HDAC-IN-30 是一种新颖的多靶点HDAC抑制剂，靶点主要有 HDAC1 (IC50=13.4 nM)，HDAC2 (IC50=28.0 nM)， HDAC3 (IC50=9.18 nM)，HDAC6 (IC50=42.7 nM)，HDAC8 (IC50=131 nM)。HDAC-IN-30 表现出非常强大的抗肿瘤作用。

体外研究：

HDAC-IN-30 (compound 8 h; 0.5, 1, 2 μM; 48 hours) can effectively activate the p53 pathway by promoting the phosphorylation of p53[1]. HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours; HepG2 cells) induces cell cycle arrest at the G2 phase in a concentration-dependent manner[1]. HDAC-IN-30 (0, 1, 2.5, 5 mM; 48 hours) possesses prominent anticancer activity in HepG2 cells[1].

体内研究：

HDAC-IN-30 (12, 24 mg/kg; intraperitoneal injection, every two days for 4 weeks) exhibits potent anticancer activity and no side effects even at high dose (24 mg/kg)[1].

CAS 号：2756809-34-2
分子量：405.45
分子式：C22H23N5O3

参考文献：
Discovery of phthalazino[1,2-b]-quinazolinone derivatives as multi-target HDAC inhibitors for the treatment of hepatocellular carcinoma via activating the p53 signal pathway【DOI: 10.1016/j.ejmech.2021.114058】