KRAS G12D-IN-37 is a KRASG12D inhibitor. KRAS G12D-IN-37 shows antiproliferative activity against KRASG12D mutant tumor cells and minimal cytotoxicity toward normal cells. KRAS G12D-IN-37 binds stably to KRASG12D via hydrogen bond interactions with residues His 95, Arg 68, and Asp 12, and inhibits downstream ERK/AKT signaling pathways. KRAS G12D-IN-37 elevates ROS levels, induces apoptosis, disrupts mitochondrial membrane potential. KRAS G12D-IN-37 downregulates the level of anti-apoptotic protein Bcl-2, and upregulates the levels of pro-apoptotic proteins Bax and caspase 3. KRAS G12D-IN-37 can be used for the research of cancer, such as gastric adenocarcinoma and colorectal cancer[1].
Molekulargewicht:
557.61
Formel:
C29H34F3N5O3
Target-Kategorie:
Akt,Apoptosis,Bcl-2 Family,Caspase,ERK,Ras,Reactive Oxygen Species (ROS)
Anwendungsbeschreibung:
MCE Product type: Reference compound
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