FKBP12 PROTAC dTAG-13(Synonyms: dTAG-13)

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FKBP12 PROTAC dTAG-13 (Synonyms: dTAG-13) 纯度: 99.52%

FKBP12 PROTAC dTAG-13 (dTAG-13) 是一种基于 PROTAC 的双功能降解剂，可降解 FKBP12F36V。FKBP12 PROTAC dTAG-13 有效地接合 FKBP12F36V 和 CRBN，从而选择性地降解 FKBP12F36V。

FKBP12 PROTAC dTAG-13(Synonyms: dTAG-13)

FKBP12 PROTAC dTAG-13 Chemical Structure

CAS No. : 2064175-41-1

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FKBP12 PROTAC dTAG-13 相关产品

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生物活性

FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12F36V and CRBN, thereby selectively degrading FKBP12F36V[1].

IC50 & Target[1]

Cereblon

 

FKBP12(F36V)

 

体外研究
(In Vitro)

TAG-13 (1-1000 nM; 4 hours; 293FTWT cells) treatment potently reduces FKBP12F36V-Nluc levels in 293FTWT cell, indicating the requirement of CRBN for the observed effects[1].
Treatment of MV4;11 cells expressing BRD4(short)-FKBP12F36V 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 FKBP12WT[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: 293FTWT cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 4 hours
Result: Potently reduced FKBP12F36V-Nluc levels in 293FTWT cell.

体内研究
(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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1049.17

Formula

C57H68N4O15
CAS 号

2064175-41-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 180 mg/mL (171.56 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.9531 mL 4.7657 mL 9.5313 mL
5 mM 0.1906 mL 0.9531 mL 1.9063 mL
10 mM 0.0953 mL 0.4766 mL 0.9531 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Nabet B, et al. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018 May;14(5):431-441.

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