PI3Kδ/HDAC6-IN-1

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3[1].

Product Specifications

CAS Number

[3075011-99-0]

UNSPSC

12352005

Target

Apoptosis; Bcl-2 Family; Caspase; HDAC; Histone Methyltransferase; Microtubule/Tubulin; PI3K; Reactive Oxygen Species (ROS)

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

CCC(N1C2=NC(N(C)C(CN3C(CN(CC4=CC=C(/C=C/C(NO)=O)C=C4)CC3)=O)=N5)=C5C(N6CCOCC6)=N2)=NC7=C1C=CC=C7

Molecular Formula

C34H38N10O4

Molecular Weight

650.73

References & Citations

[1]Zuo Y, et al. Design, synthesis, and biological evaluation of novel PI3Kδ/HDAC6 dual inhibitors for the treatment of non-Hodgkin's lymphoma. Eur J Med Chem. 2025 Oct 15;296:117852.