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。
产品描述
HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 ( IC 50 =13.4 nM), HDAC2 ( IC 50 =28.0 nM), HDAC3 ( IC 50 =9.18 nM), HDAC6 ( IC 50 =42.7 nM), HDAC8 ( IC 50 =131 nM). HDAC-IN-30 exhibits potent antitumor efficacy [1].
体外活性
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]. Western Blot Analysis [1] Cell Line: HepG2 cells Concentration: 0.5, 1, 2 μM Incubation Time: 24 hours Result: Could effectively activate the p53 pathway by promoting the phosphorylation of p53 Cell Cycle Analysis [1] Cell Line: HepG2 cells Concentration: 0, 1, 2.5, 5 μM Incubation Time: 48 hours Result: Cells were arrested at the G2 phase in a dose-dependent manner. Apoptosis Analysis [1] Cell Line: HepG2 cells Concentration: 0, 1, 2.5, 5 μM Incubation Time: 24 hours Result: Possessed prominent anticancer activity in HepG2 cells.
体内活性
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]. Animal Model: HepG2 xenograft mouse model [1] Dosage: 12, 24 mg/kg Administration: Intraperitoneal injection, every 2 days, 4 weeks Result: Exhibited potent anticancer activity
Cas No.
2756809-34-2
分子式
C22H23N5O3
分子量
405.45
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years