SMARCA2/4 degrader-1

SMARCA2/4 degrader-1 (Compound 1) (10^-7-1 μM; 12-24 h) induces potent, proteasome-dependent degradation of SMARCA2, SMARCA4, and PBRM1 in HEK293T and HCT-116 cells^[1].
SMARCA2/4 degrader-1 (16-25 h) induces SMARCA4 degradation in HEK293T cells with a DC₅₀ of 2.2 nM, relying redundantly on both CRL4^DCAF16 and CRL1^FBXO22 E3 ligase complexes^[1].
SMARCA2/4 degrader-1 forms ternary complexes with SMARCA2 bromodomain and CRL4^DCAF16 (EC₅₀ = 110 nM) or CRL1^FBXO22 (EC₅₀ > 1 μM)^[1].
SMARCA2/4 degrader-1 (1 μM; 24 h) relies on DCAF16 residues C173 and Y62 for SMARCA2 degradation in DCAF16+FBXO22 double KO HEK293T cells, with C173 being a critical covalent binding site^[1].
SMARCA2/4 degrader-1 forms a covalent ternary complex with SMARCA2 bromodomain and DCAF16:DDB1(ΔBPB):DDA1, with the degrader covalently bound to DCAF16 C173 and forming multiple stabilizing non-covalent interactions^[1].

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