2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC-IN-47

HDAC-IN-47 是一种具有口服活性的组蛋白去乙酰化酶 (HDAC) 的抑制剂，IC50 分别为 19.75 nM (HDAC1)，5.63 nM (HDAC6)，40.27 nM (HDAC3)，57.8 nM (HDAC2)，302.73 nM (HDAC8)。HDAC-IN-47 能抑制细胞自噬，并通过 Bax/Bcl-2 和 caspase-3 通路诱导凋亡 (apoptosis)。HDAC-IN-47 能够在G2/M期阻滞细胞周期，并在体内表现出抗肿瘤作用。

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HDAC-IN-47

HDAC-IN-47 Chemical Structure

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HDAC-IN-47 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-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo[1].

IC50 & Target[1]

HDAC1

19.75 nM (IC50)

HDAC6

5.63 nM (IC50)

HDAC3

40.27 nM (IC50)

HDAC2

57.8 nM (IC50)

HDAC8

302.73 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.24 μM
Compound: 21
Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
HL-60 IC50
0.22 μM
Compound: 21
Anticancer activity against human HL-60 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human HL-60 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
HepG2 IC50
0.16 μM
Compound: 21
Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
MDA-MB-238 IC50
0.45 μM
Compound: 21
Anticancer activity against human MDA-MB-238 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
Anticancer activity against human MDA-MB-238 cells assessed as cell growth inhibition measured after 72 hrs by CCK-8 staining based microplate reader analysis
[PMID: 36215854]
体外研究
(In Vitro)

HDAC-IN-47 (compound 21) shows antiproliferative activity and inhibits A549 cell growth with an IC50 value of 0.24 μM[1].
HDAC-IN-47 (0.5 and 1 μM; 72 h) exhibits profound G2/M arrest in A549 cells and induces cell apoptosis[1].
HDAC-IN-47 (0.1 and 0.5 μM; 24 h) increases the expression levels of Bax and Caspase3, decreases the level of Bcl-2, activates the intrinsic (mitochondrial) apoptotic pathway[1].

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

HDAC-IN-47 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2, MDA-MB-238, HL-60 cells
Concentration: 0.16-0.45 μM
Incubation Time: 72 hours
Result: Inhibited cancer cells with IC50s of 0.16 μM (HepG2), 0.45 μM (MDA-MB-238), 0.22 μM (HL-60), respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 and 1 μM
Incubation Time: 24 hours
Result: Induced marked arrest of cells in the G2/M phase of 28.38% (0.5 μM) and 31.70% (1.0 μM).

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 0.5 and 1 μM
Incubation Time: 24 hours
Result: Resulted 21.09% (0.5 μM) and 30.58% (1 μM) apoptotic cells.
体内研究
(In Vivo)

HDAC-IN-47 (compound 21) (50, and 100 mg/kg; p.o.; once daily; 18 d) exhibits significant antitumor activity in a dosedependent manner without no significant body weight loss in A549 xenograft mouse model[1].

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

Animal Model: A549 xenograft model in mouse (female, BALB/c nu/nu mice, 6-8 weeks old)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: Oral gavage; once daily; for 18 consecutive days
Result: Decreased the tumor volume and weight by 48% and 45%, respectively.
分子量

410.26

Formula

C17H20BrN3O4
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-47 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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-47HDACHistone deacetylasesantiproliferativeanti-tumorarrests cell cycleG2/MHepG2MDA-MB-238HL-60A549Inhibitorinhibitorinhibit

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目录号：
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