Bioactivity | BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC50 of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC50 >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer[1]. |
Target | IC50: 0.92 μM (AIMP2-DX2), IC50: >100 μM (AIMP2) |
Invitro | BC-DXI-843 (0.0316-31.6 μM; 72 hours) suppresses cancer cell proliferation in a DX2-dependent manner. The EC50 in A549 cells is 1.20 μM, which is similar to the IC50 for inhibition of DX2. However, no inhibition of WI-26 cells is observed, suggesting that BC-DXI-843 specifically reduces the viability of cancer cells[1]. Cell Proliferation Assay[1] Cell Line: |
In Vivo | BC-DXI-843 (50 mg/kg; intraperitoneally administered; every other day for 15 days) demonstrates in vivo efficacy in a tumor xenograft mouse model (H460 cells)[1]. Animal Model: |
Name | BC-DXI-843 |
CAS | 2421117-98-6 |
Formula | C28H26N4O4S2 |
Molar Mass | 546.66 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. Aneesh Sivaraman, et al. Synthesis and Structure-Activity Relationships of Arylsulfonamides as AIMP2-DX2 Inhibitors for the Development of a Novel Anticancer Therapy. J Med Chem. 2020 May 28;63(10):5139-5158. |