2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis Caspase
  4. HDAC1-IN-13

HDAC1-IN-13 是一种口服有效的 HDAC1 抑制剂，对 HDAC1、HDAC2、HDAC3 和 HDAC10 的 IC50 为 91、185 、170 和 280 nM，对 HDAC4、HDAC5、HDAC6、HDAC7 和 HDAC9 无活性。HDAC1-IN-13 通过激活 caspase-8 通路诱导外源性细胞凋亡 (apoptosis)，引发 G0/G1 期细胞周期阻滞。HDAC1-IN-13 可用于白血病的研究。

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HDAC1-IN-13

HDAC1-IN-13 Chemical Structure

CAS No. : 3053289-22-5

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HDAC1-IN-13 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 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC1-IN-13 is an orally active HDAC1 inhibitor with IC50 values of 91, 185, 170, and 280 nM against HDAC1, HDAC2, HDAC3, and HDAC10, respectively, and shows no activity against HDAC4, HDAC5, HDAC6, HDAC7, and HDAC9. HDAC1-IN-13 induces extrinsic apoptosis by activating the caspase-8 pathway and triggers G0/G1 cell cycle arrest. HDAC1-IN-13 can be used for the research of leukemia[1].

IC50 & Target[1]

HDAC1

91 nM (IC50)

HDAC2

181 nM (IC50)

HDAC3

170 nM (IC50)

HDAC10

280 nM (IC50)

Caspase-8

 

体外研究
(In Vitro)

HDAC1-IN-13 (Compound 6B) 可强效抑制 HDAC1 (IC50 = 91 nM)、HDAC2 (IC50 = 185 nM)、HDAC3 (IC50 = 170 nM) 和 HDAC10 酶，对 HDAC4、HDAC5、HDAC7、HDAC8 或 HDAC9 无活性[1]。
HDAC1-IN-13 (Compound 6b) (72 h) 可在体外强效抑制 HL-60 (IC50 = 0.31 μM)、CCRF-CEM (IC50 = 0.36 μM) 和 HepG2 (IC50 = 1.01 μM) 癌细胞的增殖[1]。
HDAC1-IN-13 (72 h) 对人正常肝细胞 LO2 的细胞毒性较低 (IC50 = 5.67 μM)，相对于 HL-60 癌细胞的选择性指数高达 18.3[1]。
HDAC1-IN-13 (0.1-2.5 μM; 48 h) 可浓度依赖性地增加组蛋白 H3 的乙酰化水平，下调 Rb/p-Rb 和 caspase-8 前体，并调控 HL-60 细胞中 BAX、BAK 和 BCL-2 的表达[1]。
HDAC1-IN-13 (0-2.5 μM; 48 h) 可浓度依赖性地诱导 HL-60 细胞发生凋亡[1]。
HDAC1-IN-13 (0-2.5 μM; 48 h) 可浓度依赖性地诱导 HL-60 细胞发生 G0/G1 期细胞周期阻滞[1]。

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

HDAC1-IN-13 相关抗体:

Western Blot Analysis[1]

Cell Line: HL-60 promyelocytic leukemia cells
Concentration: 0.1 μM, 0.5 μM, 2.5 μM
Incubation Time: 48 h
Result: Induced a concentration-dependent increase in acetylated histone H3 (Ac-H3) levels, while total histone H3 levels remained unchanged.
Downregulated expression of Rb, phosphorylated Rb (p-Rb), and caspase-8 precursor in a concentration-dependent manner.
Downregulated BAX, BAK, and BCL-2 expression.

Apoptosis Analysis[1]

Cell Line: HL-60 promyelocytic leukemia cells
Concentration: 0 μM, 0.1 μM, 0.5 μM, 2.5 μM
Incubation Time: 48 h
Result: Induced apoptosis in a concentration-dependent manner, with apoptosis rates of 13.87% (0 μM), 25.6% (0.1 μM), 27.6% (0.5 μM), and 46.1% (2.5 μM).
Reached a late apoptotic cell proportion of 22.7% at the highest concentration.

Cell Cycle Analysis[1]

Cell Line: HL-60 promyelocytic leukemia cells
Concentration: 0 μM, 0.1 μM, 0.5 μM, 2.5 μM
Incubation Time: 48 h
Result: Induced G0/G1 phase cell cycle arrest in a concentration-dependent manner, with the proportion of cells in G0/G1 phase increasing from 56.4% (0 μM) to 76.5% (2.5 μM).
体内研究
(In Vivo)

HDAC1-IN-13 (Compound 6b) (15-30 mg/kg；灌胃；每日一次；18 天) 经灌胃给药后在小鼠模型中展现出显著的体内抗白血病活性，且无明显毒性[1]。
HDAC1-IN-13 (20 mg/kg；腹腔注射；每日一次；连续 7 天) 经腹腔给药后在小鼠模型中展现出强效的体内抗白血病活性，且无明显毒性[1]。

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

Animal Model: BALB/c nude (male, 6-8 weeks old, 18-22 g, subcutaneous xenograft model)[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.g.; daily; 18 days
Result: Achieved a tumor growth inhibition (TGI) rate of 20.72% at 30 mg/kg.
Showed no obvious pathological changes in heart, liver, spleen, lung, or kidney tissue.
Maintained stable mouse body weights throughout the study.
Animal Model: BALB/c nude (male, 6-8 weeks old, 18-22 g, subcutaneous xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 7 days
Result: Reduced tumor volume by 58.4% after 7 days.
Showed no changes in mouse body weight during the study, indicating low in vivo toxicity.
分子量

368.43

Formula

C23H20N4O
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

HDAC1-IN-13 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

HDAC1-IN-133053289-22-5HDACApoptosisCaspaseHistone deacetylasesHL-60HDAC1histone H3HDAC3G0/G1 phaseHDAC2HepG2HDAC10CCRF-CEMcaspase-8 pathwayInhibitorinhibitorinhibit

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