GSK778

• UNSPSC Description:

  GSK778 (iBET-BD1) 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. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models[1].

• Target Antigen:

  Apoptosis; Epigenetic Reader Domain

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Epigenetics

• Field of Research:

  Cancer; Inflammation/Immunology

• Assay Protocol:

  https://www.medchemexpress.com/gsk778.html

• 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

• Molecular Weight:

  511.61

• 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

• CAS Number:

  2451862-42-1