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SR-0813

Chemical Structure : SR-0813

CAS No.: 2597186-19-9

SR-0813 (SR0813)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 496.63
Formula C25H32N6O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Imidazo[1,2-a]pyridine-6-carboxamide, N-cyclobutyl-2-[3-[[[[2-(1-piperidinyl)ethyl]amino]sulfonyl]amino]phenyl]-

References

1. Garnar-Wortzel L, ACS Cent Sci. 2021 May 26;7(5):815-830.

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