UNC8732 | NSD2 degrader | Probechem Biochemicals

Chemical Structure : UNC8732

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UNC8732 (UNC 8732, UNC-8732)

货号: PC-22588Not For Human Use, Lab Use Only.

UNC8732 is a highly potent, second-generation NSD2 degrader with DC50 of 0.06 uM and Dmax of 97%, SPR KD of 76 nM, facilitates FBXO22-mediated degradation of NSD2 in NSD2-mutant ALL.

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生物&药学活性

UNC8732 is a highly potent, second-generation NSD2 degrader with DC50 of 0.06 uM and Dmax of 97%, SPR KD of 76 nM, facilitates FBXO22-mediated degradation of NSD2 in NSD2-mutant ALL.
UNC8732 demonstrates improved NSD2 degradation and H3K36me2 reduction in cells, compared with UNC8153.
UNC8732 promotes highly selective NSD2 degradation within the measurable proteome.
UNC8732 inhibits cell growth and restores GC sensitivity of NSD2 p.E1099K mutant ALL cells, induces apoptosis of NSD2 mutant cells.
The metabolism of UNC8732 to the aldehyde is required for effective degradation.
UNC8732 recruits the SCFFBXO22 ubiquitin ligase complex for compound-mediated degradation of NSD2, binds and recruits FBXO22 via interactions with C326.

物理化学性质&存储条件

分子量	609.73
分子式	C35H39N5O5
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-(4-((2-(6-aminohexanoyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)carbamoyl)benzyl)-N-cyclopropyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide

参考文献

1. Nie DY, et al. Nat Chem Biol. 2024 Jul 4. doi: 10.1038/s41589-024-01660-y.

UNC8732 (UNC 8732, UNC-8732)

生物&药学活性

物理化学性质&存储条件

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UNC8732 (UNC 8732, UNC-8732)

生物&药学活性

物理化学性质&存储条件

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