UNC0379
UNC0379 Basic information
- Product Name:
- UNC0379
- Synonyms:
-
- UNC0379
- 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine
- 6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine UNC0379
- UNC0379, >=98%
- UNC03
- 6,7-Dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine
- UNC0379, UNC-0379, UNC 0379
- UNC 0379; UNC-0379
- CAS:
- 1620401-82-2
- MF:
- C23H35N5O2
- MW:
- 413.56
- Product Categories:
-
- Inhibitors
- Mol File:
- 1620401-82-2.mol
UNC0379 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.
UNC0379 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) Ma et al. (2014), Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8; J. Med. Chem. 57 6822 2) Veschi et al. (2017), Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma; Cancer Cell 31 50
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