Catalog No.: PC-72696Not For Human Use, Lab Use Only.
DTP3 (MKK7 inhibitor DTP3) is a specific D-tripeptide that disrupts the GADD45β/MKK7 complex (Kd=64.8 nM), kills MM cells effectively, and lacks toxicity to normal cells.
DTP3 (MKK7 inhibitor DTP3) is a specific D-tripeptide that disrupts the GADD45β/MKK7 complex (Kd=64.8 nM), kills MM cells effectively, and lacks toxicity to normal cells.
DTP3 bind to MKK7, but not to GADD45β, DTP3 dissociates the GADD45β/MKK7 complex via an allosteric mechanism, potentially involving a conformational rearrangement of the kinase.
DTP3 demonstrated potent and cancer-selective activity in MM cells from patients, effectively kills MM cells by inducing MKK7/JNK-dependent apoptosis, displayed synergistic activity with bortezomib in different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells.
DTP3 exhibited potent therapeutic activity against MM in vivo, in the absence of any apparent side effects.
