2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Apoptosis
  4. HDAC-IN-54

HDAC-IN-54 是一种 HDAC 抑制剂，对人源 HDAC1 的 IC50 为 25 nM，对 HDAC2 的 IC50 为 66 nM，对 HDAC3 的 IC50 为 6.5 nM，对 HDAC6 的 IC50 为 281 nM。HDAC-IN-54 诱导 α-微管蛋白 (α-tubulin) 及组蛋白 H3 的乙酰化。HDAC-IN-54 可与顺铂协同诱导癌细胞凋亡 (apoptosis)。HDAC-IN-54 可用于头颈癌、卵巢癌、舌鳞状细胞癌的相关研究。

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HDAC-IN-54

HDAC-IN-54 Chemical Structure

CAS No. : 2098896-13-8

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HDAC-IN-54 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-54 is a HDAC inhibitor with an IC50 of 25 nM against human HDAC1, 66 nM against HDAC2, 6.5 nM against HDAC3, and 281 nM against HDAC6. HDAC-IN-54 induces acetylation of α-tubulin and histone H3. HDAC-IN-54 acts synergistically with cisplatin to induce cancer cell apoptosis. HDAC-IN-54 can be used in research related to head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma[1].

IC50 & Target

hHDAC1

25 nM (IC50)

HDAC2

66 nM (IC50)

HDAC3

6.5 nM (IC50)

HDAC6

281 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-54 (Compound 4j) (18 h) 可在 A2780、A2780CisR、Cal27 和 Cal27CisR 细胞中抑制细胞 HDAC 活性，IC50 值分别为 0.48、0.32、0.27、0.35 μM[1]。
HDAC-IN-54 (72 h) 可降低 A2780、A2780CisR、Cal27 和 Cal27CisR 细胞的活力，IC50 值分别为 0.47、1.62、0
44、1.13 μM[1]。
HDAC-IN-54 (90 分钟) 可强效抑制重组人源 HDAC1-3 和 HDAC6 酶，其中对 HDAC3 的抑制活性最强 (IC50 = 6.5 nM)，其次为 HDAC1 (25.0 nM)、HDAC2 (66 nM)、HDAC6 (281 nM)，对 HDAC8 仅表现出弱活性 (2750 nM)[1]。
HDAC-IN-54 (10 μM; 24 h) 可在 Cal27 和 Cal27CisR 细胞中诱导 α-微管蛋白及组蛋白 H3 的乙酰化，证实其可同时抑制 I 类 HDAC 和 HDAC6[1]。
HDAC-IN-54 (250-500 nM; 48 h preincubation) 可在 Cal27 和 Cal27CisR 细胞中以浓度依赖的方式增强 Cisplatin (HY-17394) 敏感性[1]。
HDAC-IN-54 (250-500 nM; 48 h preincubation) 可协同增强 Cisplatin 诱导的 Cal27 和 Cal27CisR 细胞凋亡[1]。

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

HDAC-IN-54 相关抗体:

Western Blot Analysis[1]

Cell Line: Cal27, Cal27CisR
Concentration: 10 μM
Incubation Time: 24 h
Result: Induced an increase in acetylation of α-tubulin and histone H3 in both cell lines, with effects more pronounced in Cal27 than in Cal27CisR.

Cell Viability Assay[1]

Cell Line: Cal27, Cal27CisR
Concentration: 250 nM, 500 nM
Incubation Time: 48 h (preincubation); 72 h (total incubation)
Result: Reduced the IC50 of Cisplatin from 3.01 μM to 1.95 μM (shift factor = 1.5) in Cal27, and from 50.4 μM to 16.1 μM (shift factor = 3.1) in Cal27CisR at 250 nM.
Reduced the IC50 of Cisplatin from 3.01 μM to 0.78 μM (shift factor = 3.9) in Cal27, and from 50.4 μM to 7.37 μM (shift factor = 6.8) in Cal27CisR at 500 nM.

Apoptosis Analysis[1]

Cell Line: Cal27, Cal27CisR
Concentration: 250 nM, 500 nM
Incubation Time: 48 h (preincubation)
Result: Induced a significant increase in apoptotic nuclei in Cal27 when combined with Cisplatin at 250 nM and 500 nM.
Induced a significant increase in apoptotic nuclei in Cal27CisR when combined with Cisplatin at 500 nM.
分子量

440.54

Formula

C24H32N4O4
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

HDAC-IN-54 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

HDAC-IN-542098896-13-8HDACMicrotubule/TubulinApoptosisHistone deacetylasesA2780cisplatin-resistant head-neck cancer cellsCal27histone deacetylaseA2780CisRHDAC3HDAC1Cal27CisRHDAC6HDAC2HDAC inhibitorhead and neck cancerovarian cancertongue squamous cell carcinomInhibitorinhibitorinhibit

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