1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis Bcl-2 Family CDK
  3. HDAC-IN-51

HDAC-IN-51 是一种有效的组蛋白脱乙酰酶 (HDAC) 抑制剂,对 HDAC10、HDAC1、HDAC2、 HDAC3HDAC11IC50 值分别为 0.32、0.353、0.431、0.515 和 85.4 μM。HDAC-IN-51 诱导细胞周期停滞和细胞凋亡,调节细胞周期/细胞凋亡相关的 miRNA 表达。HDAC-IN-51 可用于癌症研究。

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HDAC-IN-51 Chemical Structure

HDAC-IN-51 Chemical Structure

CAS No. : 3026728-28-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer[1].

IC50 & Target[1]

HDAC10

0.32 μM (IC50)

HDAC1

0.353 μM (IC50)

HDAC2

0.431 μM (IC50)

HDAC3

0.515 μM (IC50)

HDAC11

85.4 μM (IC50)

体外研究
(In Vitro)

HDAC-IN-51 (compound 8d; 1 nM-10 μM; 48 h) has antiproliferative activity with IC50 values of 0.54, 0.56, and 1.35 μM for K562, HCT116, and A549 cells, respectively[1].
HDAC-IN-51 (1 and 5 μM; 24 and 48 h; U937 leukaemia cells) arrests cell cycle at the G1 phase[1].
HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) induces apoptosis and down-regulates miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p)[1].
HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) increases mRNA expression of p21, BAX and BAK, down-regulates cyclin D1 and BCL-2[1].

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

Cell Viability Assay[1]

Cell Line: K562, HCT116, and A549 cells
Concentration: 1 nM-10 μM
Incubation Time: 48 hours
Result: Inhibited cell growth in cancer cells.

Cell Cycle Analysis[1]

Cell Line: U937 leukaemia cells
Concentration: 1 and 5 μM
Incubation Time: 24 and 48 hours
Result: Blocked the cell cycle at the G1 phase in U937 leukaemia cells.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 1 and 5 μM
Incubation Time: 48 hours
Result: Down-regulates miRNAs with antiapoptotic activity including miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p.

Western Blot Analysis[1]

Cell Line: U937 cells
Concentration: 1 and 5 μM
Incubation Time: 48 hours
Result: Increased mRNA expression of p21, BAX and BAK and down-regulated cyclin D1 and BCL-2 in a dose-dependent manner.
分子量

436.51

Formula

C27H24N4O2

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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HDAC-IN-51
目录号:
HY-152173
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