Chemical Structure : UNC10013
CAS No.:
UNC10013
(UNC-10013)
Catalog No.: PC-23137Not For Human Use, Lab Use Only.
UNC10013 is a potent, selective and cell-active covalent ligand/negative allosteric modulator of triple Tudor domain (3TD) of SETDB1 with TR-FRET IC50 of 57 nM, targets the Cys385 of SETDB1.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
UNC10013 is a potent, selective and cell-active covalent ligand/negative allosteric modulator of triple Tudor domain (3TD) of SETDB1 with TR-FRET IC50 of 57 nM, targets the Cys385 of SETDB1.
UNC10013 has a kinact/KI of 1.0 x 106 M-1s-1 and demonstrates proteome-wide selectivity.
UNC10013 shows no significant direct inhibition of the methyltransferase activity of SETDB1 in vitro （IC50=64.9 uM.
UNC10013 exhibits negative allosteric modulator properties and making it a promising tool to study the biological role of SETDB1 in disease progression.
Physicochemical Properties
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M.Wt
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526.77
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Formula
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C29H50N8O
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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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(E)-4-(dimethylamino)-N-(4-((6-(dimethylamino)hexyl)amino)-2-((5-(dimethylamino)pentyl)amino)quinazolin-6-yl)but-2-enamide
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References
1. Uguen M, et al. bioRxiv [Preprint]. 2024 Sep 28:2024.09.27.615363.
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