1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. HDAC1/3-IN-1

HDAC1/3-IN-1 是一种选择性 HDAC1/3 抑制剂,对 HDAC1 HDAC3IC50 分别为 256 nM 和 340.3 nM。HDAC1/3-IN-1 可增加 SubG1 细胞群,并促进胶质瘤细胞和胶质母细胞瘤干细胞的凋亡 (apoptosis)。HDAC1/3-IN-1 可用于胶质母细胞瘤的相关研究。

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HDAC1/3-IN-1

HDAC1/3-IN-1 Chemical Structure

CAS No. : 244289-53-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC1/3-IN-1 is a selective HDAC1/3 inhibitor, with IC50 values of 256 nM and 340.3 nM against HDAC1 and HDAC3, respectively. HDAC1/3-IN-1 increases the SubG1 cell population and promotes apoptosis of glioma cells and glioblastoma stem cells. HDAC1/3-IN-1 can be used in studies related to glioblastoma[1].

IC50 & Target[1]

HDAC1

256 nM ()

HDAC3

340.3 nM ()

体外研究
(In Vitro)

HDAC1/3-IN-1 (Compound 6a) (0.6-50 μM; 24-72 h) 以时间依赖的方式抑制 HOG、T98G、U87MG 和 U251MG 胶质瘤细胞系的增殖,其中在 U251MG 细胞中孵育 72 h 后测得的最低 GI50 为 0.6 μM[1]
HDAC1/3-IN-1 (10.8-50 μM; 24 h) 可在相关浓度下作用 24 h 时抑制 HOG、T98G 和 U251MG 胶质瘤细胞系中组蛋白 H3 的去乙酰化[1]
HDAC1/3-IN-1 (10.8-50 μM; 24 h) 可在侵袭性胶质瘤细胞系 T98G 和 U251MG 中诱导 SubG1 期细胞积累,提示存在 DNA 片段化和细胞凋亡,同时可调节受试胶质瘤细胞系的细胞周期时相分布[1]
HDAC1/3-IN-1 (10.8-50 μM; 24 h) 诱导 HOG、T98G、U87MG 和 U251MG 胶质瘤细胞系发生早期凋亡[1]
HDAC1/3-IN-1 (72 h) 可抑制间质型 (GG16) 和前神经元型 (GSC23) 胶质母细胞瘤干细胞系的活力,孵育 72 h 后其 IC50 值分别为 2.079 μM 和 1.851 μM[1]

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

Western Blot Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 50 μM (HOG, T98G, U87MG); 10.8 μM (U251MG)
Incubation Time: 24 h
Result: Promoted accumulation of acetyl-histone H3 in HOG, T98G, and U251MG cell lines, with comparable effects to positive controls in these cells.

Cell Cycle Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 50 μM (T98G); 10.8 μM (U251MG)
Incubation Time: 24 h
Result: Increased the percentage of cells in the SubG1 phase in T98G and U251MG cell lines.
Modulated cell cycle phase distribution, increasing the G0/G1 phase in HOG cells and modulating the S phase in U87MG cells.

Apoptosis Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 50 μM (HOG, T98G, U87MG); 10.8 μM (U251MG)
Incubation Time: 24 h
Result: Induced early apoptosis in HOG, T98G, U87MG, and U251MG cell lines.
分子量

367.42

Formula

C19H17N3O3S

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
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HDAC1/3-IN-1
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HY-181640
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