BK50164

BK50164 is a potent CD73 inhibitor with an IC50 value of 13.089 µM. BK50164 binds to CD99 with a KD value of 1.5 µM. BK50164 shows antiproliferative activity. BK50164 induced Apoptosis and cell cycle arrest at Sub-G1 phase[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

IC50: 13.089 µM (CD73)[1]

BK50164 (0-400 µM；48 小时) 显示抗增殖活性，对 A4573, TC-32, TC-71, Saos-2, U-2 OS 细胞的 IC50 值分别为35.8, 34.28, 5.17, ≥400, ≥400 µM[2]。 BK50164 (4-16 µM; 48 h) 诱导细胞凋亡和细胞周期停滞在 Sub-G1 期[2]。 Cell Viability Assay[2] Cell Line: A4573, TC-32, TC-71, Saos-2, U-2 OS cells Concentration: 0-400 µM Incubation Time: 48 h Result: Inhibited cell viability witn IC50s of 35.8, 34.28, 5.17, ≥400, ≥400 µM for A4573, TC-32, TC-71, Saos-2, U-2 OS cells, respectively. Cell Cycle Analysis[2] Cell Line: TC-32, U-2 OS cells Concentration: 4, 8, 16 µM Incubation Time: 48 h Result: Induced apoptosis in only TC-32 ES cells but not in U-2 OS cell line and induces cell cycle arrest at Sub-G1 phase.

[1]. Roland Joseph Billedeau, et al. Ectonucleotidase inhibitors and methods of use thereof. WO2018119284A1.

[2]. Balaraman K, et al. Design, synthesis and biological evaluation of Nucleosidic CD99 inhibitors that selectively reduce Ewing sarcoma viability. Eur J Med Chem. 2023 May 5;251:115244.