DCH36_06 是一种有效的选择性 p300/CBP 抑制剂，对 p300 和 CBP 的 IC₅₀ 分别为 0.6 μM 和 3.2 μM。DCH36_06 介导的 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化。抗肿瘤活性。

DCH36_06 is a potent and selective p300/CBP inhibitor with IC 50 s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.

Solid

DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells.
DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.
DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range.
has not independently confirmed the accuracy of these methods. They are for reference only.

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: MV4-11 xen

Room temperature in continental US; may vary elsewhere.

4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

[1]. Wenchao Lu, et al. Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors. Bioorg Med Chem. 2018 Nov 1;26(20):5397-5407.

In Vitro: DMSO : 125 mg/mL (335.27 mM; Need ultrasonic)配制储备液