IBG3

Catalog #: 8129 Datasheet
Catalog # Availability Size / Price Qty
8129/2
IBG3 | Molecular Glues
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Description: Potent molecular glue Degrader of BET proteins BRD4 and BRD2

Chemical Name: tert-Butyl 2-((S)-4-(4-((4'-((S)-6-(2-(tert-butoxy)-2-oxoethyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-[1,1'-biphenyl]-4-carboxamido)methyl)phenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate

Product Details
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Biological Activity

IBG3 is a very potent JQ1-containing molecular glue Degrader of BET proteins BRD4 and BRD2 (DC50 values are 6.7 pM and 8.6 pM respectively). Induces proximity between BRD4 and DCAF16 to form a ternary complex (EC50 = 32 nM).

Scientific Data

In vitro assay Published vs Bio-Techne batch comparison for IBG3 View Larger

Published vs Bio-Techne batch comparison for IBG3. Endogenous HiBiT-BRD4 HEK293 cells were plated at a density of 20,000 cell per well in 100 µL of DMEM (10% FBS) in a white-walled 96 well plate and left overnight to adhere at 37 ºC, 5% CO2. Cells were incubated in 50 µL of 10 nM-0.1 pM of IBG3 or vehicle control (DMSO)  in Optimem (10% FBS) and left for 4 hours. Cells were then treated with HiBIT Lytic assay reagent– and plates were then read on a BMG Pherastar plate reader for luminescence detection. Data kindly provided by the Ciulli laboratory, University of Dundee.

Technical Data

M.Wt:
976.23
Formula:
C54H57N9O5S2
Solubility:
Soluble to 100 mM in DMSO
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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