Onametostat (Synonyms: JNJ-64619178)

Name: Onametostat
Brand: MedChemExpress
SKU: HY-101564
Rating: 5.0 (10 reviews)

Cat. No.: HY-101564 Purity: 99.40%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 2086772-26-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Onametostat:

Onametostat (Standard) Get quote

10 Publications Citing Use of MCE Onametostat

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

: 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.

: 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.

: 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.

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PRMT5

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 histone H2A (1 to 130 residues) as substrate after 1 hr in the presence of S-adenosyl-L-methionine by high throughput mass spectrometry 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 histone H2A (1 to 130 residues) as substrate after 1 hr in the presence of S-adenosyl-L-methionine by high throughput mass spectrometry	[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

Molecular Weight

483.36

Formula

C₂₂H₂₃BrN₆O₂

CAS No.

2086772-26-9

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.79%

Select Batch:

Data Sheet (274 KB) SDS (762 KB)

COA (247 KB) HNMR (221 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Onametostat Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Onametostat2086772-26-9JNJ-64619178JNJ64619178JNJ 64619178Histone MethyltransferaseInhibitorinhibitorinhibit

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Onametostat (Synonyms: JNJ-64619178)

Customer Review

Other Forms of Onametostat:

Onametostat Related Antibodies

10 Publications Citing Use of MCE Onametostat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Onametostat Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Onametostat Related Classifications

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