PIP-199 is the most selective inhibitor of the RMI core complex/MM2 interaction.

Altretamine is an alkylating agent proposed as an antineoplastic.

Treosulfan is an alkylating agent used for conventional, as well as high-dose chemotherapy regimens, whereby plasma concentrations over 500 μg/mL can be achieved.

CB 1954 is an anticancer prodrug used in gene therapy research and is activated by NAD(P)H Quinone Oxidoreductase 2.

Lobaplatin is a diastereometric mixture of platinum(II) complexes containing a 1,2-bis(aminomethyl)cyclobutane stable ligand and lactic acid as the leaving group. Its antitumour activity results from the formation of DNA-drug adducts, mainly as GG and AG intra-strand cross-links.

Pipobroman is an anti-cancer drug that probably acts as an alkylating agent.

Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic and immunosuppressive activities.

Nedaplatin is a derivative of cisplatin and DNA damage agent.

Bendamustine is a DNA cross-linking agent.

Carmustine is a cell-cycle phase nonspecific alkylating antineoplastic agent.

Busulfan is a bifunctional alkylating agent.

Thio-TEPA is an alkylating agent used to treat cancer, this molecule features tetrahedral phosphorus and is structurally akin to phosphate.

Ifosfamide is a nitrogen mustard alkylating agent used in the treatment of cancer.

Procarbazine HCl, an antineoplastic chemotherapy drug, is an alkylating agent for the treatment of Hodgkin's lymphoma and certain brain cancers and also inhibits MAO thus increasing the effects of sympathomimetics, TCAs, and tyramine.

Lomustine is an alkylating nitrosourea compound used in chemotherapy. Lomustine (420 μM) triggers apoptosis through the mitochondrial pathway via decrease in the level of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively, in both medulloblastoma and normal human epithelial and fibroblast cells. Lomustine induces cell cycle delay in G2/M phase in medulloblastoma cells and up-regulates p21 protein level in a p53-independent manner in HFSN1 cells.

RITA induced both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks. It is MDM2-p53 interaction inhibitor and activates p53 expression.

Palifosfamide is the functional active metabolite of ifosfamide (IFOS), a bi-functional DNA alkylator being investigated as a potential therapy for the treatment of soft tissue sarcoma (STS).