Name: PI3-Kinase α Inhibitor 2
Rating: 5 (10 reviews)

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HIT ID:HIT214320654
Cas No:371943-05-4
常用名:PI3-Kinase α Inhibitor 2
别名:PI3-Kinase α Inhibitor 2
IUPAC:3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol
IUPAC:3-[4-(morpholin-4-yl)thieno[3,2-d]pyrimidin-2-yl]phenol
InChI key:XXLAEKOWCYJOKK-UHFFFAOYSA-N

分子式:C16H15N3O2S
分子量:313.38
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:Oc1cccc(c1)-c1nc(N2CCOCC2)c2sccc2n1
SMILES:Oc1cccc(c1)-c1nc(N2CCOCC2)c2sccc2n1

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

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