ChemicalBook Product Catalog Biochemical Engineering Inhibitors Epigenetics Histone Methyltransferase Inhibitors UNC0379

UNC0379

Product NameUNC0379
CAS1620401-82-2
MFC23H35N5O2
MW413.56
EINECS
MOL File1620401-82-2.mol

Chemical Properties

Boiling point	606.3±65.0 °C(Predicted)
Density	1.168±0.06 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2–8 °C
solubility	Soluble in DMSO (up to 30 mg/ml)
pka	10.54±0.20(Predicted)
form	solid
color	Tan
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

Usage And Synthesis

Description

UNC0379 (CAS 1620401-82-2) is an inhibitor of the lysine methyltransferase SETD8 with selectivity over 15 other methyltransferases.1 IC50’s = 7.3 μM in a radioactive methyl transfer assay and 9.0 μM in an MCE assay. UNC0379 treatment of SY5Y and NGP neuroblastoma cell lines lead to activation of p53 and decreased tumor growth in an ex-vivo tumorigenicity assay.2

Uses

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].

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:	Bleomycin (BLM)-induced lung fibrosis mouse model^[3]
Dosage:	1 mg/kg/day
Administration:	Intratracheal administration, on day7, 8, and 9.
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.

IC 50

SETD8/KMT5A

References

[1] ANQI MA. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8[J]. Journal of Medicinal Chemistry, 2014, 57 15: 6822-6833. DOI:10.1021/jm500871s
[2] VERONICA VESCHI. Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma.[J]. Cancer Cell, 2017, 31 1 1: 50-63. DOI:10.1016/j.ccell.2016.12.002

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