A selective inhibitor of p110α with an IC50 value of 5.8 nM; inhibits p110γ and p110β with IC50 values of 0.076 µM and 1.3 µM

PIK-75 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
372196-77-5
Storage:
-20
UN-No:
Non-Hazardous - /

Phosphatidylinositol 3-kinase (PI3K) catalyzes the synthesis of the second messengers PtdIns-(3)-P, PtdIns-(3,4)-P2, and PtdIns-(3,4,5)-P3. The PI3K family of enzymes is comprised of 15 members that are divided into three classes according to their structure, substrate specificity, and mode of regulation.{14311} In the class I PI3Ks, p110α is the primary PI3K isoform required for insulin signaling in adipocytes and myotubes and is frequently mutated in primary tumors.{14312} Small molecule inhibitors of p110α are of interest in cancer treatment research. PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.{14312} It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 µM and 1.3 µM, respectively.{14312} In adipocytes and myotubes, PIK-75 blocks production of PIP2 and/or PIP3, phosphorylation of Akt, and activation of mTORC1.{14312}  

 

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SKU: 10009210 - 1 mg Category:

Description

A selective inhibitor of p110α with an IC50 value of 5.8 nM; inhibits p110γ and p110β with IC50 values of 0.076 µM and 1.3 µM, respectively

Formal name: 2-methyl-5-nitro-2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide-benzenesulfonic acid, monohydrochloride

Synonyms: 

Molecular weight: 488.7

CAS: 372196-77-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling

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