ME0328

SKU: orb1223300

Description

ME0328 is an inhibitor of PARP-3 (IC50 = 0.89 μM). ME0328 displays selectivity for PARP-3 over PARP-1, PARP-2 and other ARDT enzymes (IC50 values are 6.3, 10.8 and >30 μM respectively). ME0328 also enhances CRISPR-Cas9-mediated HER2 mutation frequency, resulting in increased reduction in proliferation of HER2-positive breast cancer cells.(In Vitro):ME0328 is a potent and selective inhibitor of ARTD3/PARP3 that is active in cells. In in vitro histone H1 modification assay, ME0328 inhibits the transferase activity of ARTD3 with an IC50 of 0.89±0.28 μM. In human A549 cells, ME0328 and ME0355 (at 10 μM) delay the resolution of γH2AX-containing foci that serve as markers for DNA double strand break repair following γ-irradiation (2 Gy). In silico and in vitro physicochemical and metabolic profiling indicated that ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes.

Key Properties

• CAS Number: 1445251-22-8
• MW: 321.37
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₉N₃O₂
• SMILES: C[C@H](NC(=O)CCC1=NC2=CC=CC=C2C(=O)N1)C1=CC=CC=C1
• Target: Tyrosinase
• Solubility: DMSO : 75 mg/mL. 233.38 mM;H2O : < 0.1 mg/mL

Bioactivity

• In Vitro:
  ME0328 is a potent and selective inhibitor of ARTD3/PARP3 that is active in cells. In in vitro histone H1 modification assay, ME0328 inhibits the transferase activity of ARTD3 with an IC50 of 0.89±0.28 μM. In human A549 cells, ME0328 and ME0355 (at 10 μM) delay the resolution of γH2AX-containing foci that serve as markers for DNA double strand break repair following γ-irradiation (2 Gy). In silico and in vitro physicochemical and metabolic profiling indicated that ME0328 is soluble, cell permeable, and metabolically stable in human liver microsomes and rat hepatocytes.

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

ME0328 | ME 0328 | ME-0328

Quick Database Links

Gene Symbol

Tyrosinase