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首页-小分子抑制剂&激动剂-Autophagy-ULK-MA9-060
MA9-060

Chemical Structure : MA9-060

CAS No.: 2413026-03-4

MA9-060 (MA9060, MA9)

货号: PC-28344Not For Human Use, Lab Use Only.

MA9-060 (MA9) is a potent, seletive small molecule Unc-51 like kinase 3 (ULK3) inhibitor with IC50 of 226 nM, weakerly inhibits ULK1 (IC50=1046 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MA9-060 (MA9) is a potent, seletive small molecule Unc-51 like kinase 3 (ULK3) inhibitor with IC50 of 226 nM, weakerly inhibits ULK1 (IC50=1046 nM).
MA9-060 (MA9) is a type-1 inhibitor that engages the hinge Cys94 residue via hydrogen bonding to its pyrimidine N1 and 2-anilinyl NH groups.
MA9-060 (MA9) provokes rapid reductions in ULK3 levels and autophagy effectors in U266 MM cells, is not toxic to normal primary human MSCs. inhibit the proper formation of autophagolysosomes.
MA9-060 (MA9) significantly reduces MM growth and myeloma-associated bone disease in vivo, is sensitive for drug-resistant MM cells express increased levels of ULK3.
MA9-060 (MA9) displays potent anti-myeloma activity against patient derived MM cells ex vivo.

物理化学性质&存储条件

分子量 561.12
分子式 C27H34ClFN6O2S
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

N-(2-chloro-5-((2-((3-fluoro-4-(1-methylpiperidin-4-yl)phenyl)amino)-5-methylpyrimidin-4-yl)amino)phenyl)-2-methylpropane-2-sulfonamide

参考文献

1. Tauro M, et al. Nat Commun. 2026 Aug 25;17(1):10142.

2. Patent WO2022155593 A1 2022-07-21.

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