2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Apoptosis Caspase Bcl-2 Family
  4. HDAC6-IN-67

HDAC6-IN-67 是一种选择性 HDAC6 抑制剂（IC50 = 17.15 nM），其对 HDAC1 的选择性是 HDAC1 的 19 倍。HDAC6-IN-67 通过与 Ser531 和 His614 相互作用选择性抑制 HDAC6。HDAC6-IN-67 通过诱导 caspase 9、8、3 和 PARP 的裂解、上调 Bax 表达以及下调 Bcl-2 表达来诱导细胞凋亡 (apoptosis)。HDAC6-IN-67 能有效诱导 MCF-7/ADR 细胞中 α-微管蛋白 (α-tubulin) 的乙酰化，而不影响组蛋白 H3 的乙酰化。HDAC6-IN-67 可用于乳腺癌的研究。

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HDAC6-IN-67

HDAC6-IN-67 Chemical Structure

CAS No. : 2196247-20-6

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HDAC6-IN-67 相关抗体

Top Publications Citing Use of Products

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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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

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer[1].

体外研究
(In Vitro)

HDAC6-IN-67 在所有测试的人类癌细胞系中均表现出显著的时间依赖性肿瘤细胞抑制作用，GI50 值范围为 2.9 至 24.8 μM，72 小时后对 MCF-7/ADR 细胞也表现出强烈的抗增殖活性 (GI50 = 2.4 μM)[1]。
HDAC6-IN-67 (0.01-2 μM，24 小时) 可剂量依赖性地增加 MCF-7/ADR 细胞中 α-微管蛋白的乙酰化，即使在高浓度也不会影响组蛋白 H3 的乙酰化[1]。
HDAC6-IN-67 (0.1-2 μM，10 天) 可显著且呈剂量依赖性地抑制 MCF-7/ADR 细胞的集落形成[1]。
HDAC6-IN-67 (0.1-2 μM，24 小时) 显著诱导早期和晚期细胞凋亡，并且在 MCF-7/ADR 细胞中，可剂量依赖性地诱导 Caspase 9、Caspase 8、Caspase 3 和 PARP 的裂解，同时显著上调促凋亡蛋白 Bax 的表达，并下调抗凋亡蛋白 Bcl-2 的表达[1]。

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

HDAC6-IN-67 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Dose-dependently increased the acetylation of α-tubulin.
Induced α-tubulin acetylation at concentrations as low as 0.1 μM, without affecting the acetylation of Histone H3 even at concentrations up to 1 μM.

Cell Proliferation Assay[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 10 days
Result: Resulted in a significant dose-dependent inhibition of colony formation.
A concentration of 1 μM was able to suppress colony formation by approximately 65 %.

Western Blot Analysis[1]

Cell Line: MCF-7/ADR cells
Concentration: 0.1 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 24 h
Result: Significantly induces early and late apoptosis by 25.4% and 15.7%.
The cleavage of Caspase 9, Caspase 8, Caspase 3, and PARP were significantly induced in a dose-dependent manner.
The apoptotic protein Bax was significantly induced, whereas the anti-apoptotic protein Bcl-2 was remarkably decreased in a dose-dependent manner.
体内研究
(In Vivo)

HDAC6-IN-67 (5 mg/kg、10 mg/kg，腹腔注射，工作日每日一次，周末休息，持续 17 天) 在小鼠体内以剂量依赖的方式抑制 HCT116 肿瘤的生长，且无明显毒性[1]。

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

Animal Model: Subcutaneously injecting nude mice with HCT116 human colon cancer cells (2.0 × 106 cells/ mice).
Dosage: 5 mg/kg, 10 mg/kg
Administration: I.p., daily during weekdays, followed by weekend rest for 17 days
Result: Showed delayed tumor growth starting right after the first measurement.
Found no differences in body weight, treatment-related deaths, or abnormal behaviors between the control and experimental groups.
分子量

309.32

Formula

C17H15N3O3
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-67 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:

HDAC6-IN-672196247-20-6HDACMicrotubule/TubulinApoptosisCaspaseBcl-2 FamilyHistone deacetylasesAnticancer drugEpigeneticsHDAC6InhibitorsQuinazolin-4-oneInhibitorinhibitorinhibit

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