Home Epigenetics Histone Methyltransferase inhibitor - PRMT inhibitor Onametostat (JNJ-64619178) For research use only.

Onametostat (JNJ-64619178)

Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.

Onametostat (JNJ-64619178) Chemical Structure

Onametostat (JNJ-64619178) Chemical Structure

CAS No. 2086772-26-9

Purity & Quality Control

Onametostat (JNJ-64619178) Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Function assay Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infected Sf9 insect cells assessed as reduction of S-adenosyl-L-homocysteine formation using human recombinant , IC50=0.00013μM 30956011
Sf9 Function assay 120 mins Inhibition of full-length human N-terminal FLAG-tagged PRMT5 expressed in Sf9 insect cells using histone H2A as peptide after 120 mins in presence of SAM by high throughput mass spectrometer assay, IC50=0.00014μM 30366617
A549 Function assay 48 hrs Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immunohistochemistry method, IC50=0.00025μM 30956011
HEK293 Function assay 60 mins Inhibition of human N-terminal FLAG-tagged PRMT5 (2 to end) expressed in HEK293 cells using biotinylated H2A as substrate measured after 60 mins in presence of SAM by high throughput mass spectrometer assay, IC50=0.0063μM 29870258
Click to View More Cell Line Experimental Data

Biological Activity

Description Onametostat (JNJ-64619178) is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.
Targets
PRMT5 [1]
0.14 nM
In vitro
In vitro

JNJ-64619178 binds into the SAM binding pocket and reaches the substrate binding pocket to inhibit PRMT5/MEP50 function in a time-dependent manner. Broad cell line panel profiling of JNJ-64619178 reveals a wide range of sensitivity, which is indicative of a genomic dependency instead of a general cytotoxic on-target consequence of PRMT5 inhibition[1].
In Vivo
In vivo

JNJ-64619178, dosed orally (10 mg/kg, every day), shows selective and efficient blockage of the methylation of SMD1/3 proteins, which are crucial components of the spliceosome and substrates of PRMT5/MEP50. JNJ-64619178 also demonstrates tumor regression in a biomarker-driven human small cell lung cancer xenograft model (NCI-H1048) and prolongs tumor growth inhibition after dosing cessation. In rodent and nonrodent toxicology studies, a tolerated dose of JNJ-64619178 has been identified, with the observed toxicity consistent with on-target activity. In summary, JNJ-64619178 has a favorable preclinical package that supports clinical testing in patients diagnosed with lung cancer and hematologic malignancies1[1].
Animal Research Animal Models C57BL/6 mice
Dosages 10 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03573310 Active not recruiting
Neoplasms|Solid Tumor Adult|Non-Hodgkin Lymphoma|Myelodysplastic Syndromes
Janssen Research & Development LLC
 July 13 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 483.36 Formula

C22H23BrN6O2
CAS No. 2086772-26-9 SDF Download Onametostat (JNJ-64619178) SDF
Smiles C1C(C(C(C1N2C=CC3=C(N=CN=C32)N)O)O)CCC4=CC5=NC(=C(C=C5C=C4)Br)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (200.67 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

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