GNE-987

• Target:

  Epigenetic Reader Domain|||PROTACs

• Related Pathways:

  PROTAC|||Chromatin/Epigenetic

• Bioactivity:

  GNE-987 is a highly active chimeric BET degrader. GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50: 4.7 and 4.4 nM, respectively) . GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50: 0.03 nM for EOL-1 AML cell line) .

• Smiles:

  O=C ([C@H] (C[C@@H] (O) C1) N1C ([C@@H] (NC (CCCCCCCCCCNC (C2=C (CS (=O) (C) =O) C=C (C (N (C3=NC=C (F) C=C3F) C4) =C2) C5=CN (C) C (C6=C5C4=CN6) =O) =O) =O) C (C) (C) C) =O) NCC7=CC=C (C (SC=N8) =C8C) C=C7

• Molecular Formula:

  C56H67F2N9O8S2

• Molecular Weight:

  1096.31

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2417371-71-0