1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. 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。

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HDAC-IN-30 Chemical Structure

HDAC-IN-30 Chemical Structure

CAS No. : 2756809-34-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
0.0738 μM
Compound: 8h
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
HepG2 IC50
0.0822 μM
Compound: 8h
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
HL-60 IC50
0.677 μM
Compound: 8h
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HL-60 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
HUVEC IC50
1.91 μM
Compound: 8h
Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
K562 IC50
0.719 μM
Compound: 8h
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
L02 IC50
1.96 μM
Compound: 8h
Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
MCF7 IC50
0.256 μM
Compound: 8h
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
PC-3 IC50
0.921 μM
Compound: 8h
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
RS4-11 IC50
1.26 μM
Compound: 8h
Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 34954595]
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
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
HDAC-IN-30
目录号:
HY-144292
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