2. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  3. HDAC Microtubule/Tubulin Caspase Apoptosis
  4. HDAC1-IN-5

HDAC1-IN-5 是一种有效的 HDAC1 抑制剂，对 HDAC1 和HDAC6 的 IC50 分别为 15 nM 和 20 nM。HDAC1-IN-5 可增强癌细胞中组蛋白 H3 和 α-微管蛋白 (α-tubulin) 的乙酰化，促进 caspase 3 的活化，从而诱导细胞凋亡 (apoptosis)。HDAC1-IN-5 通过与 DNA 结合诱导染色质损伤。HDAC1-IN-5 在异种移植瘤小鼠中表现出较强的肿瘤生长抑制活性。

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HDAC1-IN-5 Chemical Structure

HDAC1-IN-5 Chemical Structure

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HDAC1-IN-5 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HDAC1-IN-5 is a potent HDAC1 inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice[1].

IC50 & Target[1]

HDAC1

15 nM (IC50)

HDAC6

20 nM (IC50)

体外研究
(In Vitro)

HDAC1-IN-5 (compound 4j) (0-50 μM; 48 h) exhibits strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL[1].
HDAC1-IN-5 (0.16-1.5 μM; 48 h) induces apoptosis in a dose-dependent manner[1].
HDAC1-IN-5 (0.17-1.5 μM; 24 h or 48 h) induces downregulation of SPT16 and SSRP-1, induces the cleavage of caspase-3, and increases the expression of Acetyl-Histone H3 and Acetyl-α-tubulin[1].

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

HDAC1-IN-5 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HCT116, HeLa, HepG2, MC38, K562 and HEL
Concentration: 0-50 μM
Incubation Time: 48 h
Result: Showed strong inhibitory effects on HCT116, HeLa, HepG2, MC38, K562 and HEL with IC50s of 0.47 μM, 0.78 μM, 1.4 μM, 0.43 μM, 0.91 μM and 0.28 μM, respectively.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 0.16 μM, 0.5 μM and 1.5 μM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner, and induced 38.5% at the concentration of 1.5 μM (both early and late apoptotic cells).

Western Blot Analysis[1]

Cell Line: HCT116 and MC38
Concentration: 0.17 μM, 0.5 μM and 1.5 μM
Incubation Time: 24 h or 48 h
Result: Induced downregulation of SPT16 and SSRP-1 in HCT116.
Induced the cleavage of caspase-3 in HCT116 and MC38.
Increased the expression of HDAC1, 2, 6 substrate Acetyl-Histone H3 and Acetyl-α-tubulin with a dose-dependent manner.
体内研究
(In Vivo)

HDAC1-IN-5 (50 and 100 mg/kg; IP; every two days; for 16 days) significantly decreases the tumor volume and weight in MC38 xenograft mice[1].

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

Animal Model: C57BL/6 mice (6-10 weeks; 2×106 MC38 cells were injected subcutaneously into the right flank regions)[1]
Dosage: 50 and 100 mg/kg
Administration: IP; every two days; for 16 days
Result: Significantly decreased the tumor volume and weight with tumor growth inhibition (TGI) of 66% at 50 mg/kg.
分子量

367.46

Formula

C20H21N3O2S
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

HDAC1-IN-5 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:

HDAC1-IN-5HDACMicrotubule/TubulinCaspaseApoptosisHistone deacetylasesanticancerHCT116MC38tumor growthC57BL/6 miceInhibitorinhibitorinhibit

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