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FKBP12 PROTAC dTAG-13

Chemical Structure : FKBP12 PROTAC dTAG-13

CAS No.: 2064175-41-1

FKBP12 PROTAC dTAG-13 (dTAG-13)

Catalog No.: PC-35859Not For Human Use, Lab Use Only.

FKBP12 PROTAC dTAG-13 (dTAG-13) is an in vivo-active heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells.

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Biological Activity

FKBP12 PROTAC dTAG-13 (dTAG-13) is an in vivo-active heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells.
dTAG-13 causes rapid degradation of nuclear and cytoplasmic FKBP12F36V fusion chimeras.
dTAG-13 displays an unexpected superior antiproliferative effect of pan-BET bromodomain degradation over selective BRD4 degradation, characterize immediate effects of KRASG12V loss on proteomic signaling, and demonstrate rapid degradation in vivo.

Physicochemical Properties

M.Wt 1049.184
Formula C57H68N4O15
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1R)-3-(3,4-dimethoxyphenyl)-1-(2-(2-((6-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)hexyl)amino)-2-oxoethoxy)phenyl)propyl (2S)-1-((S)-2-(3,4,5-trimethoxyphenyl)butanoyl)piperidine-2-carboxylate

References

1. Nabet B, et al. Nat Chem Biol. 2018 May;14(5):431-441.

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