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FKBP12 PROTAC dTAG-13

CAS No. : 2064175-41-1

MCE 站：FKBP12 PROTAC dTAG-13

产品活性：FKBP12 PROTAC dTAG-13 (dTAG-13) 是一种基于 PROTAC 的双功能降解剂。FKBP12 PROTAC dTAG-13 (dTAG-13) 既是一种 FKBP12^F36V 的降解剂，又是一种选择性的 BET BRD4 降解剂，FKBP12 PROTAC dTAG-13 (dTAG-13) 通过将 BET 溴结构域桥接至 E3 泛素连接酶 (cereblon; CRBN) 而形成降解剂。

研究领域：PROTAC  |  Autophagy  |  Apoptosis  |  Immunology/Inflammation  |  Epigenetics

作用靶点：PROTAC  |  FKBP  |  Epigenetic Reader Domain

In Vitro: TAG-13 (1-1000 nM; 4 hours; 293FT^WT cells) treatment potently reduces FKBP12^F36V-Nluc levels in 293FT^WT cell, indicating the requirement of CRBN for the observed effects.
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12^F36V with dTAG-13 leads to robust degradation of BRD4. dTAG-13 treatment leads to rapid degradation of BRD4 within one hou. dTAG-13 treatment leads to rapid and potent degradation of the BRD4 fusion chimera in the heterozygous and homozygous knock-in clones, with no effect on endogenous FKBP12^WT.

In Vivo: Following bone marrow engraftment of MV4;11 cells expressing luc-FKBP12F36V in mice, the bioluminescent signal after vehicle or dTAG-13 administration is monitored. A significant, rapid, and durable effect on bioluminescent signal is observed four hours after dTAG-13 administration, indicating effective degradation of luc-FKBP12F36V. Twenty-eight hours following the final treatment, the recovery of cellular bioluminescence to levels comparable between vehicle and dTAG-13 treatment groups is observed.

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