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HDAC1-IN-5

产品编号 T61433

HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]

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HDAC1-IN-5

HDAC1-IN-5, CAS N/A

规格	价格/CNY	货期
25 mg	￥ 10,600	10-14周
50 mg	￥ 13,800	10-14周
100 mg	￥ 17,500	10-14周

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生物活性

化学信息

存储 & 溶解度

产品描述	HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]
体外活性	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]. 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 IC 50 s 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.
体内活性	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]. Animal Model: C57BL/6 mice (6-10 weeks; 2×10 6 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
分子式	C20H21N3O2S

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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