Ep300/CREBBP-IN-3

Names

[ CAS No. ]:
2259641-47-7

[ Name ]:
Ep300/CREBBP-IN-3

Biological Activity

[Description]:

Ep300/CREBBP-IN-3 (Example 61) is a potent Ep300 and CREBBP inhibitor with IC50s of 0.056 and 0.095 μM, respectively. Ep300/CREBBP-IN-3 can be used for the research of cancer[1].

[Related Catalog]:

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

[Target]

EP300:0.056 μM (IC50)

CREBBP:0.095 μM (IC50)


[In Vitro]

Ep300/CREBBP-IN-3 (Example 61) 抑制细胞内 H3K27Ac 活性，其 IC50 为 0.021 μM[1]。 Ep300/CREBBP-IN-3 (38 nM-10 mM; 3 days) 抑制 LK2 和 TE-8 细胞生长，GI50 分别为 148.858 μM 和 215.717 μM [1]。 Cell Viability Assay[1] Cell Line: LK2 and TE-8 cells Concentration: 38 nM-10 mM Incubation Time: 3 days Result: Inhibited LK2 and TE-8 cell growth with GI50s of 148.858 and 215.717 μM, respectively.

[References]

[1]. NAITO Hiroyuki, et al. EP300 / CREBBP inhibitor. Patent JPWO2018235966A1.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H25F4N5O3

[ Molecular Weight ]:
531.50

Related Compounds

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