Ep300/CREBBP-IN-8

Ep300/CREBBP-IN-8 (Example 37) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.014 and 0.018 μM, respectively. Ep300/CREBBP-IN-8 can be used for the research of cancer[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

EP300:0.014 μM (IC50)

CREBBP:0.018 μM (IC50)

Ep300/CREBBP-IN-8 (Example 37) 抑制细胞内 H3K27Ac 活性，其 IC50 为 0.016 μM[1]。 Ep300/CREBBP-IN-8 (38 nM-10 mM; 3 days) 抑制 LK2 和 TE-8 细胞生长，GI50 分别为 85.917 μM 和 112.922 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 85.917 and 112.922 μM, respectively.

Ep300/CREBBP-IN-8 (Example 37; 6.25 mg/kg/day; oral; twice daily for 11 days) 抑制小鼠肿瘤增殖[1]。 Animal Model: Female BALB/c-nu/nu mice, LK2 cell subcutaneous transplant model[1] Dosage: 6.25 mg/kg/day Administration: Oral administration, twice a day for 11 days Result: Inhibited tumor volume by 42%.

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