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HLCL65 hydrochloride
- Parent CAS: 1627865-11-5
- Soluble in DMSO
- MF: C23H23BrN2O.HCl
- MW: 459.81
Description
HLCL65 hydrochloride is a selective, cell-active inhibitor of protein arginine methyltransferase 5 (PRMT5) and a more potent, bioavailable derivative of CMP5. By reducing PRMT5-dependent symmetric arginine dimethylation, HLCL65 disrupts methylation programs required for activated lymphocyte proliferation and cell-cycle progression.
HLCL65 inhibits mouse T-helper-cell proliferation with IC50 values of 1.1 µM for Th1 cells and 4.0 µM for Th2 cells, with Th1 responses showing greater sensitivity. PRMT5 blockade with HLCL65 suppresses recall T-cell responses and reduces inflammation and clinical disease in delayed-type hypersensitivity and experimental autoimmune encephalomyelitis models. The parent probe CMP5 (Axon 2709) is available for comparative studies.
Key Features
- Selective PRMT5 inhibitor
- IC50: 1.1 µM in mouse Th1 cells
- IC50: 4.0 µM in mouse Th2 cells
- Suppresses PRMT5-dependent lymphocyte proliferation
Applications
- PRMT5 and symmetric arginine methylation
- CD4-positive T-cell activation and cell-cycle research
- Th1 and Th2 response studies
- Delayed-type hypersensitivity models
- Experimental autoimmune encephalomyelitis research
More Information
| Parent CAS No. | 1627865-11-5 |
|---|---|
| Chemical Name | 1-(6-Bromo-9-ethyl-9H-carbazol-3-yl)-N-(2-methoxybenzyl)methanamine hydrochloride |
| SMILES | C12C=C(Br)C=CC=1N(CC)C1C=CC(CNCC3C(OC)=CC=CC=3)=CC2=1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C23H23BrN2O.ClH/c1-3-26-21-10-8-16(12-19(21)20-13-18(24)9-11-22(20)26)14-25-15-17-6-4-5-7-23(17)27-2;/h4-13,25H,3,14-15H2,1-2H3;1H |
| InChiKey | RCHOCKASSZYCEX-UHFFFAOYSA-N |
| CID | 129909864 |
| Short Description | PRMT5 inhibitor |
References
- D El-Gamal et al. Expression of PRMT5 in B-Cell Chronic Lymphocytic Leukemia and Its Significance in Disease Progression and Richter's Transformation. Blood 2014 124:2197.
- LM Webb et al. Protein Arginine Methyltransferase 5 (PRMT5) Selective Inhibitors Suppress Inflammatory T Cell Responses and Experimental Autoimmune Encephalomyelitis. J Immunol 198 (4), 1439-1451. 2017 Jan 13.
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