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KL-50 is a selective toxin toward tumors that lack the DNA repair protein O6-methylguanine-DNA-methyltransferase (MGMT), which reverses the formation of O6-alkylguanine lesions. KL-50 activates DNA damage response pathways and cycle arrest in MGMT-cells, independent of mismatch repair (MMR). KL-50 is promising for research of brain tumors that lack the DNA repair protein MGMT[1][2].

[1] Huseman ED, et al. Mechanism of Action of KL-50, a Candidate Imidazotetrazine for the Treatment of Drug-Resistant Brain Cancers. J Am Chem Soc. 2024 Jul 10;146(27):18241-18252. DOI:10.1021/jacs.3c06483
[2] HERZON Seth, et al. Preparation of imidazotetrazine compounds and methods for treating cancers that are MGMT deficient regardless of MMR status. WO2023049806. 2022 September 22.