DYR684 | DYRK1 PROTAC | Probechem Biochemicals

Chemical Structure : DYR684

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DYR684 (DYR-684)

货号: PC-23233Not For Human Use, Lab Use Only.

DYR684 is a potent, and selective PROTAC degrader of DYRK1 with KD of 6.3/16 nM for DYRK1A/DYRK1B, DC50 value of 12.3 nM for DYRK1A in HEK293 cells.

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生物&药学活性

DYR684 is a potent, and selective PROTAC degrader of DYRK1 with KD of 6.3/16 nM for DYRK1A/DYRK1B, DC50 value of 12.3 nM for DYRK1A in HEK293 cells.
The maximum percentage of degradation (Dmax) is ∼90% for DYRK1A and ∼50% for DYRK1B.
DYR684 does not alter the cellular levels of DCAF7 (a.k.a. WDR68), an adaptor protein that forms stoichiometric complexes with DYRK1A and DYRK1B.
DYRK1B-p65 is resistant to DYR684-induced degradation.
DYR684 induces proteasomal degradation of DYRK1 via CRBN-mediated ubiquitination.
DYR684 (0-100 nM) inhibits downstream target of DYRK1A/B, phosphorylation of SF3B1 on Thr434 in HEK293 cells.

物理化学性质&存储条件

分子量	1064.20
分子式	C58H58FN15O5
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	4-(((1-(1-(1-(5-(3-(4-(4-(5-(2-aminopyridin-4-yl)-2-methyl-3H-imidazo[4,5-b]pyridin-3-yl)-2-fluorophenyl)piperazin-1-yl)prop-1-yn-1-yl)pyridin-2-yl)piperidine-4-carbonyl)piperidin-4-yl)-1H-pyrazol-4-yl)methyl)amino)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione

参考文献

1. Wilms G, et al. J Med Chem. 2024 Oct 10;67(19):17259-17289.

DYR684 (DYR-684)

生物&药学活性

物理化学性质&存储条件

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DYR684 (DYR-684)

生物&药学活性

物理化学性质&存储条件

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