SR-0813 (SR0813) is a potent, selective, dual ENL/AF9 YEATS domain inhibitor (IC50 =25/311 nM).
SR-0813 engages the ENL YEATS domain more potently in cells consistent with its 25 nM potency in the HTRF assay.
SR-0813 is not selective for ENL over AF9, potently inhibits both.
SR-0813 is highly selective against the YEATS domains of YEATS2 and YEATS4. SR-0813 is potently engaged in cells (ENL EC50=205 nM, AF9 =76 nM).
SR-0813 shows no off-target effects on bromodomain proteins, and a kinase selective profile 3/468 kinases using the KINOMEscan profiling service.
SR-0813 (1 uM) downregulated ENL target genes, HOXA9, MEIS1, and MYC following treatment of MV4;11 cells, inhibited the growth of ENL-dependent leukemia.
SR-0813 as an exquisitely selective chemical probe for the ENL YEATS domain.
