EN4 是一种针对MYC的半胱氨酸 171 (C171) 的共价配体。EN4 对c-MYC的选择性高于 N-MYC 和 L-MYC。EN4 抑制 MYC 转录活性，下调 MYC 靶标，并具有抗肿瘤作用。
| 生物活性 | EN4 is a covalent ligand that targets cysteine 171 (C171) ofMYC. EN4 is selective forc-MYCover N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis[1]. |
体外研究
(In Vitro) | EN4 (1-50 μM; for 72 hours) treatment significantly impaires 231MFP breast cancer cell proliferation in a dosedependent manner, with >90% inhibition of proliferation at 50 μM[1].
EN4 (50 μM; for 60 hours) treatment significantly decreases the protein levels of representative MYC-regulated target genes, including CDK2 and CDC25A. EN4 treatment also substantially reduces MYC levels[1].
EN4 shows the strongest inhibition of both MYC/MAX binding to its DNA consensus sequence in vitro as well as MYC transcriptional activity in cells. EN4 inhibited MYC/MAX binding to the E-box response element DNA consensus sequence in a dose-responsive manner with an IC50 value of 6.7 μM. EN4 also inhibits MYC luciferase reporter activity in a dose-responsive manner with an IC50 value of 2.8 μM[1].
EN4 (50 μM; for 2 hours) treatment significantly reduced MYC thermal stability in 231MFP breast cancer cells[1].
Cell Proliferation Assay[1] | Cell Line: | 231MFP breast cancer cells | | Concentration: | 1 μM, 10 μM, 50 μM | | Incubation Time: | 72 hours | | Result: | Significantly impaired 231MFP breast cancer cell proliferation in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | 231MFP breast cancer cells | | Concentration: | 50 μM | | Incubation Time: | 60 hours | | Result: | The protein levels of CDK2 and CDC25A were significantly lowered. |
|
体内研究
(In Vivo) | EN4 (50 mg/kg; intraperitoneal injection; daily; for 3 weeks) treatment significantly attenuated tumor growth in 231MFP breast tumor xenograft mice[1].
| Animal Model: | SCID mice injected with 231MFP breast cancer cells[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal injection; daily; for 3 weeks | | Result: | Significantly attenuated tumor growth in vivo. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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(300.14 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.4011 mL | 12.0057 mL | 24.0113 mL | | 5 mM | 0.4802 mL | 2.4011 mL | 4.8023 mL | | 10 mM | 0.2401 mL | 1.2006 mL | 2.4011 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℃, 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 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (4.99 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.99 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 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.99 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.99 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.99 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本网站选购。
|
