Chemical Structure : DYR684
CAS No.:
DYR684
(DYR-684)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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1050.22
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Formula
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C58H60FN15O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-(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)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
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References
1. Wilms G, et al. J Med Chem. 2024 Oct 10;67(19):17259-17289.
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