GSK778 (hydrochloride)
GSK778 (iBET-BD1) hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively[1].
Product Specifications
CAS Number
2863657-79-6
Product Name Alternative
IBET-BD1 (hydrochloride)
UNSPSC
12352005
Target
Apoptosis; Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Apoptosis; Epigenetics
Applications
COVID-19-immunoregulation
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/gsk778-hydrochloride.html
Solubility
10 mM in DMSO
Smiles
CC1=NOC(C)=C1C2=C(OC[C@@H]3CNCC3)C=C4C5=C(N=C(COC)N5[C@H](C)C6=CC=CC=C6)C=NC4=C2.Cl
Molecular Formula
C30H34ClN5O3
Molecular Weight
548.08
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
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD2; BRD3; BRD4; BRDT
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