Bioactivity | PT-179 is an orthogonal Thalidomide (HY-14658) derivative that targets cereblon without causing off-target degradation effects. PT-179 is able to specifically bind CRBN, form a ternary complex with a target protein fused to a zinc finger (ZF) degron, and mediate the degradation of the tagged protein. For example, PT-179 binds to the ubiquitin ligase substrate receptor cereblon by forming a complex with SD40 and efficiently degrades proteins N- or C-terminally fused to SD40 or SD36 (DC50 for eGFP: 4.5 nM and 14.3 nM). PT-179 can be used to develop compact protein degradation tagging platforms[1]. | ||||||||||||
Invitro | SD40 是 PT-179 特异性的降解标签。PT-179 (1-10 μM; 24 h) 能在 HEK293T 细胞中诱导 eGFP 降解,降解决定子变体的进化程度越高,引起对应标记蛋白的降解效力越强[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PT-179 相关抗体: | ||||||||||||
CAS | 2924858-25-1 | ||||||||||||
Formula | C17H17N3O5 | ||||||||||||
Molar Mass | 343.33 | ||||||||||||
Appearance | 固体 | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Mercer JAM, et al. Continuous evolution of compact protein degradation tags regulated by selective molecular glues. Science. 2024 Mar 15;383(6688):eadk4422. |