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:

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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)

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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