UNC0379 TFA
Based on 8 publication(s) in Google Scholar
UNC0379 TFA 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 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 1620401-83-3
- Formule: C25H36F3N5O4
- Masse moléculaire:527.58
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
Other In-stock Forms of UNC0379 TFA
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) UNC0379 TFA
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]
- iScience. 2026 Jul 21;29(8):116902.
- J Gastroenterol Hepatol. 2021 Oct;36(10):2850-2863. [Abstract]
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Voir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
Description
IC50 & Target
SETD8 (KMT5A)[1]
In Vitro
UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation[2].
UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells[2].
UNC0379 TFA (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.
In Vivo
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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CAS No. 1620401-83-3
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Appearance Solid
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Masse moléculaire 527.58
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Formule C25H36F3N5O4
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Color Light yellow to khaki
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SMILES
COC1=C(OC)C=C2C(N=C(N3CCCC3)N=C2NCCCCCN4CCCC4)=C1.O=C(O)C(F)(F)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (8)
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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 TFA 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 TFA 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 TFA 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 TFA 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 TFA 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 TFA 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 -
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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
Solvant et solubilité
In Vitro:
H2O : 100 mg/mL (189.54 mM; Need ultrasonic)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.8954 mL | 9.4772 mL | 18.9545 mL | 47.3862 mL |
| 5 mM | 0.3791 mL | 1.8954 mL | 3.7909 mL | 9.4772 mL | |
| 10 mM | 0.1895 mL | 0.9477 mL | 1.8954 mL | 4.7386 mL | |
| 15 mM | 0.1264 mL | 0.6318 mL | 1.2636 mL | 3.1591 mL | |
| 20 mM | 0.0948 mL | 0.4739 mL | 0.9477 mL | 2.3693 mL | |
| 25 mM | 0.0758 mL | 0.3791 mL | 0.7582 mL | 1.8954 mL | |
| 30 mM | 0.0632 mL | 0.3159 mL | 0.6318 mL | 1.5795 mL | |
| 40 mM | 0.0474 mL | 0.2369 mL | 0.4739 mL | 1.1847 mL | |
| 50 mM | 0.0379 mL | 0.1895 mL | 0.3791 mL | 0.9477 mL | |
| 60 mM | 0.0316 mL | 0.1580 mL | 0.3159 mL | 0.7898 mL | |
| 80 mM | 0.0237 mL | 0.1185 mL | 0.2369 mL | 0.5923 mL | |
| 100 mM | 0.0190 mL | 0.0948 mL | 0.1895 mL | 0.4739 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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