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SR-0813

Chemical Structure : SR-0813

CAS No.: 2597186-19-9

SR-0813 (SR0813)

货号: 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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10 mg ¥2180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 496.63
分子式 C25H32N6O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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]-

参考文献

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

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