RBPJ Inhibitor-1
产品说明书
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同义名 : | RIN1 |
| CAS号 : | 2682114-39-0 | |
| 货号 : | A1340414 | |
| 分子式 : | C17H14FN3O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 311.31 | |
| MDL号 : | MFCD32856863 | |
| 存储条件： |
Pure form Inert atmosphere,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 250 mg/mL(803.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | NOTCH proteins are trans-membrane receptors that transduce signals from cell-bound JAGGED (JAG) and Delta-like (DLL) families of ligands to mediate cell-cell interactions in processes as diverse as fetal development, heart disease and cancer. NOTCH is cleaved by γ-secretase after activation to release an intracellular domain (NICD) that binds the transcriptional effector RBPJ. RBPJ inhibitor-1 (RIN1) is the first inhibitor of RBPJ which potently disrupts the functional interaction of RBPJ with NOTCH. RIN1 inhibited Hes1-Luciferase, NOTCH3 ICD and RBPJ-VP16-dependent Hes1-Luciferase with IC50s of 0.18, 0.19, and 0.2 µM and Emaxs of 82%, 88% and 81%, respectively. RIN1 (2 µM) decreased RBPJ-VP16-dependent Hes1-Luciferase activity and caused a corresponding decrease in Luciferase reporter mRNA and endogenous RBPJ target gene expression mRNAs. RIN1 decreased cell proliferation in Jurkat, Koptk-1 and Rec-1 cancer cell lines. RIN1 (0.6 µM) decreased the number of MHC+ cells and increased the number of nuclei per cell, indicating that it induced the formation of multinucleated myofibers[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.21mL 0.64mL 0.32mL |
16.06mL 3.21mL 1.61mL |
32.12mL 6.42mL 3.21mL |
| 参考文献 |
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