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。
| 生物活性 | NVS-CECR2-1, a non-BET familyBromodomain (BRD)inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds toCECR2BRD with high affinity (IC50=47 nM;KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and inducesapoptosisagainst variouscancercells by targetingCECR2as 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) |
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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 IC50value 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].
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. |
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| 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 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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本网站选购。 |
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