Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BC-DXI-843 is inhibitor of AIMP2-DX2, and is potential for development of novel therapeutics targeting AIMP2-DX2 in lung cancer.
説明 | BC-DXI-843 is inhibitor of AIMP2-DX2, and is potential for development of novel therapeutics targeting AIMP2-DX2 in lung cancer. |
ターゲット&IC50 | AIMP2-DX2:0.92 μM (IC50), AIMP2:IC50 >100 μM |
In vitro | Optimization of hit BC-DXI-04 (IC50 = 40.1 μM) provided new potent sulfonamide based AIMP2-DX2 inhibitors.?Among these, BC-DXI-843 showed improved inhibition against AIMP2-DX2 (IC50 = 0.92 μM) with more than 100-fold selectivity over AIMP2 in a luciferase assay.?Several binding assays indicated that this compound effectively induces cancer cell apoptosis by specifically interrupting the interaction between DX2 and HSP70, which leads to the degradation of DX2 via Siah1-mediated ubiquitination. |
In vivo | BC-DXI-843 demonstrated in vivo efficacy in a tumor xenograft mouse model (H460 cells) at a dosage of 50 mg/kg, suggesting it as a promising lead for development of novel therapeutics targeting AIMP2-DX2 in lung cancer. |
分子量 | 546.66 |
分子式 | C28H26N4O4S2 |
CAS No. | 2421117-98-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 245 mg/mL (448.18 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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BC-DXI-843 2421117-98-6 Others Inhibitor BC-DXI 843 lung A549 BC-DXI843 BCDXI843 AIMP2-DX2 cancer inhibit BC DXI 843 inhibitor