DEG-35 | IKZF2/CK1α degarder | Probechem Biochemicals

Chemical Structure : DEG-35

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DEG-35 (Dual IKZF2/CK1α degarder DEG-35)

货号: PC-23961Not For Human Use, Lab Use Only.

DEG-35 is a potent, cereblon-dependent, dual degrader of IKZF2 ((DC50=4.4 nM, DCmax=92%)) and casein kinase 1α (CK1α, DC50=1.4 nM, DCmax=84%), shows leukemic cell killing activity.

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生物&药学活性

DEG-35 is a potent, cereblon-dependent, dual degrader of IKZF2 (DC50=4.4 nM, DCmax=92%) and casein kinase 1α (CK1α, DC50=1.4 nM, DCmax=84%), shows leukemic cell killing activity.
DEG-35 efficiently degrades IKZF2 with limited activity against IKZF1, IKZF3 and IKZF4 in a Cullin-dependent manner.
DEG-35 inhibits growth activity in a panel of AML cell lines representing various oncogenic mutations with IC50 values from single digit nM to low μM concentrations (MOLM-13 cell, IC50=5.3 nM).
DEG-35 degrades dual targets IKZF2 and CK1α via Cullin-CRBN dependent pathway.
DEG-35 has higher affinity (KD = 472.6 nM) than lenalidomide (KD = 804.7 nM) for CRBN, as measured by HTR-FRET.
DEG-35 activates the p53 apoptosis pathway, activates IKZF2-dependent differentiation in MOLM-13 cells.
DEG-35 has preferential cytotoxic activity in AML cells compared to normal cells.
DEG-35 can degrade targets in AML cells in vivo and delay leukemia progression in the MLL-AF9 CrbnI391V mice model.

物理化学性质&存储条件

分子量	443.46
分子式	C25H21N3O5
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-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)-6-methoxy-2-naphthamide

参考文献

1. Park SM, et al. Cancer Cell. 2023 Apr 10;41(4):726-739.e11.

DEG-35 (Dual IKZF2/CK1α degarder DEG-35)

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DEG-35 (Dual IKZF2/CK1α degarder DEG-35)

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物理化学性质&存储条件

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