2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. HDAC-IN-89

HDAC-IN-89 是 HDAC1 (IC50: 0.95 nM)、HDAC2 (IC50: 0.86 nM)、HDAC3 (IC50: 1.06 nM)和 HDAC8 (IC50: 4.24 nM) 的抑制剂。HDAC-IN-89 可阻断细胞周期和诱导细胞凋亡 (apoptosis)。HDAC-IN-89 具有抗肿瘤活性。

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HDAC-IN-89 Chemical Structure

HDAC-IN-89 Chemical Structure

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HDAC-IN-89 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-89 is an inhibitor of HDAC1 (IC50: 0.95 nM), HDAC2 (IC50: 0.86 nM), HDAC3 (IC50: 1.06 nM) and HDAC8 (IC50: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity[1].

IC50 & Target[1]

HDAC1

0.95 nM (IC50)

HDAC2

0.86 nM (IC50)

HDAC3

1.06 nM (IC50)

HDAC8

4.24 nM (IC50)

HDAC6

>1000 nM (IC50)

体外研究
(In Vitro)

HDAC-IN-89 (Compound 12) (0-10000 nM，72 小时) 对 NCI-H1975 (IC50: 0.57 μM) 和 HT-29 (IC50: 0.17 μM) 两种癌细胞均表现细胞毒性，但在 WRL-68 (IC50: 2.6 μM) 和 HEK293 (IC50: 1.0 μM) 两种正常细胞中毒性明显降低[1]。
HDAC-IN-89 (250 nM-1 μM，48 小时) 诱导HT-29细胞系周期停滞于 G0/G1 期，并在相应浓度下显著促进早期细胞和晚期细胞凋亡[1]。
HDAC-IN-89 (0-40 μM) 对 hERG 钾通道的抑制作用小 (21%)，表明心脏毒性风险低[1]。
HDAC-IN-89 (0.1 μM，7-60 分钟)在小鼠、大鼠和人肝微粒体中均表现出中等代谢稳定性 (MF%: 30%-70%) 和较快的清除率(Clint: 21.7-43.7 mL/min/g)[1]。

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

HDAC-IN-89 相关抗体:

Cell Viability Assay[1]

Cell Line: Tumor cells (NCI-H1975 cells, HT-29 cells) and normal cells (WRL-68 cells, HEK293 cells)
Concentration: 0-10000 nM
Incubation Time: 72 h
Result: Inhibited the activity of two cancer cells, NCI-H1975 (IC50: 0.57 μM) and HT-29 (IC50: 0.17 μM).
Reduced the toxicity to two normal cells, WRL-68 (IC50: 2.6 μM) and HEK293 (IC50: 1.0 μM).

Cell Cycle Analysis[1]

Cell Line: HT-29 cells
Concentration: 250 nM, 500 nM and 1μM
Incubation Time: 48 h
Result: Induced cell cycle arrest in HT-29 cells at the G0/G1 phase (%G0/G1: 55.0%/57.2%/74.0%).

Apoptosis Analysis[1]

Cell Line: HT-29 cells
Concentration: 250 nM and 500 nM
Incubation Time: 48 h
Result: Promoted apoptosis of early cells (14.3%/19.7%) and late cells (7.57%/11.1%) at the corresponding concentrations (250 nM/500 nM).
体内研究
(In Vivo)

HDAC-IN-89 (Compound 12 ) (2.2 mg/kg 和 11 mg/kg，腹腔注射，每 3 天 1 次，21 天) 可抑制小鼠 NCI-H1975 异种移植模型中肿瘤的生长 (63.5% 和 87.9%)，并表现较低毒性[1]。

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

Animal Model: NCI-H1975 xenograft model[1]
Dosage: 2.2 mg/kg and 11 mg/kg
Administration: Intraperitoneal injection (i.p.), once every 3 days for 21 days
Result: Inhibited tumor growth (63.5% and 87.9%).
Had no significant changes in body weight compared to the same dose of Romidepsin (2.2 mg/kg).
分子量

575.69

Formula

C24H35F2N5O5S2
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-89 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-89HDACHistone deacetylasesAnti-tumorNCI-H1975HT-29hERG potassium channelNCI-H1975 xenograft modelInhibitorinhibitorinhibit

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目录号：
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