MGMT Inhibitor

Lomeguatrib is a O⁶-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC₅₀s of 9 nM in cell-free assay and ～6?nM in MCF-7 cells.

O6BTG-octylglucoside is a potent O⁶-methylguanine-DNAmethyl-transferase (MGMT) inhibitor, with IC₅₀s of 32 nM in vitro (cell extracts) and 10 nM in HeLa S3 cells.

MGMT-IN-1 (Compound 2) is a light-activated MGMT inhibitor. MGMT-IN-1 can effectively enhance the cytotoxicity of Temozolomide (TMZ) (HY-17364) only under light conditions, significantly increasing the DNA damage caused by TMZ. MGMT-IN-1 can be used for the study of chordoma.

Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM).