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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-270-464 Revised 13-Jun-07
TGX-221
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SYNONYMS 7-Methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido-[1,2-a]pyrimidin-4-one
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-270-464-C100   100 µg 75.00 USD Add To Cart
ALX-270-464-M001   1 mg 580.00 USD Add To Cart
Product Specification
FORMULA: C21H24N4O2
MW: 364.4
CAS NUMBER: 663619-89-4
PURITY: ≥98% (NMR)
APPEARANCE: Pale yellow solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C

Product Description
Potent, selective and cell permeable inhibitor of phosphoinositide 3-kinase (PI(3)K) p110β.
Product Specific Literature References
Sequential activation of class IB and class IA PI3K is important for the primed respiratory burst of human but not murine neutrophils: A.M. Condliffe, et al.; Blood 106, 1432 (2005) Abstract; Full Text
PI 3-kinase p110beta: a new target for antithrombotic therapy: S.P. Jackson, et al.; Nat. Med. 11, 507 (2005) Abstract; Full Text
 
 
ALX-350-020 Revised 27-Aug-08
Wortmannin
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SYNONYMS KY 12420
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-020-M001   1 mg 40.00 USD Add To Cart
ALX-350-020-M005   5 mg 140.00 USD Add To Cart
ALX-350-020-M025   25 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C23H24O8
MW: 428.4
CAS NUMBER: 19545-26-7
MERCK INDEX: 14: 10053
RTECS: CB9641000
SOURCE/HOST: Isolated from Talaromyces wortmannin KY 12420.
PURITY: ≥96% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (25mg/ml), methanol (5mg/ml) or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.

Product Description
Potent and specific inhibitor of  phosphoinositide 3-kinase (PI(3)K), myosin light chain kinase and of neutrophil and formyl-Met-Leu-Phe-mediated phospholipase D activation. Strongly inhibits autophagy (proteolysis). Markedly potentiates the LPS-induced nitric oxide (NO) production from macrophages. Induces in vivo Alzheimer-like hyperphosphorylation in tau.
Product Specific Literature References
Activation of human neutrophil phospholipase D by three separable mechanisms: S.I. Reinhold, et al.; FASEB J. 4, 208 (1990) Abstract
Demethoxyviridin and wortmannin block phospholipase C and D activation in the human neutrophil: R.W. Bonser, et al.; Br. J. Pharmacol. 103, 1237 (1991) Abstract
Inhibition of IgE-mediated histamine release by myosin light chain kinase inhibitors: S. Kitani, et al.; BBRC 183, 48 (1992) Abstract
Wortmannin, a microbial product inhibitor of myosin light chain kinase: S. Nakanishi, et al.; J. Biol. Chem. 267, 2157 (1992) Abstract; Full Text
Wortmannin is a potent phosphatidylinositol 3-kinase inhibitor: the role of phosphatidylinositol 3,4,5-trisphosphate in neutrophil responses: A. Arcaro & M.P. Wyman; Biochem. J. 296, 297 (1993) Abstract
Inhibition of histamine secretion by wortmannin through the blockade of phosphatidylinositol 3-kinase in RBL-2H3 cells: H. Yano, et al.; J. Biol. Chem. 268, 25846 (1993) Abstract; Full Text
Effects of wortmannin on increased glucose transport by insulin and norepinephrine in primary culture of brown adipocytes: Y. Shimizu & T. Shimazu; BBRC 202, 660 (1994) Abstract
A comparison of demethoxyviridin and wortmannin as inhibitors of phosphatidylinositol 3-kinase: R. Woscholski, et al.; FEBS Lett. 342, 109 (1994) Abstract
Wortmannin inhibits insulin-stimulated but not contraction-stimulated glucose transport activity in skeletal muscle: A.D. Lee, et al.; FEBS Lett. 361, 51 (1995) Abstract
Wortmannin, a specific inhibitor of phosphatidylinositol-3 kinase, blocks osteoclastic bone resorption: I. Nakamura, et al.; FEBS Lett. 361, 79 (1995) Abstract
Wortmannin, a specific phosphatidylinositol 3-kinase inhibitor, inhibits adipocytic differentiation of 3T3-L1 cells: K. Tomiyama, et al.; BBRC 212, 263 (1995) Abstract
Wortmannin as a unique probe for an intracellular signalling protein, phosphoinositide 3-kinase: M. Ui, et al.; TIBS 20, 303 (1995), (Review) Abstract
Wortmannin inhibits carcinogen-stimulated phosphorylation of ethanolamine and choline: Z. Kiss & M. Tomono; FEBS Lett. 358, 243 (1995) Abstract
Inhibitory effect of wortmannin on phosphatidylinositol 3-kinase-mediated cellular events: O. Hazeki, et al.; J. Lipid Mediat. Cell Signal. 14, 259 (1996)
The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes: E.F. Blommaart, et al.; Eur. J. Biochem. 243, 240 (1997) Abstract
Wortmannin, a specific inhibitor of phosphatidylinositol-3-kinase, enhances LPS-induced NO production from murine peritoneal macrophages: Y.C. Park, et al.; BBRC 240, 692 (1997) Abstract
Alzheimer-like tau phosphorylation induced by wortmannin in vivo and its attenuation by melatonin: S.J. Liu & J.Z. Wang; Acta Pharmacol. Sin. 23, 183 (2002) Abstract
Chemistry and biology of wortmannin: P. Wipf & R.J. Halter; Org. Biomol. Chem. 3, 2053 (2005) Abstract
 
 
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
Ordering Information
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)
 
 

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