CBP/p300-IN-10

Names

[ CAS No. ]:
2259641-71-7

[ Name ]:
CBP/p300-IN-10

Biological Activity

[Description]:

CBP/p300-IN-10 is a highly potent histone acetyltransferase EP300 and CREBBP with IC50 values of 26 nM and 39 nM, respectively. CBP/p300-IN-10 can be used to research anticancer[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

[Target]

EP300:26 nM (IC50)

CREBBP:39 nM (IC50)


[In Vitro]

CBP/p300-IN-10 (example 84) (0-1 μM; 3 h) inhibit H3K27Ac activity in LK2 cells with an IC50 of 22 nM[1]. CBP/p300-IN-10 (38 nM-10 mM; 3 days) has inhibitory activity against LK2 and TE-8[1]. Cell Proliferation Assay[1] Cell Line: LK2 and TE-8 Concentration: 38 nM-10 mM Incubation Time: 3 days Result: Inhibited LK2 and TE-8 with GI50s of 97.163 nM and 152.484 nM, respectively.

[References]

[1]. Naito, Hiroyuki, et al. Preparation of amino acid amide derivatives such as L- and D-prolinamide derivatives as Ep300/CREBBP inhibitors. WO2018235966A1

Chemical & Physical Properties

[ Molecular Formula ]:
C25H24F5N5O3

[ Molecular Weight ]:
537.48


Related Compounds