BRD4/FKBP12 ligand 2

BRD4/FKBP12 ligand 2 (compound a1d) (5 days) reduces viability of FKBP12-replete MV4-11 cells with an IC₅₀ of 235 nM, and shows a 138-fold reduction in potency ratio in FKBP12-depleted MV4-11 cells (IC₅₀ = 1.7 nM)^[1].
BRD4/FKBP12 ligand 2 (5 days) potently reduces viability of wild-type INA-6 cells with an IC₅₀ of 0.4 nM, and shows reduced potency (IC₅₀ = 480 nM) in FKBP12-knockout INA-6 cells^[1].
BRD4/FKBP12 ligand 2 (10-100 nM; 6 hours) represses MYC mRNA expression in FKBP12-replete MV4-11 cells in a FKBP12-dependent manner^[1].
BRD4/FKBP12 ligand 2 binds to purified FKBP12 protein with a K_d of 1.0 nM^[1].
BRD4/FKBP12 ligand 2 binds to purified BRD4 BD1 and BRD4 BD2 domains with K_d values of 680 nM and 440 nM, respectively, in the absence of FKBP12^[1].
BRD4/FKBP12 ligand 2 binds to purified BRD4 BD1 domain with 27-fold positive cooperativity (K_d = 25 nM) in the presence of 15 μM FKBP12^[1].
BRD4/FKBP12 ligand 2 binds to purified BRD4 BD2 domain with 7.7-fold positive cooperativity (K_d = 57 nM) in the presence of 15 μM FKBP12^[1].
BRD4/FKBP12 ligand 2 induces formation of ternary complexes between purified eGFP-FKBP12 and His-BRD4 BD1 protein or His-BRD4 BD2 protein^[1].
BRD4/FKBP12 ligand 2 binds to intracellular FKBP12 and BRD4 in HEK293T cells with IC₅₀ values of 14 nM and 820 nM, respectively, as measured by NanoBRET assay^[1].

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