DTP3 是一种选择性 MKK7/GADD45β 抑制剂,靶向 NF-Κb 通路,可抑制癌症。
产品描述
DTP3 is a selective MKK7/GADD45β inhibitor, which inhibits cancer-selective NF-κB survival pathway.
体外活性
DTP3 physically interacts with MKK7 in isolation and within the complex with GADD45β, and dissociates the GADD45β/MKK7 complex via an allosteric mechanism. DTP3 selectively kills cells and induces apoptosis in MM cells with functional MKK7 and elevated GADD45β expression without toxicity to normal cells. In addition, DTP3 displays synergistic activity with bortezomib in two different MM cell lines, exhibiting a combination index of 0.56 in KMS-12 cells and of 0.21 in U266 cells. [1]
体内活性
DTP3 treatment with 14.5 mg/kg/day exhibits potent antitumor activity against MM in mouse plasmacytoma model. [1]
Cas No.
1809784-29-9
分子式
C26H35N7O5
分子量
525.6
储存和溶解度
Ethanol:100 mg/ml (190.26 mM)
H2O:100 mg/ml (190.26 mM)
DMSO:100 mg/ml (190.26 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years