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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-UNC10013
UNC10013

Chemical Structure : UNC10013

CAS No.:

UNC10013 (UNC-10013)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 526.77
分子式 C29H50N8O
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

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

参考文献

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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