NVS-CECR2-1

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NVS-CECR2-1  纯度: ≥99.0%

NVS-CECR2-1 是一种非 BET 家族的 Bromodomain (BRD) 抑制剂，是一种有效的，选择性的猫眼综合征染色体区域候选物 2 (CECR2) 抑制剂。NVS-CECR2-1 以高亲和力结合 CECR2 BRD (IC50=47 nM; KD=80 nM)。NVS-CECR2-1 表现出癌细胞毒性作用，并通过靶向 CECR2 以及非 CECR2 依赖性机制诱导癌细胞的凋亡。

NVS-CECR2-1

NVS-CECR2-1 Chemical Structure

CAS No. : 1992047-61-6

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5 mg ￥6500 In-stock
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生物活性

NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism[1].

IC50 & Target[1]

CECR2

47 nM (IC50)

CECR2

80 nM (Kd)

BRD4

>37 μM (IC50)

BRD7

5.5 μM (IC50)

BRD9

2.3 μM (IC50)

体外研究
(In Vitro)

NVS-CECR2-1 (1-4 μM; 72 hours) decreases the viability of all cancer cells[1].
NVS-CECR2-1 (1-6 μM; 72 hours) increases apoptosis in a dose-dependent manner[1].
NVS-CECR2-1 (10 μM; 2 hours) inhibits chromatin binding of CECR2 BRD within SW48 cells. NVS-CECR2-1 (5, 10, 15 μM; 2 hours) dissociates CECR2 from chromatin in a dose-dependent manner without affecting BRG1[1].
NVS-CECR2-1 (0.5-4 μM; 10 days) inhibits the clonogenic ability of SW48 cells in a dose dependent manner and its IC50 value is estimated to be 0.64 μM[1].
NVS-CECR2-1 inhibits chromatin binding of CECR2 BRD and displaces CECR2 from chromatin within cells[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 Viability Assay[1]

Cell Line: Colon (SW48, HT29 and HCT116), lung (H460), uroepithelium (SV-HUC-1), cervix (HeLa) and bone (U2OS), human embryonic kidney (HEK) 293 T cells
Concentration: 1, 1.5, 2, 2.5, 3, 4 μM
Incubation Time: 72 hours
Result: Decreased the viability of all cancer cells analyzed in a dose dependent manner.
Showed a dose-dependent cytotoxicity on HEK 293 T cells.

Apoptosis Analysis[1]

Cell Line: SW48 cells
Concentration: 0.5, 1, 1.5, 2, 4, 6 μM
Incubation Time: 72 hours
Result: Increased apoptosis in a dose-dependent manner, with more than 80% cells undergoing apoptosis at 6 μM, and had virtually no effect on necrosis.

分子量

495.68

Formula

C27H37N5O2S
CAS 号

1992047-61-6
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 : 66.67 mg/mL (134.50 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0174 mL 10.0872 mL 20.1743 mL
5 mM 0.4035 mL 2.0174 mL 4.0349 mL
10 mM 0.2017 mL 1.0087 mL 2.0174 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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.04 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 25.0 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]. Seul Gi Park, et al. Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells. Sci Rep. 2020 Oct 1;10(1):16330.

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