BC-DXI-495 is a AIMP2-DX2 inhibitor. BC-DXI-495 disrupts the interaction of HSP70 and destabilizes DX2. BC-DXI-495 induces DX2 degradation via Siah1 -mediated ubiquitination. BC-DXI-495 exerts tumor suppressive activity in cancer cells. BC-DXI-495 serves as a chemical probe to elucidate the mechanism of action of arylsulfonamide-based DX2 inhibitors. BC-DXI-495 can be used in lung cancer research [1].
In Vitro, BC-DXI-495 (Compound 2) inhibits the level of NanoLuciferase-tagged DX2 by 67.10%[1]. BC-DXI-495 inhibits the degradation of DX2 protein, with an IC50 value of 4.20 μM[1]. BC-DXI-495 (72 h) inhibits the viability of A549 lung cancer cells with an EC50 of 14.2 μM[1].
References:
[1]. Sivaraman A, 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;63(10):5139-5158.
In Vitro, BC-DXI-495 (Compound 2) inhibits the level of NanoLuciferase-tagged DX2 by 67.10%[1]. BC-DXI-495 inhibits the degradation of DX2 protein, with an IC50 value of 4.20 μM[1]. BC-DXI-495 (72 h) inhibits the viability of A549 lung cancer cells with an EC50 of 14.2 μM[1].
References:
[1]. Sivaraman A, 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;63(10):5139-5158.