FKBP12 PROTAC dTAG-13

Modify Date: 2024-01-15 19:17:19

FKBP12 PROTAC dTAG-13 Structure
FKBP12 PROTAC dTAG-13 structure
Common Name FKBP12 PROTAC dTAG-13
CAS Number 2064175-41-1 Molecular Weight 1049.168
Density 1.3±0.1 g/cm3 Boiling Point 1134.0±65.0 °C at 760 mmHg
Molecular Formula C57H68N4O15 Melting Point N/A
MSDS N/A Flash Point 639.6±34.3 °C

 Use of FKBP12 PROTAC dTAG-13


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; causes rapid degradation of nuclear and cytoplasmic FKBP12F36V fusion chimeras, and 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.

 Names

Name (1R)-3-(3,4-Dimethoxyphenyl)-1-(2-{2-[(6-{[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}hexyl)amino]-2-oxoethoxy}phenyl)propyl (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]-2-piperidinecarboxylate
Synonym More Synonyms

 FKBP12 PROTAC dTAG-13 Biological Activity

Description 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; causes rapid degradation of nuclear and cytoplasmic FKBP12F36V fusion chimeras, and 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.
References References 1. Nabet B, et al. Nat Chem Biol. 2018 May;14(5):431-441. View Related Products by Target PROTAC

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 1134.0±65.0 °C at 760 mmHg
Molecular Formula C57H68N4O15
Molecular Weight 1049.168
Flash Point 639.6±34.3 °C
Exact Mass 1048.468140
LogP 6.98
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.581

 Synonyms

(1R)-3-(3,4-Dimethoxyphenyl)-1-(2-{2-[(6-{[2-(2,6-dioxo-3-piperidinyl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]oxy}hexyl)amino]-2-oxoethoxy}phenyl)propyl (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]-2-piperidinecarboxylate
2-Piperidinecarboxylic acid, 1-[(2S)-1-oxo-2-(3,4,5-trimethoxyphenyl)butyl]-, (1R)-3-(3,4-dimethoxyphenyl)-1-[2-[2-[[6-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]hexyl]amino]-2-oxoethoxy]phenyl]propyl ester, (2S)-
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