| Bioactivity | 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[1][2][3]. |
| Target | SETD8 (KMT5A) |
| Invitro | 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]. Cell Viability Assay[1] Cell Line: |
| In Vivo | UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse[3]. Animal Model: |
| Name | UNC0379 TFA |
| CAS | 1620401-83-3 |
| Formula | C25H36F3N5O4 |
| Molar Mass | 527.58 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. [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. [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. |
UNC0379 TFA
CAS: 1620401-83-3 F: C25H36F3N5O4 W: 527.58
UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC50 of 7.
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