TD-522

TD-522 (0.064 nM-1 μM, 72 h) exhibits strong anti-proliferative effects in both KG-1 (EC₅₀ = 0.5 nM) and TMD-8 (EC₅₀ = 5.2 nM) cell lines, and shows no cytotoxic effect on VERO cells^[1].
TD-522 (0.001-10 μM, 6 h) induces effectively GSPT1 degradation in a dose-dependent manner in KG1 cells, slightly degraded IKZF1 and shows no effect on CK1α^[1].
TD-522 (1 μM, 3 h) significantly decreases the protein levels of GSPT1 and MYC in KG1 cells, while not affecting other IMiD’s well-known neosubstrates including IKZF1 and CK1α^[1].
TD-522 displays weak hERG inhibition (IC₅₀ = 31.6 μM) and weak inhibition of CYP 1A2, 2D6, and 3A4 at 10 μM, while exhibiting potent inhibition of CYP2C9 and 2C19^[1].
TD-522 (0.001-10 μM) degrades GSPT1 and exerts its cytotoxic effects in KG-1 cells by activating the integrated stress response pathway, including the upregulation of ATF4, CHOP, and ATF3, thereby inducing apoptotic cell death^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.