A potent

TGX-221 – 10 mg

Brand:
Cayman
CAS:
663619-89-4
Storage:
-20
UN-No:
Non-Hazardous - /

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}  

 

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SKU: 10007349 - 10 mg Category:

Description

A potent, selective, and cell permable inhibitor of PI3K p110b; IC50 value increases from 5 to ~50 nM at ATP concentrations of 50 µM and 1 mM, respectively; inhibits PtdIns-(3,4)-P2 production in platelets with an IC50 value of 50 nM

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

Synonyms: 

Molecular weight: 364.4

CAS: 663619-89-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Blood|Coagulation & Hemostasis||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling

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