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PI(3)K-Akt-mTOR Pathway
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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
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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:
Enzymes • Recombinant Proteins / Fusion Proteins
 
 
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.
- Lipids 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:
Recombinant Proteins / Fusion Proteins • Enzymes
 
 
ALX-270-460 Revised 04-Sep-07
PI-103
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SYNONYMS 3-(4-(4-Morpholinyl)pyrido[3’,2’:4,5]furo[3,2-d]pyrimidin-2-yl)phenol
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Phosphoinositide 3-kinase [PI(3)K] / Related Products
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ALX-270-460-M001   1 mg 70.00 USD Add To Cart
ALX-270-460-M005   5 mg 280.00 USD Add To Cart
ALX-270-460-M025   25 mg 980.00 USD Add To Cart
Product Specification
FORMULA: C19H16N4O3
MW: 348.4
CAS NUMBER: 371935-74-9
PURITY: ≥97% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO (5mg/ml; warm).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY:

Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light. After reconstitution, prepare aliquots and store at -20°C.

Product Description
Potent, cell permeable and ATP-competitive inhibitor of DNA-PK, phosphoinositide 3-kinase (PI(3)K), the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. Exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10µM. Effectively blocks cell proliferation in glioma cell lines both in vitro and in vivo.
Product Specific Literature References
A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma: Q.W. Fan, et al.; Cancer Cell 9, 341 (2006) Abstract
A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling: Z.A. Knight, et al.; Cell 125, 733 (2006) Abstract
Further Categories Containing This Product:
Mammalian Target of Rapamycin [mTOR] / Related Products
 
 
ALX-380-281 Revised 20-Jun-08
PKC412
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SYNONYMS 4’-N-Benzoyl-staurosporine
Midostaurin
CGP 41251
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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ALX-380-281-M001   1 mg 60.00 USD Add To Cart
ALX-380-281-M005   5 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C35H30N4O4
MW: 570.6
CAS NUMBER: 120685-11-2
MERCK INDEX: 14: 6185
SOURCE/HOST: Semisynthetic product prepared from staurosporine (a fermentation product of Streptomyces staurosporeus) (Prod. No. ALX-380-014).
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO (10mg/ml), MDC (10mg/ml) or methanol (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Inhibitor of a variety of serine/threonine and tyrosine kinases, like protein kinase C (PKC), cyclic AMP-dependent protein kinase (PKA), S6 kinase, Akt (protein kinase B; PKB) and epidermal growth factor receptor (EGFR) tyrosine kinase activity. Potently inhibits FLT-3 kinase in vitro and in vivo. Apoptosis inducer. Showed broad antiproliferative activity against various tumor cell lines. Selectively inhibits T lymphocyte production of TNF-α. Upregulates endothelial nitric oxide synthase (eNOS; NOS III).
Product Specific Literature References
Differential inhibition of the epidermal growth factor-, platelet-derived growth factor-, and protein kinase C-mediated signal transduction pathways by the staurosporine derivative CGP 41251: E. Andrejauskas-Buchdunger & U. Regenass; Cancer Res. 52, 5353 (1992) Abstract; Full Text
Analogs of staurosporine: potential anticancer drugs?: A. Gescher; Gen. Pharmacol. 31, 721 (1998), (Review) Abstract
Differential effects of UCN-01, staurosporine and CGP 41 251 on cell cycle progression and CDC2/cyclin B1 regulation in A431 cells synchronized at M phase by nocodazole: T. Akiyama, et al.; Anticancer Drugs 10, 67 (1999) Abstract
Inhibitors of protein kinases: CGP 41251, a protein kinase inhibitor with potential as an anticancer agent: D. Fabbro, et al.; Pharmacol. Ther. 82, 293 (1999) Abstract
The phosphatidylinositide 3’-kinase/Akt survival pathway is a target for the anticancer and radiosensitizing agent PKC412, an inhibitor of protein kinase C: A. Tenzer, et al.; Cancer Res. 61, 8203 (2001) Abstract; Full Text
Phase I and pharmacokinetic study of PKC412, an inhibitor of protein kinase C: D.J. Propper, et al.; J. Clin. Oncol. 19, 1485 (2001) Abstract; Full Text
A protein kinase C inhibitor induces phenotypic reversion of ras-transformed pancreatic cancer cells and cooperatively blocks tumor cell proliferation with an anti- ras peptide.: D. Way, et al.; Cancer Chemother. Pharmacol. 49, 429 (2002) Abstract
Protein kinase C inhibitors: H.C. Swannie & S.B. Kaye; Curr. Oncol. Rep. 4, 37 (2002), (Review) Abstract
PKC412 inhibits the zinc finger 198-fibroblast growth factor receptor 1 fusion tyrosine kinase and is active in treatment of stem cell myeloproliferative disorder: J. Chen, et al.; PNAS 101, 14479 (2004) Abstract; Full Text
Cotreatment with 17-allylamino-demethoxygeldanamycin and FLT-3 kinase inhibitor PKC412 is highly effective against human acute myelogenous leukemia cells with mutant FLT-3: P. George, et al.; Cancer Res. 64, 3645 (2004) Abstract; Full Text
Effects of the kinase inhibitor CGP41251 (PKC 412) on lymphocyte activation and TNF-alpha production: M.S. Si, et al.; Int. Immunopharmacol. 5, 1141 (2005) Abstract
N-Benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells.: N.J. Bahlis, et al.; Leuk. Lymphoma 46, 899 (2005) Abstract
Midostaurin upregulates eNOS gene expression and preserves eNOS function in the microcirculation of the mouse: H. Li, et al.; Nitric Oxide 12, 231 (2005) Abstract
Inhibitors of the PI3-kinase/Akt pathway induce mitotic catastrophe in non-small cell lung cancer cells: T.H. Hemström, et al.; Int. J. Cancer 119, 1028 (2006) Abstract
Antitumor and normal cell protective effect of PKC412 in the athymic mouse model of ovarian cancer: M. Kim, et al.; Ann. Clin. Lab. Sci. 36, 455 (2006) Abstract
PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects.: K.V. Gleixner, et al.; Blood 107, 752 (2006) Abstract; Full Text
Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT: K.V. Gleixner, et al.; Haematologica 92, 1451 (2007) Abstract; Full Text
PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer: J. El Fitori, et al.; Cancer 110, 1457 (2007) Abstract
PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.7 macrophages: K. Miyatake, et al.; BBRC 360, 115 (2007) Abstract
Divergent cytotoxic effects of PKC412 in combination with conventional antileukemic agents in FLT3 mutation-positive versus -negative leukemia cell lines.: Y. Furukawa, et al.; Leukemia 21, 1005 (2007) Abstract
PKC412 demonstrates JNK-dependent activity against human multiple myeloma cells: J. Sharkey, et al.; Blood 109, 1712 (2007) Abstract
The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations: T. Odgerel, et al.; Oncogene 27, 3102 (2008) Abstract
The FLT3 inhibitor PKC412 in combination with cytostatic drugs in vitro in acute myeloid leukemia: L. Möllgard, et al.; Cancer Chemother. Pharmacol. 62, 439 (2008) Abstract
Related Products
Further Categories Containing This Product:
PKA Inhibitors • PKC Inhibitors • Akt [PKB] / Related Products • EGFR Kinase Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • Antitumor Agents (Anti-proliferative) • Natural Products - Apoptosis Inducers & Inhibitors • NOS Cofactors & Activators
 
 
ALX-210-226 Revised 17-Dec-07
Polyclonal Antibody to Akt
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SYNONYMS anti-PKB PAb
anti-Protein Kinase B PAb
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Akt [PKB] / Related Products
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ALX-210-226-C200   200 µg 379.00 USD Add To Cart
Product Specification
SPECIES CROSSREACTIVITY:
Human
Mouse
Rat
SOURCE/HOST: From rabbit.
CONCENTRATION: 1mg/ml.
PURITY DETAIL: Epitope-affinity purified IgG.
FORMULATION: Liquid. In PBS containing 1mg/ml BSA and 0.05% sodium azide.
IMMUNOGEN: Synthetic phosphopeptide corresponding to aa 302-314 (D302GATMKTpFCGTPE314) of mouse Akt (protein kinase B; PKB).
SPECIFICITY: Recognizes the phosphorylated and non-phosphorylated form of human, mouse, rat and drosophila Akt. Detects a band of ~55kDa by Western blot.
APPLICATION: Western Blot (10µg/ml)
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
BLOCKING PEPTIDE: For Blocking Peptide see Prod. No. ALX-165-039.
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Further Categories Containing This Product:
Polyclonal Antibodies
 
 
ALX-210-534 Revised 27-Dec-06
Polyclonal Antibody to Akt (mouse)
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SYNONYMS anti-PKB (mouse) PAb
anti-Protein Kinase B (mouse) PAb
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Akt [PKB] / Related Products
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ALX-210-534-R100   100 µl 220.00 USD Add To Cart
Product Specification
SPECIES CROSSREACTIVITY:
Human
SOURCE/HOST: From rabbit.
PURITY: Liquid. Neat serum containing 0.05% sodium azide.
IMMUNOGEN: Recombinant mouse Akt (protein kinase B; PKB).
SPECIFICITY: Recognizes mouse Akt. Does not cross-react with other species.
APPLICATION: ELISA
Immunoprecipitation (5µl/700µl protein extracts)
Western Blot
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
Further Categories Containing This Product:
Phospho-specific Antibodies • Polyclonal Antibodies
 
 
ALX-210-142 Revised 12-Jun-06
Polyclonal Antibody to FKBP12
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SYNONYMS anti-FK506 Binding Protein (12kDa) PAb
PRODUCT LINE Immunology
PRODUCT CATEGORY Immunophilins / Related Products
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ALX-210-142-R100   100 µl 379.00 USD Add To Cart
Product Specification
SPECIES CROSSREACTIVITY:
Human
Mouse
Rat
SOURCE/HOST: From rabbit.
CONCENTRATION: 1mg/ml.
PURITY DETAIL: Epitope-affinity purified IgG.
FORMULATION: Liquid. In PBS containing 1mg/ml BSA and 0.05% sodium azide.
IMMUNOGEN: Synthetic peptide corresponding to aa 1-13 (G1VQVETISPGDGR13) of human FKBP12 (FK506 binding protein 12kDa).
SPECIFICITY: Recognizes human, mouse and rat FKBP12. Detects a band of ~12kDa by Western blot.
APPLICATION: Immunohistochemistry (frozen sections (2µg/ml); paraffin sections)
Immunoprecipitation
Western Blot (1µg/ml)
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
BLOCKING PEPTIDE: For Blocking Peptide see Prod. No. ALX-156-002.
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Product Specific Literature References
The effects of FK506 on retinal ganglion cells after optic nerve crush: E.E. Freeman and C.L. Grosskreutz; IOVS 41, 1111 (2000) Abstract
Immunophilin expression in the HIV-infected brain: C.L. Achim, et al.; J. Neuroimmunol. 157, 126 (2004) Abstract
Related Products
Further Categories Containing This Product:
Mammalian Target of Rapamycin [mTOR] / Related Products • Polyclonal Antibodies
 
 
ALX-210-115/1 Revised 10-Oct-07
Polyclonal Antibody to Inositol 1,4,5-trisphosphate Receptor (Type-I)
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SYNONYMS anti-IP3 Receptor (Type-I) PAb
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Inositols & Inositolphosphates / Related Products
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ALX-210-115/1-R100   100 µl 379.00 USD Add To Cart
Product Specification
SPECIES CROSSREACTIVITY:
Mouse
Rat
SOURCE/HOST: From rabbit.
FORMULATION: Liquid. In PBS containing 0.05% sodium azide.
IMMUNOGEN: Synthetic peptide corresponding to aa 1829-1848(N1829KKKDD
EVDRDAPSRKKAKE1848) of the cytoplasmic C-terminal domain of human IP3R-I (inositol 1,4,5-trisphosphate receptor (type-I)). This sequence is completely conserved in mouse and rat IP3R-I.
SPECIFICITY: Recognizes mouse and rat IP3R-I. Detects a band of ~240-260kDa by Western blot.
APPLICATION: Immunohistochemistry (not tested yet)
Immunoprecipitation (not tested yet)
Western Blot
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
BLOCKING PEPTIDE: For Blocking Peptide see Prod. No. ALX-159-003.
Related Products
Further Categories Containing This Product:
Polyclonal Antibodies
 
 
ALX-210-169 Revised 10-Oct-07
Polyclonal Antibody to Inositol 1,4,5-trisphosphate Receptor (Type-I)
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SYNONYMS anti-IP3 Receptor (Type-I) PAb
anti-IP3R-I PAb
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Inositols & Inositolphosphates / Related Products
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-210-169-R100   100 µl 379.00 USD Add To Cart
Product Specification
SPECIES CROSSREACTIVITY:
Mouse
Rat
Dog
SOURCE/HOST: From rabbit.
PURITY DETAIL: Epitope-affinity purified IgG.
FORMULATION: Liquid. In PBS containing 1mg/ml BSA and 0.05% sodium azide.
IMMUNOGEN: Synthetic peptide corresponding to aa 1829-1848 N1829KKKDDEVDRDAPSRKKAKE1848) of the cytoplasmic C-terminal domain of human IP3R-I (inositol 1,4,5-triphosphate receptor (type-I)). This sequence is completely conserved in mouse and rat IP3R-I.
SPECIFICITY: Recognizes human (weak), mouse, rat and dog IP3R-I. Detects a band of ~240kDa by Western blot.
APPLICATION: Immunohistochemistry (1:250)
Immunoprecipitation
Western Blot (1:1’000)
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Avoid freeze/thaw cycles.
BLOCKING PEPTIDE: For Blocking Peptide see Prod. No. ALX-159-003.
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Further Categories Containing This Product:
Polyclonal Antibodies
 
 
ALX-210-224 Revised 10-Mar-06
Polyclonal Antibody to Inositol 1,4,5-trisphosphate Receptor (Type-II)
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SYNONYMS anti-IP3 Receptor (Type-II) PAb
PRODUCT LINE