Name: HLCL-61
Price: 290.00 USD

- Overview
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    Background
    
    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.
- Properties
  - Alternative Name
    
    1-(9-ethyl-9H-carbazol-3-yl)-N-(2-methoxybenzyl)methanamine hydrochloride
    
    CAS Number
    
    1158279-20-9
    
    Molecular Formula
    
    C23H25ClN2O
    
    Molecular Weight
    
    380.91
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥20.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

HLCL-61

HLCL-61

Background

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