GSK343

SKU: orb1301110

Description

GSK343

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1346704-33-3
• MW: 541.69
• Purity: 99.90%
• Formula: C₃₁H₃₉N₇O₂
• SMILES: CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccnc(c1)N1CCN(C)CC1
• Target: Autophagy,Histone Methyltransferase
• Solubility: DMSO:22.27 mg/mL (41.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.85 mM)

Bioactivity

• Target IC50:
  EZH2:4 nM
• In Vivo:
  Mice treated with GSK343 (5 mg/kg) displayed significantly inhibited tumor growth compared to the control group. The average volume and weight of tumors in the GSK343-treated group were notably decreased. This reduction in tumor growth was evident as early as 20 days post-implantation and continued throughout the study. Furthermore, in the GSK343-treated animals within the xenograft model, there was a substantial increase in the levels of E-cadherin mRNA, alongside a significant decrease in vimentin mRNA levels, compared to the control group.
• Cell Research:
  To account for varying doubling rates among cancer cell lines, the optimal cell seeding is determined empirically for all cell lines by examining their growth in a 384-well plate over 6 days with a wide range of seeding densities. Cells are then plated at the optimal seeding density and allowed to adhere overnight. Cells are treated in duplicate with a 20-point 2-fold dilution series of compound or 0.147% DMSO (vehicle control) and incubated for 6 days at 37C in 5% CO2. Cells are then lysed with 25 μl CellTiter-Glo per well and chemiluminescence is quantified with a TECAN Safire2 microplate reader. In addition, an untreated plate of cells is harvested at the time of compound addition (T0) to quantify the starting number of cells. CTG values after 6 days of treatment were expressed as a percent of the T0 value and plotted against compound concentration. Data are fit with a 4-parameter equation to generate a concentration response curve and the concentration of compound required to inhibit 50% of growth (gIC50) is determined(Only for Reference)

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, EZH2, EZH1, GSK 343, GSK343, GSK-343, Inhibitor, Histone Methyltransferase, HistoneMethyltransferase, inhibit

Compound Identifiers

PubChem CID

71268957