PI3Kα-IN-28

PI3Kα-IN-28 is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 (IC50 = 1.46 µM) and KYSE450 (IC50 = 0.57 µM) cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer[1].

Product Specifications

CAS Number

[3095278-75-1]

UNSPSC

12352005

Target

Akt; AMPK; c-Myc; DNA/RNA Synthesis; Epigenetic Reader Domain; PI3K

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; PI3K/Akt/mTOR

Field of Research

Cancer

Smiles

CC1=C2C(C(OC3CCN(CC3)CC4CCN(CC4)C(C[C@@H]5N=C(C6=C(N7C5=NN=C7C)SC(C)=C6C)C8=CC=C(C=C8)Cl)=O)=CC(C9=CC(NS(C%10=CC=C(C=C%10F)F)(=O)=O)=C(N=C9)OC)=C2)=NC=N1

Molecular Formula

C51H51ClF2N10O5S2

Molecular Weight

1021.59

References & Citations

[1]Peng S, et al. Discovery of Novel PI3K/BRD4 Dual Inhibitors for Esophageal Cancer: Rational Design, Optimization, and Senescence-Inducing Mechanisms. J Med Chem. 2025 Oct 20.