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My CartCAS：1950634-92-0
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 1950634-92-0 |
| Name | DBET 6 |
| Molecular Formula | C42H45ClN8O7S |
| Molecular Weight | 841.37 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD31692407 |
| SMILES | O=C(NCCCCCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4 |
| Target Point | BRD4 |
| Passage | Epigenetics |
| Background | DBET6 is a BET bromodomains PROTAC degrader. |
| Biological Activity | 是一种具有良好的细胞通透性的BET bromodomainsPROTAC降解剂，与BRD4结合的IC50值为14 nM。dBET6 还可诱导c-MYC的下调和凋亡。[1] |
| In Vitro | dBET6是一种具有高细胞透性的BET溴区降解剂。它在大多数癌细胞系中都有效。dBET6在低于纳摩尔级别的浓度下，在细胞中具有明显的降解效果。对细胞处理100 nM dBET6，1小时后，BRD4降解并促进c-Myc的下调和诱导凋亡。dBET6破坏整体高效的转录延伸，可造成稳态mRNA水平大范围地降低。BET降解所引起的核心转录机器的瓦解导致强烈的凋亡反应[1]。 |
| In Vivo | dBET6耐受性良好。在弥散性T-ALL小鼠模型中，dBET6可引起白血病负荷显著减少。此外，给小鼠每日两次dBET6给药(7.5 mg/kg)，相对于对照组小鼠和处理了JQ1(20 mg/kg QD)的小鼠，dBET6的处理有利于小鼠生存[1]。 |
| Cell Experiment | 用不同浓度的dBET1或dBET6处理细胞，处理3小时。通过离心收集细胞，用PBS洗涤一次，然后转移至PCR管内。快速离心，在47.5℃下孵育3分钟，25℃孵育3分钟，然后加入30 μL lysis buffer裂解溶解细胞。用液氮进行冻融循环，循环3次。[1] |
| Animal Experiment | Animal Models: 雄性CD-1小鼠;Dosages: 10 mg/kg;Administration: i.p.[1] |
| Data Literature Source | [1] Winter GE，et al. Mol Cell. 2017，67(1):5-18.e19. |
| Unit | Bottle |
| Specification | 5mg 10mg |
DBET6是一种BET bromodomainsPROTAC降解剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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