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Phosphoinositide 3-kinase [PI(3)K] / Related Products
You are here: Product Lines > Signal Transduction > PI(3)K-Akt-mTOR Pathway > Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-151-026 Revised 20-Jun-08
N-Acetyl-Asp-Tyr(2-malonyl)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-026-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C39H57N7O14S
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
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PeptidesPhosphoinositide 3-kinase [PI(3)K] / Related Products
 
 
ALX-151-027 Revised 17-Jan-05
N-Acetyl-Asp-Tyr(PO3H2)-Val-Pro-Met-Leu-NH2
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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ALX-151-027-M001   1 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C36H57N7O13SP
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
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PeptidesPhosphoinositide 3-kinase [PI(3)K] / Related Products
 
 
ALX-201-055 Revised 17-Apr-07
Phosphoinositide 3-kinase p110γ (human) (recombinant)
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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 Add To Cart
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 MgCl2; 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 32P-ATP.
- Reaction was started by addition of the 32P-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 32P 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 32P-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:
EnzymesRecombinant Proteins / Fusion Proteins
 
 
ALX-201-119 Revised 01-Mar-05
Phosphoinositide 3-kinase p110α/p85 (bovine) (recombinant)
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SYNONYMS PI(3)K p110α/p85 (bovine) (recombinant)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-201-119-C005   5 µg 440.00 USD Add To Cart
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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:
EnzymesRecombinant Proteins / Fusion Proteins
 
 
ALX-210-747 Revised 18-Sep-08
Polyclonal Antibody to Phosphoinositide 3-kinase p110δ (human)
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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 Add To Cart
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 (S1026WKTKVNWLAHNVSKDNRQ1044) 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
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Polyclonal Antibodies
 
 
ALX-210-770 Revised 11-Apr-06
Polyclonal Antibody to pp36 (human)
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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 Add To Cart
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 (C29HRLPGSYDSTSSDSLYPRGI49) 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
 
 
ALX-270-038 Revised 03-Jan-08
LY-294,002
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SYNONYMS 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-038-M001   1 mg 30.00 USD Add To Cart
ALX-270-038-M005   5 mg 50.00 USD Add To Cart
ALX-270-038-M025   25 mg 245.00 USD Add To Cart
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Product Specification
FORMULA: C19H17NO3
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
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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]
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-292-M001   1 mg 85.00 USD Add To Cart
ALX-270-292-M005   5 mg 330.00 USD Add To Cart
Product Specification
FORMULA: C30H58O10
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) (IC50=2.0µM). Weak inhibitor of PI(3)K (phosphoinositide 3-kinase) (IC50=83µM). Has been shown to inhibit the growth of the following cancer cell lines: HeLa (IC50=2.5µM), HT-29 (IC50=10µM), MCF-7 (IC50=1.2µM) and PC-3 (IC50=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
 
 
ALX-270-410 Revised 05-Sep-08
LY-303,511
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-410-M001   1 mg 60.00 USD Add To Cart
ALX-270-410-M005   5 mg 240.00 USD Add To Cart
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Product Specification
FORMULA: C19H18N2O2
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: IC50=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
Further Categories Containing This Product:
Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-454 Revised 26-Mar-07
ZSTK474
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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
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not sold in USA
Product Specification
FORMULA: C19H21F2N7O2
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 (IC50=17nM for PI(3)K p110β, IC50=53nM for PI(3)K p110γ and IC50=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-270-038in 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
Further Categories Containing This Product:
PI(3)K-Akt-mTOR Pathway Other ProductsAntitumor Agents (Anti-proliferative)
 
 
ALX-270-455 Revised 18-Dec-06
Compound 15e