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UNC10013

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

M.Wt 526.77
Formula C29H50N8O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

(E)-4-(dimethylamino)-N-(4-((6-(dimethylamino)hexyl)amino)-2-((5-(dimethylamino)pentyl)amino)quinazolin-6-yl)but-2-enamide

References

1. Uguen M, et al. bioRxiv [Preprint]. 2024 Sep 28:2024.09.27.615363.
2. Uguen M, et al. Nat Commun. 2025 Feb 24;16(1):1905.

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