HDAC-IN-30

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HDAC-IN-30 

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。

HDAC-IN-30

HDAC-IN-30 Chemical Structure

CAS No. : 2756809-34-2

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生物活性

HDAC-IN-30 is a novel multi-target HDAC inhibitor, including 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 exhibits potent antitumor efficacy[1].

IC50 & Target

HDAC1

13.4 nM (IC50)

HDAC2

28.0 nM (IC50)

HDAC3

9.18 nM (IC50)

HDAC6

42.7 nM (IC50)

HDAC8

131 nM (IC50)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

分子量

405.45

Formula

C22H23N5O3
CAS 号

2756809-34-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Liu Q, et al. 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. Eur J Med Chem. 2022, 229:114058.

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