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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-LS-170
LS-170

Chemical Structure : LS-170

CAS No.: 3099617-79-2

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LS-170 (LS170)

货号: PC-26818Not For Human Use, Lab Use Only.

LS-170 is a potent, specific inhibitor of ATAC (Ada-two-A-containing) HAT complex subunit YEATS2 with IC50 of 0.14 uM (YEATS2 YEATS domain), shows no inhibitory effect for other YEATS domain family members, AF9, ENL and GAS41.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LS-170 is a potent, specific inhibitor of ATAC (Ada-two-A-containing) HAT complex subunit YEATS2 with IC50 of 0.14 uM (YEATS2 YEATS domain), shows no inhibitory effect for other YEATS domain family members, AF9, ENL and GAS41.
LS-170 also shows no activity against a panel of selected epigenetic 'reader' and 'eraser' proteins, including Kac readers (BRD2(2), BRD4(2), BRD9, TAF1(2) and CECR2), Kme readers (ING2 and SPIN1) and Kac erasers (Sirt3 and Sirt6).
LS-170 is cell-permeable and could dissociates YEATS2 from chromatin in cells.
LS-170 selectively engages with the ATAC complex in cells, displaces the ATAC complex from chromatin to suppress its activity.
LS-170 inhibits the ATAC-governed DNA replication pathway, without impairing SAGA localization or function.
LS-170 inhibited NSCLC cell lines H1299 and H157 growth with GI50 of 15.6 μM and 6.8 μM, respectively, strongly suppressed colony formation in H1299, A549 and PC9 cells, also significantly inhibited migration and invasion of H1299 cells.
LS-170 significantly suppressed tumor growth without reducing body weight in H1299 xenograft models.

物理化学性质&存储条件

分子量 764.71
分子式 C34H43BrFN5O7S
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

6-bromo-N-((S)-6-(((S)-3-(4-fluorophenyl)-1-(methyl((S)-1-oxo-1-(piperidin-1-yl)propan-2-yl)amino)-1-oxopropan-2-yl)amino)-5-(methylsulfonamido)-6-oxohexyl)benzofuran-2-carboxamide

参考文献

1. Sha Liu, et al. Nat Chem Biol. 2026 Mar;22(3):471-481.

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