PI3Kα/HDAC6-IN-1

PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC50 of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT (Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC50=0.17 μM) and has good anti-cancer activity[1].

Product Specifications

CAS Number

[3007565-26-3]

UNSPSC

12352005

Target

HDAC; PI3K

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pi3kα-hdac6-in-1.html

Solubility

10 mM in DMSO

Smiles

CC(C(F)(F)F)(C)C1=CC(C2=C(C)N=C(NC(N3C[C@H](NS(=O)(CC4=CC=C(C(NO)=O)C=C4)=O)C[C@H]3C(N)=O)=O)S2)=CC=N1

Molecular Formula

C27H30F3N7O6S2

Molecular Weight

669.70

References & Citations

[1]Zhang Y, et al. Discovery of (S) -N1- (thiazol-2-yl) pyrrolidine-1,2-dicarboxamide derivatives targeting PI3Ka/HDAC6 for the treatment of cancer. Bioorg Med Chem Lett. 2023 Oct 1;94:129462.. .