SJ6986 is a degrader of G1 to S phase transition 1 (GSPT1) and GSPT2.1 It reduces the levels of GSPT1 and GSPT2 in MV4-11 cells in a concentration-dependent manner. SJ6986 inhibits proliferation of MV4-11, MHH-CALL-4, MB002, MB004, and HD-MB03 cells (EC50s = 1.5, 0.4, 726, 336, and 3,583 nM, respectively) and reduces the viability of MV4-11 cells endogenously expressing cereblon but not MV4-11 cereblon knockout cells.
1.Nishiguchi, G., Keramatnia, F., Min, J., et al.Identification of potent, selective, and orally bioavailable small-molecule GSPT1/2 degraders from a focused library of cereblon modulatorsJ. Med. Chem.64(11)7296-7311(2021)