生物活性分子抑制剂DIM-C-pPhOH

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DIM-C-pPhOH  纯度: 99.05%

DIM-C-pPhOH 是核受体 4A1 (NR4A1) 拮抗剂。DIM-C-pPhOH 抑制癌细胞的生长和 mTOR 信号传导，诱导细胞凋亡和细胞应激。DIM-C-pPhOH 可降低细胞增殖，对 ACHN 细胞和 786-O 细胞的 IC50 值分别为 13.6 μM 和 13.0 μM。

DIM-C-pPhOH

DIM-C-pPhOH Chemical Structure

CAS No. : 151358-47-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥558 In-stock
1 mg ￥500 In-stock
5 mg ￥750 In-stock
10 mg ￥950 In-stock
25 mg ￥1900 In-stock
50 mg ￥2900 In-stock
100 mg ￥4900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

DIM-C-pPhOH 相关产品

•相关化合物库:

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  • Apoptosis Compound Library
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  • Transcription Factor Targeted Library
  • Targeted Diversity Library

生物活性

DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively[1].

IC50 & Target

Nuclear receptor 4A1 (NR4A1)[1]
体外研究
(In Vitro)

DIM-C-pPhOH (7.5-20 μM; 24 hours; ACHN and 786-O cells) treatment significantly decreases cell proliferation[1].
DIM-C-pPhOH (20 μM; 24 hours; ACHN and 786-O cells) treatment induces Annexin V staining in ACHN and 786-O cells, confirming that DIM-C-pPhOH induce apoptosis, and also induces cleavage of caspases 7 and 8[1].
DIM-C-pPhOH (15-20 μM; 24 hours; ACHN and 786-O cells) treatment inhibits NR4A1-regulated expression of survivin, bcl-2 and EGFR in ACHN and 786-O cells. And also induces sestrin 2, activates AMPKα and inhibits activation of mTOR and downstream kinases[1].
DIM-C-pPhOH decreases expression of β1-integrin protein and mRNA and β1-integrin-dependent responses in MCF7, MDA-MB-231, and SKBR3 cells and also inhibits migration of the latter two cell lines[2].

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 Proliferation Assay[1]

Cell Line: ACHN and 786-O cells
Concentration: 7.5 μM, 15 μM, 20 μM
Incubation Time: 24 hours
Result: Significantly decreased cell proliferation.

Apoptosis Analysis[1]

Cell Line: ACHN and 786-O cells
Concentration: 20 μM
Incubation Time: 24 hours
Result: Induced apoptosis in ACHN and 786-O cells.

Western Blot Analysis[1]

Cell Line: ACHN and 786-O cells
Concentration: 15 μM, 20 μM
Incubation Time: 24 hours
Result: Inhibited NR4A1-regulated expression of survivin, bcl-2 and EGFR in ACHN and 786-O cells. And also induced sestrin 2, activated AMPKα and inhibited activation of mTOR and downstream kinases.

体内研究
(In Vivo)

DIM-C-pPhOH (30 mg/kg; oral gavage; daily; for 50 days; male athymic nude mice) treatment results in a significant inhibition of tumor growth[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: Male athymic nude mice (aged 6-7 weeks) injected with ACHN cells[1]
Dosage: 30 mg/kg/day
Administration: Oral gavage; daily; for 50 days
Result: Resulted in a significant inhibition of tumor growth.

分子量

338.40

Formula

C23H18N2O
CAS 号

151358-47-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (738.77 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9551 mL 14.7754 mL 29.5508 mL
5 mM 0.5910 mL 2.9551 mL 5.9102 mL
10 mM 0.2955 mL 1.4775 mL 2.9551 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。-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 (6.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.15 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 (6.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.15 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 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    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玉米油中，混合均匀。

*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]. Hedrick E, et al. Nuclear Receptor 4A1 (NR4A1) as a Drug Target for Renal Cell Adenocarcinoma. PLoS One. 2015 Jun 2;10(6):e0128308.

    [2]. Hedrick E, et al. NR4A1 Antagonists Inhibit β1-Integrin-Dependent Breast Cancer Cell Migration. Mol Cell Biol. 2016 Apr 15;36(9):1383-94.

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