2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC Topoisomerase
  4. HDAC/Top-IN-1

HDAC/Top-IN-1 是一种具有口服活性的、广谱的 HDAC/Top 双重抑制剂，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50 分别为 0.036 μM、0.14 μM、0.059 μM、0.089 μM 和 9.8 μM。HDAC/Top-IN-1 能有效诱导 HEL 细胞凋亡 (apoptosis)，能将细胞阻滞在 S 期。

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HDAC/Top-IN-1 Chemical Structure

HDAC/Top-IN-1 Chemical Structure

CAS No. : 2411379-14-9

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HDAC/Top-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Topoisomerase 亚型特异性产品:

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Topoisomerase Topo I Topo II

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy[1].

IC50 & Target[1]

HDAC1

34 nM (IC50)

HDAC2

140 nM (IC50)

HDAC3

59 nM (IC50)

HDAC6

89 nM (IC50)

HDAC8

9.8 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.68 μM
Compound: 16j
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
[PMID: 35238576]
HCT-116 IC50
0.21 μM
Compound: 16j
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
[PMID: 35238576]
HEL IC50
0.029 μM
Compound: 16j
Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
[PMID: 35238576]
HepG2 IC50
0.26 μM
Compound: 16j
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
[PMID: 35238576]
K562 IC50
0.35 μM
Compound: 16j
Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
[PMID: 35238576]
MCF7 IC50
> 2 μM
Compound: 16j
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay
[PMID: 35238576]
体外研究
(In Vitro)

HDAC/Top-IN-1 (compound 16j) (0-2 μM; 48 hours) exhibits remarkable inhibitory activities against the tested cell lines[1].
HDAC/Top-IN-1 (20 and 100 nM; 24 hours) dramatically increases acetyl-H3 and acetyl-H4 levels in HEL cells[1].
HDAC/Top-IN-1 (0.1 and 0.5 μM; 48 hours) effectively induces HEL cell apoptosis in a dose-dependent manner[1].
HDAC/Top-IN-1 (0.02-0.5 μM; 48 hours) arrests HEL cells at the S phase[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC/Top-IN-1 相关抗体:

Cell Proliferation Assay

Cell Line: MCF-7, A549, HCT116, HepG-2, K562 and HEL[1]
Concentration: 0-2 μM
Incubation Time: 48 hours
Result: Exhibited remarkable inhibitory activities against the tested cell lines, and IC50s of 0.68, 0.21, 0.26, 0.35 and 0.029 μM in MCF-7, A549, HCT116, HepG-2, K562 and HEL, respectively.

Western Blot Analysis

Cell Line: HEL[1]
Concentration: 20 and 100 nM
Incubation Time: 24 hours
Result: Dramatically increased in acetyl-H3 and acetyl-H4 levels.

Apoptosis Analysis

Cell Line: HEL[1]
Concentration: 0.1 and 0.5 μM
Incubation Time: 48 hours
Result: Led to 56.02% and 76.45% apoptotic cell death at concentration of 0.1 and 0.5 μM, respectively

Cell Cycle Analysis

Cell Line: HEL[1]
Concentration: 0.02, 0.1 and 0.5 μM
Incubation Time: 48 hours
Result: The ratios in the S phase were changed dramatically 9.8%, 15.4%, and 25.8% at 0.02, 0.1 and 0.5 μM, respectively.
体内研究
(In Vivo)

HDAC/Top-IN-1 exhibits good metabolic properties with a half-life (T1/2) of 31.49 min, and the clearance is 173.32 mL/min/mg[1].
HDAC/Top-IN-1 (5 and 10 mg/kg; PO; daily, for 14 days) exhibits potent oral antitumor activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C nude mice (5-6 weeks, 18-20 g; injected with human K562 cells)[1]
Dosage: 5 and 10 mg/kg
Administration: PO; daily, for 14 days
Result: Exhibited potent oral antitumor activity at 5 mg/kg with a TGI value of 41.4% and a T/C value of 54.3%, and achieved better tumor growth inhibition with a TGI of 68.5% and a T/C of 25.5%.
分子量

512.53

Formula

C29H25FN4O4
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

HDAC/Top-IN-1 相关分类

  • 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.

Keywords:

HDAC/Top-IN-12411379-14-9HDACTopoisomeraseHistone deacetylasesAntitumorOrally activeHEL cellsCell cycleInhibitorinhibitorinhibit

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