2365116-48-7
Chemical Structure
dTAG-Fluorescein
- CAS No.: 2365116-48-7
- Formula:C59H60N2O15
- Molecular Weight:1037.11
InChIKey: PYSNCVLWRQOZJE-UWPQOEEGSA-N
SMILES: O=C1OC2(C3=CC=C(O)C=C3OC4=CC(O)=CC=C42)C5=CC(C(NCCOC6=CC([C@@H](CCC7=CC(OC)=C(C=C7)OC)OC([C@H]8N(CCCC8)C([C@H](C9=CC(OC)=C(C(OC)=C9)OC)CC)=O)=O)=CC=C6)=O)=CC=C51
Biological Activity: dTAG-Fluorescein is a dTAG-class PROTAC conjugated with fluorescein. dTAG-Fluorescein is applicable to homogeneous time-resolved fluorescence (HTRF) competitive displacement binding assays to detect binding affinity with His-FKBP12F36V. dTAG-Fluorescein can recruit VHL or CRBN E3 ligase complexes, thereby specifically driving the selective degradation of FKBP12F36V-tagged proteins, with very limited activity against FKBP12WT and IKZF1[1][2][3][4][5].
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dTAG-Fluorescein | dTAG-Fluorescein is a dTAG-class PROTAC conjugated with fluorescein. dTAG-Fluorescein is applicable to homogeneous time-resolved fluorescence (HTRF) competitive displacement binding assays to detect binding affinity with His-FKBP12F36V. dTAG-Fluorescein can recruit VHL or CRBN E3 ligase complexes, thereby specifically driving the selective degradation of FKBP12F36V-tagged proteins, with very limited activity against FKBP12WT and IKZF1. | |||||||||||||||||||||
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References
- [1]. Islam S, et al. A Tandem-Affinity Purification Method for Identification of Primary Intracellular Drug-Binding Proteins. ACS Chem Biol. 2024;19(2):233-242. [Content Brief]
- [2]. Li S, et al. Systematic investigation of BRCA1-A,-B, and-C complexes and their functions in DNA damage response and DNA repair[J]. Oncogene, 2024, 43(35): 2621-2634.
- [3]. Nabet B, et al. Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules. Nat Commun. 2020;11(1):4687. Published 2020 Sep 18. [Content Brief]
- [4]. Yenerall P, et al. Use of the dTAG system in vivo to degrade CDK2 and CDK5 in adult mice and explore potential safety liabilities. Toxicol Sci. 2023;194(1):53-69. [Content Brief]
- [5]. Nabet B, et al. The dTAG system for immediate and target-specific protein degradation. Nat Chem Biol. 2018;14(5):431-441. [Content Brief]
