1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis Caspase
  3. HDAC-IN-100

HDAC-IN-100 是一种组蛋白去乙酰化酶抑制剂,对 HDAC1IC50 为 0.038 μM,对 HDAC2IC50 为 0.283 μM,对 HDAC3IC50 为 0.586 μM。HDAC-IN-100 可作为化学增敏剂和凋亡 (apoptosis) 诱导剂,激活 caspase 3/7,并逆转 Cisplatin (HY-17394) 耐药性。HDAC-IN-100 可在卵巢癌细胞和鳞状癌细胞中发挥抗增殖作用。HDAC-IN-100 可用于卵巢癌、鳞状细胞癌和 Cisplatin (HY-17394) 耐药性鳞状细胞癌的相关研究。

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Custom Peptide Synthesis

HDAC-IN-100

HDAC-IN-100 Chemical Structure

CAS No. : 2390474-88-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-100 is a histone deacetylase inhibitor with an IC50 of 0.038 μM against HDAC1, 0.283 μM against HDAC2, and 0.586 μM against HDAC3. HDAC-IN-100 acts as a chemosensitizer and apoptosis inducer, activates caspase 3/7, and reverses Cisplatin (HY-17394) resistance. HDAC-IN-100 exerts antiproliferative effects in ovarian cancer cells and squamous cancer cells. HDAC-IN-100 is applicable for research related to ovarian cancer, squamous cell carcinoma, and Cisplatin (HY-17394)-resistant squamous cell carcinoma[1].

IC50 & Target[1]

HDAC1

0.038 μM (IC50)

HDAC2

0.283 μM (IC50)

HDAC3

0.586 μM (IC50)

Caspase-3

 

Caspase-7

 

体外研究
(In Vitro)

HDAC-IN-100 (compound 2a) (72 h) 可降低 A2780 (IC50 2.40 μM) 和 Cal27 (IC50 1.60 μM) 人源癌细胞的存活率[1]
HDAC-IN-100 (0-100 μM; 18 h) 可强效抑制 A2780 (IC50 0.48 μM) 和 Cal27 (IC50 0.11 μM) 人癌细胞中的细胞 HDAC 活性[1]
HDAC-IN-100 (0.5 μM; 48 h) 可与 Cisplatin (HY-17394) 产生强烈的协同作用,降低 Cal27 细胞和 Cisplatin 耐药性 Cal27CisR 细胞的活力,完全逆转 Cal27CisR 细胞的 Cisplatin 耐药性[1]
HDAC-IN-100 (0.5 μM; 48 h) 可显著提高 Cal27 细胞和 Cisplatin (HY-17394) 耐药性 Cal27CisR 细胞的凋亡水平[1]
HDAC-IN-100 (0.5 μM; 24 h) 可在 Cal27 细胞和 Cisplatin (HY-17394) 耐药 Cal27CisR 细胞中诱导组蛋白 H3 的高乙酰化[1]

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

Cell Viability Assay[1]

Cell Line: Human tongue squamous cell carcinoma Cal27 cells, cisplatin-resistant Cal27CisR cells
Concentration: 0.5 μM
Incubation Time: 48 h (pretreatment); 72 h (Cisplatin incubation)
Result: Reduced the cisplatin IC50 from 9.79 μM to 1.26 μM in Cal27 cells.
Reduced the cisplatin IC50 from 63.2 μM to 8.42 μM in Cal27CisR cells,.
Showed synergistic interaction with Cisplatin, with strong synergism observed at multiple concentration combinations.
分子量

535.64

Formula

C32H33N5O3

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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产品名称:
HDAC-IN-100
目录号:
HY-P11678
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