P-SETDB1-4

P-SETDB1-4 (5 μM; 24-96 h) exhibits good serum stability, with ~40% of the reagent remaining intact after 24 h incubation in 20% fresh serum^[1].
P-SETDB1-4 (100 μM) binds purified SETDB1 TTDs with high affinity, exhibiting a K_d of 86 nM^[1].
P-SETDB1-4 specifically binds endogenous SETDB1 and CRBN in MCF-7 cell lysates^[1].
P-SETDB1-4 (62.5 nM-1000 nM; 2-24 h) induces CRBN- and proteasome-dependent, post-translational degradation of SETDB1 in MCF-7 and T47D breast cancer cells, with substantial degradation observed at 12 h and dose-dependent effects at concentrations ≥500 nM after 24 h^[1].
P-SETDB1-4 (1 μM; 24-96 h) significantly reduces the viability of MCF-7 and T47D breast cancer cells after 24-96 h of incubation^[1].
P-SETDB1-4 (1 μM; 24 h) decreases DNA synthesis in MCF-7 and T47D breast cancer cells, as shown by reduced EdU-positive cell percentages after 24 h of incubation^[1].
P-SETDB1-4 treatment activates the transcriptome and transposable elements (predominantly LTR-type) in MCF-7 breast cancer cells, upregulating genes involved in focal adhesion, cancer pathways, and p53 signaling, including a 2.1-fold increase in CDKN1A and 1.6-fold increase in SNAIL1^[1].

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