MR-9036 | ULK1 degrader | Probechem Biochemicals

Chemical Structure : MR-9036

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MR-9036 (MR9036)

货号: PC-28568Not For Human Use, Lab Use Only.

MR-9036 is a potent, selective cereblon-recruiting ULK1 degrader with DC50 of 67 nM in MOLT-4 cells.

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生物&药学活性

MR-9036 is a potent, selective cereblon-recruiting ULK1 degrader with DC50 of 67 nM in MOLT-4 cells.
MR-9036 does not affect the abundance of ULK1 isoforms (e.g. ULK2, ULK3 or ULK4), and does not reduce the levels of IMiD neo-substrates (such as, IKZF1, IKZF3, CK1α, GSPT1, SALL4, and PLZF).
MR-9036 induces the degradation of ULK1 via the E3 ligase, CRBN, and subsequently through the ubiquitin-proteasomal system.
MR-9036 blocks autophagic flux in H2030 cells, exhibits superior autophagy inhibition than DCC-3116.
MR-9036 exhibits greater synergistic antiproliferative activity with the combination of sotorasib, than DCC-3116.
MR-9036 effectively reduced the levels of ULK1 (<20%) along with substantial suppression of downstream phospho-ATG14 (pATG14) in tumor tissue at 30 and 90 mg/kg.

物理化学性质&存储条件

分子量	860.94
分子式	C43H51F3N10O6
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	2-(2,6-Dioxopiperidin-3-yl)-5-((S)-3-((4-(3-ethyl-4-((4-((3-(5-oxo-1,4-oxazepan-4-yl)propyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)phenyl)piperazin-1-yl)methyl)pyrrolidin-1-yl)isoindoline-1,3-dione

参考文献

1. Sean Chin Chan, et al. J Med Chem. 2026 Oct 22;69(20):23744-23769.

MR-9036 (MR9036)

生物&药学活性

物理化学性质&存储条件

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MR-9036 (MR9036)

生物&药学活性

物理化学性质&存储条件

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