2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton
  3. HDAC Microtubule/Tubulin Histone Methyltransferase
  4. HDAC6-IN-65

HDAC6-IN-65 是一种选择性 HDAC6 抑制剂 (IC50 = 0.9 nM) ，同时对 HDAC3 也具有一定的抑制作用 (IC50 = 39.4 nM) 。HDAC6-IN-65 可诱导 Neuro-2a 细胞中 α-微管蛋白 (ac-tubulin) 和乙酰化组蛋白 H3 (ac-histone H3，一种 I 类 HDAC 抑制标志物) 的积累。HDAC6-IN-65 可用于黑色素瘤的研究。

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HDAC6-IN-65

HDAC6-IN-65 Chemical Structure

CAS No. : 3028442-70-5

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HDAC6-IN-65 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 Histone Methyltransferase 亚型特异性产品:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-65 is a selective HDAC6 inhibitor (IC50 = 0.9 nM) and also exhibits a certain suppressive effect on HDAC3 (IC50 = 39.4 nM). HDAC6-IN-65 can induce the accumulation of α-tubulin (ac-tubulin) and acetylated histone H3 (ac-histone H3, a class I HDAC inhibition marker) in Neuro-2a cells. HDAC6-IN-65 can be used for the study of melanoma[1].

IC50 & Target[1]

HDAC6

0.9 nM (IC50)

HDAC3

39.4 nM (IC50)

体外研究
(In Vitro)

HDAC6-IN-65 (Compound 14) 对白血病细胞系 (MV4-11，IC50 = 0.57 μM) 以及对其他肿瘤细胞 (MM.1S，IC50 = 2.45 μM；Neuro-2a，IC50 = 6.24 μM；SH-SY5Y，IC50 = 3.75 μM) 均表现出显著的抗增殖活性，且对正常细胞 (HEK-293，IC50 = 6.09 μM；pNHF，IC50 = 16.24 μM；MRC9，IC50 = 19.08 μM) 的毒性较低[1]。
HDAC6-IN-65 (0.05-5 μM) 在浓度为 50 nM 时可显著诱导 Neuro-2a 细胞中 α-微管蛋白 (ac-tubulin) 的积累 (HDAC6 抑制的标志物) ，并且在浓度为 1 μM 时乙酰化组蛋白 H3 (ac-histone H3，I 类 HDAC 抑制的标志物) 也增加[1]。
HDAC6-IN-65 (0.5 μM，6-72 小时) 在 RDES 细胞中虽然对 I 类 HDAC 的抑制作用较弱或持续时间较短，但其药理作用可能在全身暴露后持续存在[1]。

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

HDAC6-IN-65 相关抗体:

Western Blot Analysis[1]

Cell Line: RDES cell line
Concentration: 0.5 μM
Incubation Time: 6 h, 12 h, 24 h, 48 h, 72 h
Result: Significantly increased ac-tubulin levels in RDES cells at 6 h, which persist until 48 h, and begin to decline at 72 h. Ac-histone H3 levels increased at 6 and 12 h, but returned to baseline at 24 h.
体内研究
(In Vivo)

HDAC6-IN-65 (Compound 14) (25 mg/kg，腹腔注射，每日一次，持续 14 天，周一至周五) 可有效抑制小鼠 SM1 黑色素瘤模型中的肿瘤生长并激活免疫调节，且在测试浓度下对小鼠无明显毒性[1]。

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

Animal Model: C57BL/6 female mice were injected subcutaneously with 106 in vivo passaged SM1 melanoma cells suspended in 100 μL of PBS[1].
Dosage: 25 mg/kg
Administration: I.p., once daily for 14 days, M-F
Result: The mean tumor growth inhibition rate (TGI) was 56%.
All mice showed normal body weight and organ function, with no signs of toxicity.
Flow cytometry revealed an increase in CD4+ and CD8+ T cells, NK cells, and M1 macrophages, and a decrease in M2 macrophages in the tumor microenvironment.
分子量

431.89

Formula

C20H18ClN3O4S
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

HDAC6-IN-65 相关分类

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  • 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:

HDAC6-IN-653028442-70-5HDACMicrotubule/TubulinHistone MethyltransferaseHistone deacetylasesTO-317SM1 Melanoma ModelHDAC6HDAC3Inhibitorinhibitorinhibit

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