Chemical Structure : SR-0813
CAS No.: 2597186-19-9
Catalog No.: PC-72573Not For Human Use, Lab Use Only.
SR-0813 (SR0813) is a potent, selective, dual ENL/AF9 YEATS domain inhibitor (IC50 =25/311 nM).
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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.
M.Wt | 496.63 | |
Formula | C25H32N6O3S | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Imidazo[1,2-a]pyridine-6-carboxamide, N-cyclobutyl-2-[3-[[[[2-(1-piperidinyl)ethyl]amino]sulfonyl]amino]phenyl]- |
1. Garnar-Wortzel L, ACS Cent Sci. 2021 May 26;7(5):815-830.
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