UNC0379

SKU: orb1226042

Description

UNC0379 is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 with IC50 of 7.3 uM, displays good selectivity over 15 other methyltransferases, including G9a and GLP (IC50>100 uM); causes neuroblastoma (NB) cell growth inhibition which is p53 dependent, reduces levels of p53K382me1 modification in xenografts.

Key Properties

• CAS Number: 1620401-82-2
• MW: 413.5563
• Purity: >98% (HPLC)
• Formula: C₂₃H₃₅N₅O₂
• SMILES: COC1=C(OC)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1
• Target: HMTase
• Solubility: 10 mM in DMSO

Bioactivity

• 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. Animal model: Bleomycin (BLM)-induced lung fibrosis mouse model. 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.
• In Vitro:
  UNC0379 (1-10 μM, 9 days) inhibits HGSOC cells proliferation. UNC0379 (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells. UNC0379 (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation. Cell Viability Assay Cell line: JHOS2, JHOS3, JHOS4, OVCAR3, OVCAHO, OVKATE, KURAMOCHI, TYKnu. Concentration: 1-10 μM. Incubation time: 9 days. Result: Inhibited HGSOC cells proliferation with IC50s ranging from 0.39 to 3.20 μM. Cell Cycle Analysis Cell line: JHOS3, OVCAR3. Concentration: 10 μM. Incubation time: 96 h. Result: Arrested cells in sub-G1 phase.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

UNC 0379 | UNC-0379

Quick Database Links

Gene Symbol

HMTase