HDAC-IN-30

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-30amp;;

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].

MCE 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].

MCE 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.