UNC0379 (TFA)

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].

Product Specifications

CAS Number

[1620401-83-3]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/UNC0379-trifluoroacetate.html

Purity

99.91

Solubility

H2O : 100 mg/mL (ultrasonic)

Smiles

COC1=C(OC)C=C2C(N=C(N3CCCC3)N=C2NCCCCCN4CCCC4)=C1.O=C(O)C(F)(F)F

Molecular Formula

C25H36F3N5O4

Molecular Weight

527.58

References & Citations

[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.