Art. -Nr.: HY-101564

Onametostat

(Synonyms: JNJ-64619178)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Onametostat (JNJ-64619178) is a selective, orally active and pseudo-irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC₅₀ of 0.14 nM. Onametostat has potent activity in lung cancer.

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Reinheit: 99.40%
CAS. Nr.: 2086772-26-9
Formel: C₂₂H₂₃BrN₆O₂
Molecular Weight:483.36

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Onametostat Chemical Structure

CAS. Nr.: 2086772-26-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PRMT5

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.25 nM Compound: JNJ64619178; 21	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 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	[PMID: 30956011]
MOLM-13	IC₅₀	<1 nM Compound: JNJ64619178	Antiproliferation activity against human MOLM-13 cells assessed as cell viability incubated for 6 days by CCK-8 assay Antiproliferation activity against human MOLM-13 cells assessed as cell viability incubated for 6 days by CCK-8 assay	[PMID: 38301329]
NCI-H1048	GI₅₀	1.3 nM Compound: 11; JNJ64619178	Antiproliferative activity against human NCI-H1048 cells assessed as cell growth inhibition incubated for 6 days by MTT assay Antiproliferative activity against human NCI-H1048 cells assessed as cell growth inhibition incubated for 6 days by MTT assay	[PMID: 37366223]
Sf9	IC₅₀	0.13 nM Compound: JNJ64619178; 21	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 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	[PMID: 30956011]
Sf9	IC₅₀	0.14 nM Compound: 6; JNJ-64619178	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 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	[PMID: 30366617]
Z-138	IC₅₀	<1 nM Compound: JNJ64619178	Antiproliferation activity against human Z138 cells assessed as cell viability incubated for 6 days by CCK-8 assay Antiproliferation activity against human Z138 cells assessed as cell viability incubated for 6 days by CCK-8 assay	[PMID: 38301329]

In Vitro

Onametostat binds simultaneously to the S-adenosylmethionine (SAM)- and protein substrate- binding pockets of the PRMT5/MEP50 complex with a pseudo-irreversible mode-of-action. Onametostat shows potent and broad inhibition of cellular growth^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration of Onametostat results in efficient inhibition of dimethylation of SMD1/3 proteins, components of the splicing machinery and direct substrates of the methylosome, in several non-small cell lung cancer and small cell lung cancer? cancer mouse xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2086772-26-9
Appearance Solid
Molecular Weight 483.36
Formel C₂₂H₂₃BrN₆O₂
Color Off-white to light yellow
SMILES

BrC1=C(N)N=C(C=C(CC[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C=C3)C2)C=C5)C5=C1
Synonyms

JNJ-64619178
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyWB

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Journal Impact Factor

Gut

Identification of PRMT5 as a therapeutic target in cholangiocarcinoma. [Abstract]

2024 Sep 11:gutjnl-2024-332998. PMID: 39266051

Onametostat purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

GI₅₀ values for the PRMT5 inhibitors GSK3326595 and JNJ64619178 (Onametostat) in the indicated CCA cell lines.

Onametostat purchased from MedChemExpress. Usage Cited in: Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]

Immunoblot analysis of PRMT5-dependent symmetric dimethylarginine (SMDA) protein marks in control and GSK3326595 or JNJ64619178 (Onametostat) treated HuCCT-1 and TFK-1 cells at the indicated doses for 5 days.
Nat Commun

Dysregulation of PRMT5 in chronic lymphocytic leukemia promotes progression with high risk of Richter's transformation. [Abstract]

2023 Jan 6;14(1):97. PMID: 36609611

Onametostat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jan 6;14(1):97. [Abstract]

Dose-dependent proliferative potential as measured by cell growth in CLL cell lines upon treatment with Onametostat (JNJ-64619178) (1 nM-1 μM) (n = 2). Cell growth is plotted as fold change relative to vehicle-treated cells ±SD. Fresh culture media and PRMT5 inhibitor (Onametostat (JNJ-64619178)) at indicated concentrations were supplied every 3 days for continuous exposure over 12 days.
MedComm (2020)

SCR-7952, a highly selective MAT2A inhibitor, demonstrates synergistic antitumor activities in combination with the S-adenosylmethionine-competitive or the methylthioadenosine-cooperative protein arginine methyltransferase 5 inhibitors in methylthioadenosine phosphorylase-deleted tumors. [Abstract]

2024 Sep 20;5(10):e705. PMID: 39309689

Onametostat purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Sep 20;5(10):e705. [Abstract]

Impact of SCR‐7952 and Onametostat (JNJ-64619178) (1.0 mg/kg; oral gavage; once daily) alone and in combination on tumor growth, tumor SDMA levels on HCT116 MTAP^−/− tumor-bearing mice (mean ± SEM, n = 8). The results showed that treatment with SCR-7952 (0.3 mg/kg) or JNJ-64619178 (1.0 mg/kg) alone both led to a remarkable reduction in SDMA levels. In the combination group, SDMA levels were significantly lower than those in the single-drug-treated groups, indicating a synergistic effect between SCR-7952 and JNJ-64619178.

Onametostat purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Sep 20;5(10):e705. [Abstract]

Immunoblot analysis of SDMA and MAT2A after combination treatment (SCR‑7952 and Onametostat (JNJ‐64619178)) for 96 h.
Oncogene

MYCN and SNRPD3 cooperate to maintain a balance of alternative splicing events that drives neuroblastoma progression. [Abstract]

2024 Jan;43(5):363-377. PMID: 38049564
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Biomed J

PRMT5-mediated methylation of LKB1 controls PD-L1 expression in NSCLC. [Abstract]

2026 Jun 10:101002. PMID: 42270077
bioRxiv

2026 Apr 13.
bioRxiv

PRMT5 inhibitors actively promote metastatic progression of lung adenocarcinoma. [Abstract]

2026 Feb 2:2026.01.30.702866. PMID: 41676495
SRRN

2025 Jun 9.
bioRxiv

The PRMT5-splicing axis is a critical oncogenic vulnerability that regulates detained intron splicing. [Abstract]

2024 Dec 20:2024.12.17.628905. PMID: 39763796
bioRxiv

2024 Feb 21.
University of Munich

2022 Oct.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 125 mg/mL (258.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0689 mL

10.3443 mL

20.6885 mL

5 mM

0.4138 mL

2.0689 mL

4.1377 mL

10 mM

0.2069 mL

1.0344 mL

2.0689 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.30 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Tongfei Wu, et al. Abstract 4859: JNJ-64619178, a selective and pseudo-irreversible PRMT5 inhibitor with potent in vitro and in vivo activity, demonstrated in several lung cancer models.

[2]. Tao H, et al. Discovery of Novel PRMT5 Inhibitors by Virtual Screening and Biological Evaluations. Chem Pharm Bull (Tokyo). 2019;67(4):382-388. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0689 mL	10.3443 mL	20.6885 mL	51.7213 mL
	5 mM	0.4138 mL	2.0689 mL	4.1377 mL	10.3443 mL
	10 mM	0.2069 mL	1.0344 mL	2.0689 mL	5.1721 mL
	15 mM	0.1379 mL	0.6896 mL	1.3792 mL	3.4481 mL
	20 mM	0.1034 mL	0.5172 mL	1.0344 mL	2.5861 mL
	25 mM	0.0828 mL	0.4138 mL	0.8275 mL	2.0689 mL
	30 mM	0.0690 mL	0.3448 mL	0.6896 mL	1.7240 mL
	40 mM	0.0517 mL	0.2586 mL	0.5172 mL	1.2930 mL
	50 mM	0.0414 mL	0.2069 mL	0.4138 mL	1.0344 mL
	60 mM	0.0345 mL	0.1724 mL	0.3448 mL	0.8620 mL
	80 mM	0.0259 mL	0.1293 mL	0.2586 mL	0.6465 mL
	100 mM	0.0207 mL	0.1034 mL	0.2069 mL	0.5172 mL

Keywords

Onametostat

12 Cited Publications

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Onametostat

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Onametostat

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Onametostat

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Onametostat

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Onametostat Related Classifications

HY-101564 Related Classifications