TGX-221

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TGX-221

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Cat No: 10007349

Biochemicals - Kinase Inhibitors

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3.{8039,12235,13740} Class 1 PI3Ks...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

7-methyl-2-(4-morpholinyl)-9-[1-(phenylamino)ethyl]-4H-pyrido[1,2-a]pyrimidin-4-one

Correlated keywords:

phosphatidylinositol-3-kinases PI3K catalyzes phosphorylation produces second messengers (3,4)-biphosphates -P2 (3,4,5)-P3 Class 1 p110.alpha. .beta. .delta. .gamma. p85 regulatory subunits cells permeable inhibitors inhibition inhibits ATP binding sites platelets defective thrombus formation antithrombotic therapy atherosclerosis

Product Overview:
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of phosphatidylinositol at the 3 position to produce the second messengers phosphatidylinositol-3,4-bisphosphate (PtdIns-(3,4)-P2) and PtdIns-(3,4,5)-P3.{8039,12235,13740} Class 1 PI3Ks are composed of a p110 catalytic subunit, of which there are 4 isoforms (p110α, p110β, p110δ, and p100γ), and a p85 regulatory subunit.{13740} TGX-221 is a potent, selective, and cell permeable inhibitor of PI3K p110β.{13192} Inhibition appears to occur at the ATP binding site based on the observed increase in IC50 value from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively. TGX-221 inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM.{13192} Selective inhibition of PI3K p110β results in defective platelet thrombus formation and defines PI3K as a target for antithrombotic therapy.{13192}

Size	500 µg
Shipping	dry ice
CAS Number	663619-89-4
Molecular Formula	C₂₁H₂₄N₄O₂
SMILES	CC(C=C1C(NC2=CC=CC=C2)C)=CN3C1=NC(N4CCOCC4)=CC3=O
Molecular Weight	364,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.59
UNSPSC code	12352100

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Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

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