PI3K/HDAC-IN-2
Names
[ CAS No. ]:
2361418-65-5
[ Name ]:
PI3K/HDAC-IN-2
Biological Activity
[Description]:
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects[1].
[Related Catalog]:
[Target]
PI3Kα:226 nM (IC50)
PI3Kβ:279 nM (IC50)
PI3Kγ:467 nM (IC50)
PI3Kδ:29 nM (IC50)
HDAC1:1.3 nM (IC50)
HDAC2:3.4 nM (IC50)
HDAC4:972 nM (IC50)
HDAC6:17 nM (IC50)
HDAC8:12 nM (IC50)
[In Vitro]
For PI3K/HDAC-IN-2 (Compound 8), the IC50 values in the growth inhibition assay against MDA-MB-453, HCT116 and HGC-27 cells are as low as namomolar level, which are 4 nM, 7 nM and 14 nM respectively[1]. PI3K/HDAC-IN-2 (Compound 8) shows antiproliferative activities against 16 DLBCL cell lines with IC50s of 3.6-21 nM[1].
[In Vivo]
In the zebrafish xenograft model of SU-DHL-4 cells, PI3K/HDAC-IN-2 (Compound 8) exhibits in vivo growth inhibitory activity at 3 μM[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C23H23N7O4
[ Molecular Weight ]:
461.47