UNC0379
Based on 7 publication(s) in Google Scholar
UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.3 μM, KD value of 18.3 μM. UNC0379 can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.17%
- No. CAS: 1620401-82-2
- Fòrmula: C23H35N5O2
- Peso molecular:413.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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
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Help & FAQs
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Epigenetics Compound Library
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Publications Citing Use of MedChemExpress (MCE) UNC0379
More- Cell Metab. 2021 Jan 5;33(1):160-173.e6. [Abstract]
- Nat Commun. 2024 Jun 10;15(1):4920. [Abstract]
- Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
- Diabetologia. 2025 Apr;68(4):835-853. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- Sci Rep. 2020 Mar 11;10(1):4490. [Abstract]
- J Gastroenterol Hepatol. 2021 Oct;36(10):2850-2863. [Abstract]
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Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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SETD8/KMT5A |
UNC0379 (1-10 μM, 9 days) inhibits HGSOC cells proliferation[2].
UNC0379 (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells[2].
UNC0379 (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu
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Concentration:1-10 μM
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Incubation Time:9 days
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Result:Inhibited HGSOC cells proliferation with IC50s ranging from 0.39 to 3.20 µM.
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Cell Line:JHOS3, OVCAR3
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Concentration:10 µM
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Incubation Time:96 h
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Result:Arrested cells in sub-G1 phase.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin (BLM)-induced lung fibrosis mouse model[3]
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Dosage:1 mg/kg/day
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Administration:Intratracheal administration, on day7, 8, and 9.
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Result:Ameliorated BLM-induced lung fibrosis (supported by the evaluation of the Ashcroft score and changes in the collagen content in the lung samples) without affecting pulmonary inflammation.
Chemical Information
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No. CAS 1620401-82-2
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Appearance Solid
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Peso molecular 413.56
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Fòrmula C23H35N5O2
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Color Off-white to yellow
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SMILES
COC1=C(OC)C=C2C(N=C(N3CCCC3)N=C2NCCCCCN4CCCC4)=C1
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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 1 year -20°C 6 months
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell Metab
Di-methylation of CD147-K234 Promotes the Progression of NSCLC by Enhancing Lactate Export. [Abstract]2021 Jan 5;33(1):160-173.e6. PMID: 33406400
UNC0379 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Jan 5;33(1):160-173.e6. [Abstract]
In vitro methyltransferase assay, with recombinant KMT5A and CD147 proteins incubated in methyltransferase buffer containing the methyl donor SAM. The di-methylation of CD147 was detected by western blot with a pan-anti-di-methylated-lysine antibody (DM). The KMT5A inhibitor UNC0379 was included as a negative control.
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Nat Commun
PR-SET7 epigenetically restrains uterine interferon response and cell death governing proper postnatal stromal development. [Abstract]2024 Jun 10;15(1):4920. PMID: 38858353
UNC0379 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 10;15(1):4920. [Abstract]
WB analysis of H4K20me1 level in cultured endometrial stromal cells treated with DMSO (CTR) or UNC0379 (5 μM).
UNC0379 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 10;15(1):4920. [Abstract]
Immunofluorescence analysis showed the dsRNA level of J2 in cultured endometrial stromal cells treated with DMSO (control group, CTR) or UNC0379 (5 μM).
UNC0379 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 10;15(1):4920. [Abstract]
Annexin V/PI apoptosis analysis of cultured endometrial stromal cells treated with DMSO (CTR) or UNC0379 (5 μM).
UNC0379 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Jun 10;15(1):4920. [Abstract]
Immunoblotting analysis of p-RIPK3, RIPK3, p-MLKL, MLKL, Cleaved CASPASE-3, ZBP1 and H4K20me1 in Zbp1+/− stromal cells treated with DMSO or UNC0379 and Zbp1−/− stromal cells treated with DMSO or UNC0379.
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Cell Death Dis
Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. [Abstract]2018 Jan 26;9(2):129. PMID: 29374157
UNC0379 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.
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Diabetologia
Single-cell RNA sequencing identifies endothelial-derived HBEGF as promoting pancreatic beta cell proliferation in mice via the EGFR-Kmt5a-H4K20me pathway. [Abstract]2025 Apr;68(4):835-853. PMID: 39694915 -
Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Sci Rep
Downregulation of histone methyltransferase SET8 inhibits progression of hepatocellular carcinoma. [Abstract]2020 Mar 11;10(1):4490. PMID: 32161353 -
J Gastroenterol Hepatol
SETD8 involved in the progression of inflammatory bowel disease via epigenetically regulating p62 expression. [Abstract]2021 Oct;36(10):2850-2863. PMID: 33991018
Solvente y solubilidad
DMSO : 50 mg/mL (120.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: ≥ 2.5 mg/mL (6.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33. [Content Brief]
[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686. [Content Brief]
[3]. Keita Ugai, et al. Inhibition of the SET8 Pathway Ameliorates Lung Fibrosis Even Through Fibroblast Dedifferentiation. Front Mol Biosci. 2020 Aug 5;7:192. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4180 mL | 12.0901 mL | 24.1803 mL | 60.4507 mL |
| 5 mM | 0.4836 mL | 2.4180 mL | 4.8361 mL | 12.0901 mL | |
| 10 mM | 0.2418 mL | 1.2090 mL | 2.4180 mL | 6.0451 mL | |
| 15 mM | 0.1612 mL | 0.8060 mL | 1.6120 mL | 4.0300 mL | |
| 20 mM | 0.1209 mL | 0.6045 mL | 1.2090 mL | 3.0225 mL | |
| 25 mM | 0.0967 mL | 0.4836 mL | 0.9672 mL | 2.4180 mL | |
| 30 mM | 0.0806 mL | 0.4030 mL | 0.8060 mL | 2.0150 mL | |
| 40 mM | 0.0605 mL | 0.3023 mL | 0.6045 mL | 1.5113 mL | |
| 50 mM | 0.0484 mL | 0.2418 mL | 0.4836 mL | 1.2090 mL | |
| 60 mM | 0.0403 mL | 0.2015 mL | 0.4030 mL | 1.0075 mL | |
| 80 mM | 0.0302 mL | 0.1511 mL | 0.3023 mL | 0.7556 mL | |
| 100 mM | 0.0242 mL | 0.1209 mL | 0.2418 mL | 0.6045 mL |
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