Onametostat
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.40%
- No. CAS: 2086772-26-9
- Fòrmula: C22H23BrN6O2
- Peso molecular:483.36
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Reprogramming Compound Library
HY-L039
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Publications Citing Use of MedChemExpress (MCE) Onametostat
More- Gut. 2024 Sep 11:gutjnl-2024-332998. [Abstract]
- Nat Commun. 2023 Jan 6;14(1):97. [Abstract]
- MedComm (2020). 2024 Sep 20;5(10):e705. [Abstract]
- Oncogene. 2024 Jan;43(5):363-377. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Biomed J. 2026 Jun 10:101002. [Abstract]
- bioRxiv. 2026 Apr 13.
- bioRxiv. 2026 Feb 2:2026.01.30.702866. [Abstract]
- SRRN. 2025 Jun 9.
- bioRxiv. 2024 Dec 20:2024.12.17.628905. [Abstract]
- bioRxiv. 2024 Feb 21.
- University of Munich. 2022 Oct.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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In Vivo Efficacy Study
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WB
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Cell Proliferation/Viability Assay
Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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PRMT5 |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
0.25 nM
Compound: JNJ64619178; 21
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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
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[PMID: 30956011] |
| MOLM-13 | IC50 |
<1 nM
Compound: JNJ64619178
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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
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[PMID: 38301329] |
| NCI-H1048 | GI50 |
1.3 nM
Compound: 11; JNJ64619178
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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
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[PMID: 37366223] |
| Sf9 | IC50 |
0.13 nM
Compound: JNJ64619178; 21
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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
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[PMID: 30956011] |
| Sf9 | IC50 |
0.14 nM
Compound: 6; JNJ-64619178
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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
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[PMID: 30366617] |
| Z-138 | IC50 |
<1 nM
Compound: JNJ64619178
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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
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[PMID: 38301329] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2086772-26-9
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Appearance Solid
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Peso molecular 483.36
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Fòrmula C22H23BrN6O2
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Color Off-white to light yellow
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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
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Synonyms
JNJ-64619178
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (12)
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Journal Impact Factor
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Most Recent
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Gut
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.
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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.
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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.
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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
2026 Jun 10:101002. PMID: 42270077 -
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bioRxiv
2026 Feb 2:2026.01.30.702866. PMID: 41676495 -
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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 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (274 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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.
| 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 |
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