1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. HDAC-IN-76

HDAC-IN-76 (compound 6i) 是一种组蛋白去乙酰化酶 (HDAC) 抑制剂。HDAC-IN-76 对 Pf3D7 (chloroquine (HY-17589A) 药敏品系) 和 PfDd2 (chloroquine (HY-17589A) 耐药品系) 的 IC50 分别为 30 nM 和 98 nM, 对无性血期疟原虫具有高效抗疟活性,并表现出对寄生虫的选择性抑制,对人 HDAC1HDAC6IC50 分别为 7 nM 和 9 nM,同时抑制 PfHDAC1。

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HDAC-IN-76 Chemical Structure

HDAC-IN-76 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1[1].

IC50 & Target

hHDAC1

7 nM (IC50)

hHDAC6

9 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-76 对 HEK293 细胞毒性低[1]
HDAC-IN-76 (1 μM) 有效抑制 PfHDAC1,抑制率为 70.2%[1]
HDAC-IN-76 对肝期寄生虫活性较低 (IC50 PbEEF (伯氏疟原虫红细胞外肝期寄生虫)=0.25 μM),具有良好的微粒体稳定性 (t1/2 > 60 min),并在 HEK293 细胞中的毒性较低 (IC50=136 μM,选择指数 SI=544)[1]
HDAC-IN-76 能够有效进入 HepG2 细胞,抑制 HDAC 活性[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: HEK293
Concentration: 1%
Incubation Time: 24 h
Result: Had low cytotoxicity to HEK293 cells.
分子量

470.52

Formula

C27H26N4O4

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
  • 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.

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Inquiry Information

产品名称:
HDAC-IN-76
目录号:
HY-161984
需求量: