DCH36_06

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

DCH36_06  纯度: 99.22%

DCH36_06 是一种有效的选择性 p300/CBP 抑制剂,对 p300CBPIC50 分别为 0.6 μM 和 3.2 μM。DCH36_06 介导的 p300/CBP 抑制导致白血病细胞中 H3K18 的低乙酰化。抗肿瘤活性。

DCH36_06

DCH36_06 Chemical Structure

CAS No. : 593273-05-3

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DCH36_06 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity[1].

体外研究
(In Vitro)

DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells[1].
DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner[1].
DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 6.7 μM, 20 μM
Incubation Time: 24 hours, 48 hours
Result: Dose-dependently arrested cell cycle at G1 phase.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 6.7 μM, 20 μM
Incubation Time: 24 hours, 48 hours
Result: Significantly induced apoptosis.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 5 μM, 10 μM
Incubation Time: 24 hours
Result: Significantly activated the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.

体内研究
(In Vivo)

DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MV4-11 xenograft nude mice[1]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Intraperitoneal injection; every two days; for 20 days
Result: The tumor growth rate showed significant reduction in dose-dependent manner.

分子量

372.83

Formula

C18H13ClN2O3S

CAS 号

593273-05-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 125 mg/mL (335.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6822 mL 13.4109 mL 26.8219 mL
5 mM 0.5364 mL 2.6822 mL 5.3644 mL
10 mM 0.2682 mL 1.3411 mL 2.6822 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (5.58 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.58 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Wenchao Lu, et al. Discovery and biological evaluation of thiobarbituric derivatives as potent p300/CBP inhibitors. Bioorg Med Chem. 2018 Nov 1;26(20):5397-5407.

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