UNC0379_product_DataBase

Bioactivity

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[1][2][3].

Target

SETD8 (KMT5A)

Invitro

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]. Cell Viability Assay[1] Cell Line:

In Vivo

UNC0379 (intratracheal administration, 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

CAS

1620401-82-2

Formula

C23H35N5O2

Molar Mass

413.56

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

PeptideDB

UNC0379

CAS: 1620401-82-2 F: C23H35N5O2 W: 413.56