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.