GSK046
GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity[1].
Product Specifications
CAS Number
2474876-09-8
Product Name Alternative
IBET-BD2
UNSPSC
12352005
Target
Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Epigenetics
Applications
COVID-19-immunoregulation
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/gsk046.html
Purity
99.65
Solubility
DMSO : 83.33 mg/mL (ultrasonic)
Smiles
O=C(N[C@H]1CC[C@H](O)CC1)C2=CC(O[C@H](C3=CC=CC=C3)C)=C(NC(C)=O)C(F)=C2
Molecular Formula
C23H27FN2O4
Molecular Weight
414.47
References & Citations
[1]Omer G, et, al. Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science. 2020 Apr 24; 368 (6489) : 387-394.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD2; BRD3; BRD4; BRDT
Available Sizes
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