2. Cell Cycle/DNA Damage Epigenetics Apoptosis Immunology/Inflammation
  3. HDAC Apoptosis Pyroptosis
  4. HDAC1/6-IN-3

HDAC1/6-IN-3 是一种强效的 HDAC 抑制剂。HDAC1/6-IN-3 对 HDAC1 (IC50 = 1.1 nM) 和 HDAC6 (IC50 = 2.7 nM) 具有出色的抑制作用。HDAC1/6-IN-3 能显著使 HepG2 细胞停滞在 G0/G1 期，并诱导细胞凋亡 (apoptosis) 和细胞焦亡 (pyroptosis)。HDAC1/6-IN-3 在 HepG2 肿瘤移植模型中显示出显著的抗肿瘤活性。HDAC1/6-IN-3 可用于癌症研究，如肝癌、肺癌、结肠癌、乳腺癌。

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HDAC1/6-IN-3

HDAC1/6-IN-3 Chemical Structure

CAS No. : 3038691-85-6

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HDAC1/6-IN-3 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

HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer[1].

IC50 & Target[1]

HDAC1

1.1 nM (IC50)

HDAC6

2.7 nM (IC50)

体外研究
(In Vitro)

HDAC1/6-IN-3 (Compound 15a) (72 h) 对 HepG2 (IC50 = 0.12 μM)、PC9 (IC50 = 0.53 μM)、HCT116 (IC50 = 1.12 μM) 和 MCF7细胞 (IC50 = 3.12 μM) 显示出优异的抑制活性[1]。
HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) 以剂量依赖性方式提高 HepG2 细胞中 acetyl-H3 和 H4 的水平[1]。
HDAC1/6-IN-3 (0.2-0.5 μM, 10-14 d) 以剂量依赖性方式抑制 HepG2 细胞的集落形成[1]。
HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) 诱导 HepG2 细胞发生 G0/G1 期阻滞，这可能与 CDK4 和 Cyclin D1 蛋白的下调相关[1]。
HDAC1/6-IN-3 (0.2-0.5 μM, 48 h) 通过增强 ROS 生成和 DNA 损伤积累来诱导 HepG2 细胞凋亡[1]。
HDAC1/6-IN-3 (0.2-0.5 μM, 24-48 h)通过 caspase-3 对 GSDME 的切割触发HepG2 细胞焦亡[1]。

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

HDAC1/6-IN-3 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: Significantly inhibited HepG2 cells in G0/G1 phase in a dose-dependent manner.
The G2/M ratio decreased from 25.34 to 22.85% and the S-phase value decreased from 32.99 to 13.72%.

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 48 h
Result: Induced apoptosis in 28.2% at 0.2 µM and 46.5% at 0.5 µM.

Immunofluorescence[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: The ROS levels were dose-dependently increased.
Showed dose-dependent γH2AX foci formation.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.2 and 0.5 μM
Incubation Time: 24 h
Result: increased the level of acetyl-H3 and H4 in a dose-dependent manner.
Down-regulated the expression of Cyclin D1 and CDK4.
Upregulated the expression of Cl-PARP, Cl-caspase 3 in a dose-dependent manner.
Resulted in elevated levels of the N-terminal fragment of gasdermin E (GSDME) and caspase-3.
体内研究
(In Vivo)

HDAC1/6-IN-3 (Compound 15a) (10 mg/kg, i.p., 1 周 2 次, 共 3 周) 在 HepG2 异种移植模型中显示出显著的抗肿瘤功效，以及可接受的安全性特征[1]。

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

Animal Model: HepG2 induced xenograft model established in male BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), twice a week for 3 weeks
Result: The growth of tumors was dose-dependently inhibited. A dose-dependent reduction in Ki67 immunostaining was observed. Induced the increase of Ac- H3/H4､Cl-caspase3 and GSDME-N in a dose-dependent manner.
分子量

453.55

Formula

C24H27N3O4S
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

HDAC1/6-IN-3 相关分类

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  • 稀释计算器

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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:

HDAC1/6-IN-33038691-85-6HDACApoptosisPyroptosisHistone deacetylasesHistone deacetylase inhibitorThiazoleHydroxamateAnticancerHepG2 cellsInhibitorinhibitorinhibit

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