For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I015198 |
| CAS Number | 2421117-98-6 |
| Synonyms | (2S)-3-(1H-indol-3-yl)-N-[4-(4-methoxyphenyl)-1,3-thiazol-2-yl]-2-[(4-methylphenyl)sulfonylamino]propanamide |
| Molecular Formula | C28H26N4O4S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H26N4O4S2/c1-18-7-13-22(14-8-18)38(34,35)32-25(15-20-16-29-24-6-4-3-5-23(20)24)27(33)31-28-30-26(17-37-28)19-9-11-21(36-2)12-10-19/h3-14,16-17,25,29,32H,15H2,1-2H3,(H,30,31,33)/t25-/m0/s1 |
| InChIKey | VLPGAOXBMXGNGM-VWLOTQADSA-N |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)NC(CC2=CNC3=CC=CC=C32)C(=O)NC4=NC(=CS4)C5=CC=C(C=C5)OC |
| 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. |
