dCBP-1 是一种基于Cereblon配体的p300/CBP的有效且选择性的异双功能降解剂。dCBP-1 在杀死多发性骨髓瘤细胞方面非常有效，并降低了驱动 MYC 表达的致癌增强子活性。
| 生物活性 | dCBP-1 is a potent and selective heterobifunctional degrader ofp300/CBPbased onCereblonligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression[1]. |
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体外研究
(In Vitro) | dCBP-1 (10-1000 nM; 6 hours) treatment shows near-complete degradation of p300/CBP in MM1S cells. dCBP-1 is also able to induce near-complete p300/CBP degradation across other multiple myeloma cell lines tested, including MM1R, KMS-12-BM, and KMS34[1].
Treatment of the human haploid cell line HAP1 for 6 h with dCBP-1 reveals almost complete loss of both CBP and p300 between 10 and 1000 nM doses. A time course analysis with 250 nM dCBP-1 revealed almost complete degradation of p300/CBP within an hour of treatment[1].
Western Blot Analysis[1] | Cell Line: | Multiple myeloma cell line MM1S | | Concentration: | 10 nM, 100 nM, 250 nM, 500 nM, 1000 nM | | Incubation Time: | 6 hours | | Result: | Revealed rapid degradation with near-complete loss of p300/CBP after 2 hours. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(48.63 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 0.9727 mL | 4.8633 mL | 9.7266 mL | | 5 mM | 0.1945 mL | 0.9727 mL | 1.9453 mL | | 10 mM | 0.0973 mL | 0.4863 mL | 0.9727 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 (sealed storage, away from moisture and 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% (20%SBE-β-CDin saline) Solubility: 5 mg/mL (4.86 mM); Clear solution; Need ultrasonic
此方案可获得 5 mg/mL (4.86 mM) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 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。 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.86 mg/mL (2.78 mM); Clear solution
此方案可获得 ≥ 2.86 mg/mL (2.78 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 28.6 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。 *以上所有助溶剂都可在本网站选购。
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