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UNC-926
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UNC-926图片
CAS NO:1184136-10-4
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 337.25
Formula C16H21BrN2O
CAS No. 1184136-10-4 (free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 67 mg/mL (198.7 mM)
Water: < 1mg/mL
Ethanol: 2 mg/mL (5.9 mM)
Chemical Name (3-Bromophenyl)[4-(1-pyrrolidinyl)-1-piperidinyl]methanone
Synonyms UNC926 free base; UNC 926 free base; UNC-926 free base; UNC-926; UNC926; UNC 926
SMILES Code O=C(C1=CC=CC(Br)=C1)N2CCC(N3CCCC3)CC2
实验参考方法
In Vitro

In vitro activity: UNC-926 is an inhibitor of the L3MBTL1 (Lethal(3)malignant brain tumor-like protein) domain. It binds to the MBT domain of the L3MBTL1 protein with a Kd value of 3.9 μM. The interaction between methyl-lysine binding proteins and methylated histones plays a crucial role in the regulation of gene expression. UNC-926 was demonstrated to successfully inhibit the recognition of H4K20me1 by L3MBTL1 in the context of an affinity pull down assay. Mounting evidence suggests that epigenetic alterations relate to various human diseases including inflammation, brain disorders, metabolic diseases, and cancer.1, 2, 3 One such epigenetic modification is histone lysine methylation.


Kinase Assay: UNC-926 inhibits L3MBTL1 with an IC50 of 3.9 μM. L3MBTL1UNC-926 also exhibits a low micromolar affinity for the close homolog, L3MBTL3, with a decrease in affinity for the other MBT domains and no binding to CBX7. UNC-926 inhibits binding of the 3xMBT domain to H4K20me1. It selectively inhibits the L3MBTL13xMBT-H4K20me1 interaction in a dose-dependent manner. UNC-926 does not have an effect on the binding of 53BP1 to H4K20me1, demonstrating specificity of UNC-926 for L3MBTL1 over 53BP1

In Vivo
Animal model
Formulation & Dosage
References Med. Chem. Commun., 2012, 3, 45-51; Bioorg Med Chem Lett. 2016 Sep 15;26(18):4436-4440.