eEF2K degrader C1

Chemical Structure : eEF2K degrader C1

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货号: PC-21794Not For Human Use, Lab Use Only.

eEF2K degrader C1 is a small-molecule degrader of eEF2K, acts a molecular glue to enhance the interaction of eEF2K with the ubiquitin E3 ligase βTRCP, thereby promoting the proteasomal degradation of eEF2K.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote

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生物&药学活性

eEF2K degrader C1 is a small-molecule degrader of eEF2K, acts a molecular glue to enhance the interaction of eEF2K with the ubiquitin E3 ligase βTRCP, thereby promoting the proteasomal degradation of eEF2K.
C1 decreases the level of eEF2K protein in a dose‐dependent manner in TNBC cells, with no significant effect on eEF2K mRNA levels.
MG132, a proteasome inhibitor, blocks the down regulation of eEF2K induced by C1.
C1 enhances the interaction between eEF2K and the ubiquitin E3 ligase βTRCP, MLN4924 remarkedly reverses C1 induced down regulation of eEF2K.
C1 significantly inhibits cell proliferation of MDA‐MB‐231, HCC1806, and BT549 cells with IC50 values of 0.131, 0.342, and 0.262 uM respectively.
C1 treatment (0.4 uM) remarkably inhibits the cell migration and invasion of TNBC cells in wound healing and transwell assays.
C1 shows stronger anti‐cancer activity than paclitaxel, C1 (10 mg/kg) inhibits TNBC growth in mouse xenograft models, also suppresses cell metastasis in the in vivo model.
C1 with paclitaxel synergistically inhibits the growth of TNBC cells in vitro and in vivo.

物理化学性质&存储条件

分子量	508.55
分子式	C27H29FN4O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	ethyl 1-(2-(3,4-dimethylphenyl)-4-(3-fluorobenzyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonyl)piperidine-3-carboxylate

参考文献

1. Zhong C, et al. Adv Sci (Weinh). 2024 Feb;11(5):e2305035.