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HLCL-61
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。
HLCL-61图片
CAS NO:1158279-20-9
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
HLCL-61 是一流的蛋白质精氨酸甲基转移酶 5 (PRMT5) 抑制剂。
Cas No.1158279-20-9
化学名1-(9-ethyl-9H-carbazol-3-yl)-N-(2-methoxybenzyl)methanamine hydrochloride
Canonical SMILESCCN1C2=CC=CC=C2C3=C1C=CC(CNCC4=CC=CC=C4OC)=C3.Cl
分子式C23H25ClN2O
分子量380.91
溶解度DMSO: >1mg/ml,Ethanol: >1mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

HLCL-61 is a PRMT5 inhibitor.

Aberrant methylation of protein arginine residues mediated by protein arginine methyltransferase (PRMT) enzymes is reported to be linked to cancer. PRMTs are a family of proteins with 11 known members catalyzing the transfer of methyl group(s) to the guanidine nitrogen atoms of peptide arginine residues. PRMT5 has multiple substrates including histones and other non-chromatin proteins and has been gained attention for cancer therapy.

In vitro: In previous study, HLCL-61 showed no inhibitory activity against PRMT1, PRMT4, and type II PRMT family members, therefore demonstrating its specificity for PRMT5. HLCL-61 also showed effective inhibition of symmetric arginine dimethylation of histones H3 and H4, starting at 12 h posttreatment and persisting for 48 h. Moreover, the treatment of AML cell lines and primary blasts with HLCL-61 led to the decrease of cell viability. In addition, HLCL-61-treated AML cell lines and patient samples had induction of differentiation as demonstrated by dose-dependent increases in the expression of CD11b. Furthermore, PRMT5 inhibition caused by HLCL-61 treatment led to a decrease in MV4-11 cells [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, HLCL-61 is still in the preclinical development stage.

Reference:
[1] Tarighat SS et al.  The dual epigenetic role of PRMT5 in acute myeloid leukemia: gene activation and repression via histone arginine methylation. Leukemia. 2016 Apr;30(4):789-99.