1. Cell Cycle/DNA Damage Epigenetics Cytoskeleton
  2. HDAC Microtubule/Tubulin
  3. FT108

FT108 是一种选择性 HDAC6 抑制剂,其 IC50 为 0.026 μM。FT108 对 HDAC3HDAC8 仅表现出微弱的体外活性,对应的 IC50 值分别为 6.68 μM 和 4.07 μM。FT108 可提高微管蛋白 (tubulin) 的乙酰化水平,而对乙酰化组蛋白 H3 的水平几乎无影响。FT108 对骨髓增殖性肿瘤细胞系无活性,且不会抑制 JAK2 的磷酸化及其下游靶点 pSTAT3 和 pSTAT5。

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FT108

FT108 Chemical Structure

CAS No. : 2379645-28-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FT108 is a selective HDAC6 inhibitor with an IC50 of 0.026 μM. FT108 exhibits only modest in vitro activity against HDAC3 and HDAC8 with IC50 values of 6.68 and 4.07 μM. FT108 increases acetylation of tubulin and has little to no effect on acetylated histone H3 levels. FT108 lacks activity against myeloproliferative neoplasm cell lines, and does not suppress JAK2 phosphorylation or its downstream targets pSTAT3 and pSTAT5[1].

IC50 & Target[1]

HDAC6

0.026 μM (IC50)

HDAC8

4.07 μM (IC50)

HDAC3

6.68 μM (IC50)

体外研究
(In Vitro)

FT108 (0.03-16 μM; 48 h) 在浓度高达 16 μM、处理 48 小时的条件下,不会降低 HEL92.1.7、SET-2、JAK2V617F Ba/F3 或 MPLW515L Ba/F3 骨髓增殖性肿瘤 (MPN) 细胞系的存活率[1]
FT108 (0.2-1 μM; 24 h) 可增加 HEL92.1.7 骨髓增殖性肿瘤 (MPN) 细胞中 ac-tubulin 水平 ,但对 JAK-STAT 信号通路的活性或乙酰化组蛋白 H3 的水平无明显影响[1]
FT108 是一种高选择性的 HDAC6 抑制剂 (IC50 = 0.026 μM),在酶促生化分析中对 HDAC3 (IC50 = 6.68 μM) 和 HDAC8 (IC50 = 4.07 μM) 的交叉反应性较弱[1]

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

Cell Viability Assay[1]

Cell Line: human HEL92.1.7, human SET-2, mouse JAK2V617 Ba/F3, mouse MPLW515LBa/F3 cells
Concentration: 0.03, 0.06, 0.12, 0.25, 1, 2, 4, 8,16 μM
Incubation Time: 48 h
Result: Lacked activity in all tested MPN cell lines, with cell survival remaining near 100% across all concentrations tested.

Western Blot Analysis[1]

Cell Line: human HEL92.1.7 MPN cells
Concentration: 0.2, 0.5, 1 μM
Incubation Time: 24 h
Result: Caused marked increases in ac-tubulin levels, consistent with effective HDAC6 suppression.
Had little to no effect on acetylated histone H3 levels.
Did not reduce levels of phosphorylated JAK2, phosphorylated STAT3, or phosphorylated STAT5, and had no impact on total JAK2, STAT3, or STAT5 levels.
分子量

320.34

Formula

C16H20N2O5

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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  • 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.

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FT108
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HY-182720
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