| Identification | Back Directory | [Name]
UNC0379 | [CAS]
1620401-82-2 | [Synonyms]
UNC03
UNC0379
CS-1767
UNC0379, >=98%
UNC0379 USP/EP/BP
UNC 0379; UNC-0379
UNC0379, UNC-0379, UNC 0379
6,7-Dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-4-quinazolinamine
6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine
4-Quinazolinamine, 6,7-dimethoxy-2-(1-pyrrolidinyl)-N-[5-(1-pyrrolidinyl)pentyl]-
6,7-dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine UNC0379 | [Molecular Formula]
C23H35N5O2 | [MDL Number]
MFCD28167817 | [MOL File]
1620401-82-2.mol | [Molecular Weight]
413.57 |
| Chemical Properties | Back Directory | [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) | [form ]
solid | [pka]
10.54±0.20(Predicted) | [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. |
| Hazard Information | Back Directory | [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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