Home Epigenetics Histone Methyltransferase inhibitor - PRMT inhibitor HLCL-61 HCL

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HLCL-61 HCL Histone Methyltransferase inhibitor

Cat.No.S8209

HLCL-61 hydrochloride is a potent and selective PRMT5 inhibitor for the treatment of acute myeloid leukemia.
HLCL-61 HCL Histone Methyltransferase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 380.91

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Quality Control

Batch: S820901 DMSO]76 mg/mL]false]Ethanol]76 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

Chemical Information, Storage & Stability

Molecular Weight 380.91 Formula

C23H24N2O.HCl

 Storage (From the date of receipt)
CAS No. 1158279-20-9 Download SDF Storage of Stock Solutions

Synonyms HLCL61 Smiles CCN1C2=C(C=C(C=C2)CNCC3=CC=CC=C3OC)C4=CC=CC=C41.Cl

Solubility

In vitro
Batch:

DMSO : 76 mg/mL (199.52 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 76 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
PRMT5 [1]
(In THP-1 cells)
16.74 μM
In vitro
HLCL-61 shows no inhibitory activity against the type I (PRMT1 and PRMT4) and type II (PRMT7) PRMT family members. HLCL-61 shows effective inhibition of symmetric arginine dimethylation (me2) of histones H3 and H4 in AML samples.Treatment of AML cell lines (MV4-11 and THP-1) and primary blasts with HLCL-61 also results in a decrease of cell viability. HLCL-61 is also effective in promoting apoptosis in MV4-11 and THP-1 cells after 48 h[1].
References

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