1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. HDAC6-IN-75

HDAC6-IN-75 是一种选择性 HDAC6 抑制剂,对 HDAC6IC50 为 0.17 nM。HDAC6-IN-75 可诱导胶质瘤细胞中乙酰化 α-微管蛋白 (α-tubulin) 的积累。HDAC6-IN-75 可引发细胞周期改变、增加 SubG1 细胞群,并促进胶质瘤细胞和成胶质细胞瘤干细胞的凋亡 (apoptosis)。HDAC6-IN-75 可用于胶质瘤相关研究。

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HDAC6-IN-75

HDAC6-IN-75 Chemical Structure

CAS No. : 400078-78-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-75 is a selective HDAC6 inhibitor with an IC50 of 0.17 nM against HDAC6. HDAC6-IN-75 induces the accumulation of acetylated α-tubulin in glioma cells. HDAC6-IN-75 triggers cell cycle changes, increases the SubG1 cell population, and promotes apoptosis in glioma cells and glioblastoma stem cells. HDAC6-IN-75 is applicable for glioma-related research[1].

IC50 & Target[1]

HDAC6

0.17 nM ()

体外研究
(In Vitro)

HDAC6-IN-75 (compound 3a) (0.0032-50 μM; 24-72 h) 在胶质瘤细胞系中呈现时间依赖性细胞毒性,孵育 72 h 后的 GI50 值范围为 0.8 μM 至 5.3 μM,并可在 72 h 时诱导 HOG、T98G 和 U251MG 细胞完全生长抑制[1]
HDAC6-IN-75 (16.2-50 μM; 24 h) 可上调四种受试胶质瘤细胞系中乙酰化 α-微管蛋白的水平,并在处理 24 h 后上调 HOG、T98G 和 U251MG 细胞中乙酰化组蛋白 H3 的水平,这与其 HDAC6 抑制活性以及在细胞水平浓度下同时抑制 I 类 HDAC 的作用一致[1]
HDAC6-IN-75 (16.2-50 μM; 24 h) 可在 T98G 和 U251MG 细胞中诱导 DNA 片段化 (SubG1 期累积),并在处理 24 h 后通过将 U87MG、U251MG 和 HOG 细胞的细胞群从 G0/G1 期转移至 G2/M 期来调控细胞周期进程[1]
HDAC6-IN-75 (16.2-50 μM; 24 h) 可降低 HOG 和 U251MG 胶质瘤细胞的活力,并在处理 24 h 后诱导其发生晚期凋亡和坏死[1]
HDAC6-IN-75 (0.0032-50 μM; 72 h) 对胶质母细胞瘤干细胞表现出细胞毒性,在处理 72 h 后,对神经前体型 GSC23 细胞的 IC50 为 3.725 μM,对间质型 GG16 细胞的 IC50 为 12.90 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: 34.0 μM (HOG); 16.2 μM (T98G); 50 μM (U87MG); 28.9 μM (U251MG)
Incubation Time: 24 h
Result: Significantly promoted accumulation of acetyl-α-tubulin in HOG, T98G, U87MG, and U251MG cells.
Significantly promoted accumulation of acetyl-histone H3 in HOG, T98G, and U251MG cells, with activity comparable to vorinostat in these cell lines.

Cell Cycle Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 34.0 μM (HOG); 16.2 μM (T98G); 50 μM (U87MG); 28.9 μM (U251MG)
Incubation Time: 24 h
Result: Increased the percentage of cells in the SubG1 phase in T98G and U251MG cells.
Decreased the percentage of cells in the G0/G1 phase and increased the percentage in the G2/M phase in U87MG and U251MG cells.
Decreased the percentage of cells in the G0/G1 phase in HOG cells.

Apoptosis Analysis[1]

Cell Line: Glioma cell lines HOG, T98G, U87MG, U251MG
Concentration: 34.0 μM (HOG); 16.2 μM (T98G); 50 μM (U87MG); 28.9 μM (U251MG)
Incubation Time: 24 h
Result: Decreased cell viability in all four glioma cell lines.
Increased the percentage of late apoptotic and necrotic cells in HOG and U251MG cells.
分子量

292.31

Formula

C13H12N2O4S

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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产品名称:
HDAC6-IN-75
目录号:
HY-181639
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