sodium azide.
IMMUNOGEN:
Synthetic peptide corresponding to aa 1026-1044 (S
1026
WKTKVNWLAHNVSKDNRQ
1044
) of the C-terminal domain of human PI(3)K p110δ (phosphoinositide 3-kinase p110δ)
.
SPECIFICITY:
Recognizes human PI(3)K p110δ. Detects a band of ~110kDa by Western blot.
APPLICATION:
Immunocytochemistry (1:300)
Immunohistochemistry (paraffin sections)
Western Blot (1:1'000)
QUALITY CONTROL:
Western blot on human T cell line Jurkat.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Avoid freeze/thaw cycles. For maximum product recovery after thawing, centrifuge the vial before opening the cap. After opening, prepare aliquots and store at -20°C.
BLOCKING PEPTIDE:
For Blocking Peptide see Prod. No.
ALX-165-034
.
General Literature References
p110delta, a novel phosphoinositide 3-kinase in leukocytes:
B. Vanhaesebroeck, et al.; PNAS
94
, 4330 (1997)
Abstract
;
Full Text
Further Categories Containing This Product:
Polyclonal Antibodies
ALX-210-770
Revised 11-Apr-06
Polyclonal Antibody to pp36 (human)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-210-770-C200
200 µg
340.00 USD
Product Specification
SPECIES CROSSREACTIVITY:
Human
SOURCE/HOST:
From rabbit.
CONCENTRATION:
2mg/ml.
PURITY DETAIL:
Epitope-affinity purified IgG.
FORMULATION:
Liquid. In PBS containing 1mg/ml BSA and 0.1% sodium azide.
IMMUNOGEN:
Synthetic peptide corresponding to aa 29-49 (C
29
HRLPGSYDSTSSDSLYPRGI
49
) of the N-terminal extracellular domain of human pp36.
SPECIFICITY:
Recognizes human pp36. Detects a band of ~40kDa by Western blot.
APPLICATION:
Immunocytochemistry (1:300)
Immunohistochemistry (paraffin sections)
Western Blot (1:1'000)
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
After opening, prepare aliquots and store at -20°C. For maximum product recovery after thawing, centrifuge the vial before opening the cap. Avoid freeze/thaw cycles.
BLOCKING PEPTIDE:
For Blocking Peptide see Prod. No.
ALX-165-042
.
General Information
pp36 is an adaptor protein that bridges proximal T-cell antigen receptor (TCR) signals to the activation of phosphoinositide turnover, Ras and perhaps other signaling pathways in T-cells. In natural killer cells perturbation of the low affinity Fc receptor (CD16) or the addition of target cells leads to the appearance of tyrosine phosphorylated pp36 and triggers its association with Grb2 and PLCγ-1. The amino acid sequence of human and rat pp36 also reveal potential motifs for the SH2 domains of Grb-2 and PLCγ-1, consistent with the proposed functions of pp36.
General Literature References
GRB2 and phospholipase C-gamma 1 associate with a 36- to 38-kilodalton phosphotyrosine protein after T-cell receptor stimulation
:
M. Sieh, et al.; Mol. Cell. Biol.
14
, 4435 (1994)
Abstract
Killer cell inhibitory receptor recognition of human leukocyte antigen (HLA) class I blocks formation of a pp36/PLC-gamma signaling complex in human natural killer (NK) cells
:
N.M. Valiante, et al.; J. Exp. Med.
184
, 2243 (1996)
Abstract
Impaired plasma membrane targeting of Grb2-murine son of sevenless (mSOS) complex and differential activation of the Fyn-T cell receptor (TCR)-zeta-Cbl pathway mediate T cell hyporesponsiveness in autoimmune nonobese diabetic mice K. Salojin, et al.; J. Exp. Med.
186
, 887 (1997)
Abstract
;
Full Text
CD16-mediated activation of phosphatidylinositol-3 kinase (PI-3K) in human NK cells involves tyrosine phosphorylation of Cbl and its association with Grb2, Shc, pp36 and p85 PI-3K subunit
:
C. Cerboni, et al.; Eur. J. Immunol.
28
, 1005 (1998)
Abstract
Molecular cloning of the cDNA encoding pp36, a tyrosine-phosphorylated adaptor protein selectively expressed by T cells and natural killer cells
:
J.R. Weber, et al.; J. Exp. Med.
187
, 1157 (1998)
Abstract
;
Full Text
Copresentation of natural HIV-1 agonist and antagonist ligands fails to induce the T cell receptor signaling cascade
:
M.A. Purbhoo, et al.; PNAS
95
, 4527 (1998)
Abstract
;
Full Text
Further Categories Containing This Product:
Adaptor Proteins in T Cell Signal Transduction / Related Products
•
Polyclonal Antibodies
ALX-270-038
Revised 03-Jan-08
LY-294,002
SYNONYMS
2-(4-Morpholinyl)-8-phenyl-4
H
-1-benzopyran-4-one
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
Product Numbers:
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ALX-270-038-M001
1 mg
30.00 USD
ALX-270-038-M005
5 mg
50.00 USD
ALX-270-038-M025
25 mg
245.00 USD
Product Specification
FORMULA:
C
19
H
17
NO
3
MW:
307.4
CAS NUMBER:
154447-36-6
PURITY:
≥99%
APPEARANCE:
White to off-white crystalline solid.
SOLUBILITY:
Soluble in DMSO, 100% ethanol or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Potent, cell permeable, highly specific inhibitor of PI(3)K (phosphoinositide 3-kinase) that acts on the ATP-binding site of the enzyme. Sensitizes tumor cells to drug-induced apoptosis independent of its PI3K inhibitory activity. For a negative control see LY-303,511 (Prod. No.
ALX-270-410
).
Product Specific Literature References
A specific inhibitor of phosphatidylinositol 3-kinase, 2-(4- morpholinyl)-8-phenyl-4H-1-benzopyran-4-one (LY294002):
C.J. Vlahos, et al.; J. Biol. Chem.
269
, 5241 (1994)
Abstract
;
Full Text
Investigation of neutrophil signal transduction using a specific inhibitor of phosphatidylinositol 3-kinase:
C.J. Vlahos, et al.; J. Immunol.
154
, 2413 (1995)
Abstract
LY294002 and LY303511 Sensitize Tumor Cells to Drug-Induced Apoptosis via Intracellular Hydrogen Peroxide Production Independent of the Phosphoinositide 3-Kinase-Akt Pathway:
T.W. Poh and S. Pervaiz; Cancer Res.
65
, 6264 (2005)
Abstract
Related Products
ALX-270-410
LY-303,511
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
ALX-270-292
Revised 09-Feb-05
1L-6-Hydroxymethyl-chiro-inositol-2-[(R)-2-O-methyl-3-O-octadecylcarbonate]
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-270-292-M001
1 mg
85.00 USD
ALX-270-292-M005
5 mg
330.00 USD
Product Specification
FORMULA:
C
30
H
58
O
10
MW:
578.8
PURITY:
>98%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Keep cool and dry.
Product Description
Potent inhibitor of Akt (PKB) (IC
50
=2.0µM). Weak inhibitor of PI(3)K (phosphoinositide 3-kinase) (IC
50
=83µM). Has been shown to inhibit the growth of the following cancer cell lines: HeLa (IC
50
=2.5µM), HT-29 (IC
50
=10µM), MCF-7 (IC
50
=1.2µM) and PC-3 (IC
50
=2.0µM).
Product Specific Literature References
3-(Hydroxymethyl)-bearing phosphatidylinositol ether lipid analogues and carbonate surrogates block PI3-K, Akt, and cancer cell growth:
Y. Hu, et al.; J. Med. Chem.
43
, 3045 (2000)
Abstract
Further Categories Containing This Product:
Protein Kinase Inhibitors Other Products
•
Akt [PKB] / Related Products
•
Antitumor Agents (Enzyme Inhibitors)
ALX-270-410
Revised 05-Sep-08
LY-303,511
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-410-M001
1 mg
60.00 USD
ALX-270-410-M005
5 mg
240.00 USD
Product Specification
FORMULA:
C
19
H
18
N
2
O
2
MW:
306.4
CAS NUMBER:
154447-38-8
PURITY:
≥98% (NMR)
APPEARANCE:
Yellow solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
SHORT TERM STORAGE:
+4°C
LONG TERM STORAGE:
-20°C
Product Description
Useful negative control for the PI(3)K (phosphoinositide 3-kinase) inhibitor LY-294,002 (Prod. No.
ALX-270-038
). Does not inhibit PI(3)K even at concentrations ≥100µM (LY-294,002: IC
50
=1.4µM). Sensitizes tumor cells to drug-induced apoptosis independent of its PI3K inhibitory activity.
Product Specific Literature References
Antagonists of phosphatidylinositol 3-kinase block activation of several novel protein kinases in neutrophils
:
J. Ding, et al.; J. Biol. Chem.
270
, 11684 (1995)
Abstract
;
Full Text
LY294002 and LY303511 Sensitize Tumor Cells to Drug-Induced Apoptosis via Intracellular Hydrogen Peroxide Production Independent of the Phosphoinositide 3-Kinase-Akt Pathway:
T.W. Poh and S. Pervaiz; Cancer Res.
65
, 6264 (2005)
Abstract
Related Products
ALX-270-038
LY-294,002
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
ALX-270-454
Revised 26-Mar-07
ZSTK474
SYNONYMS
2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Phosphoinositide 3-kinase [PI(3)K] / Related Products
Ordering Information
not sold in USA
Product Specification
FORMULA:
C
19
H
21
F
2
N
7
O
2
MW:
417.4
CAS NUMBER:
475110-96-4
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING:
Protect from light.
HAZARD:
IRRITANT.
Product Description
Cell permeable, reversible, potent and specific inhibitor of phosphoinositide 3-kinase (IC
50
=17nM for PI(3)K p110β, IC
50
=53nM for PI(3)K p110γ and IC
50
=6nM for PI(3)K p110δ). Blocks cellular PI(3)K/Akt (PKB) signalling
in vitro
and inhibits Akt(PKB)-dependent tumor growth in mice
in vivo
without significant toxic effect. More effective than LY 294,002 (Prod. No.
ALX-270-038
)
in vitro
and
as
in vivo
.
Product Specific Literature References
A novel phosphatidylinositol 3-kinase inhibitor, ZSTK474 exerted antitumor activity against human tumor xenografts by oral administration:
S.Yaguchi et al.; Proc. Am. Assoc. Cancer Res.
46
, 1691 (2005)
Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor:
S. Yaguchi, et al.; J. Natl. Cancer Inst.
98
, 545 (2006)
Abstract
Related Products
ALX-270-038
LY-294,002
Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other Products
•
Antitumor Agents (Anti-proliferative)
ALX-270-455
Revised 18-Dec-06
Compound 15e