alkylating

N-Nitroso-N-methylurea (NMU MNU NMH) is a nitrosourea compound with alkylating, carcinogenic, and mutagenic properties; as a direct-acting alkylating agent, it interacts with DNA and targets multiple animal organs to induce various cancers and degenerative diseases, and is commonly used to induce disease models such as gastric cancer and breast cancer in mice.

Iodoacetamide, an alkylating agent, is commonly utilized for cysteine alkylation in proteomics sample preparation.

Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Semustine, a DNA alkylating agent, is a cancer chemotherapy compound that is nephrotoxic in patients with malignant melanoma receiving adjuvant chemotherapy for the adjuvant treatment of leukemia.

Ecomustine is a water-soluble nitrosoureido sugar derived from acosamine, with alkylating activity. Ecomustine is a novel antitumor compound that alkylates and crosslinks DNA, thereby inhibiting replication and transcription and eventually resulting in a reduction of cellular proliferation.

CEP-40125 (RXDX-107) is a DNA alkylating agent used for researching advanced solid tumors.

Sarmustine (SarCNU) is an alkylating agent with anticancer activity that inhibits the growth of prostate cancer cells via p53-dependent and p53-independent pathways.Sarmustine mediates the selection of P140K methylguanine-DNA-methyltransferase-transduced human CD34(+) cells in vitro.

APE1-IN-1 is a potent inhibitor of purine pyrimidine endonuclease 1 (APE1) that crosses the blood-brain barrier, exhibits potential antitumor activity, and enhances the cytotoxicity of the alkylating agent [methyl methanesulfonate] on cancer cells.

Laromustine (VNP40101M) is a sulfonyl hydrolytic alkylating prodrug used in cancer therapy with significant anticancer activity. Inhibiting thioredoxin reductase can be used to study acute myeloid leukemia.

Bendamustine hydrochloride (EP-3101) (IC50 of 50 μM) is an alkylating agent associated with DNA damage.

Cyclophosphamide hydrate is a synthetic alkylating agent structurally related to nitrogen mustards, with antitumor and immunosuppressive activities. It is widely used in the treatment of various cancers and is also commonly employed to induce animal models of premature ovarian failure, myelosuppression, cystitis, and myocarditis.

Busulfan is an alkylating antineoplastic agent derived from dimethane sulfonate, with cytotoxic and immunosuppressive properties. It primarily acts by forming carbonium ions in vivo, which induce cross-linking between DNA strands or between DNA and proteins, leading to DNA damage, inhibition of DNA replication, and suppression of RNA transcription. In addition, Busulfan can inhibit thioredoxin reductase and induce apoptosis. It is commonly used as a myeloablative agent in preconditioning regimens for bone marrow transplantation and can also be used to establish anemia models.

Altretamine (ENT-50852) is an alkylating agent with antineoplastic activity.

Ethylene dimethanesulfonate has selective pro-apoptotic effects on LCs. Ethylene dimethanesulfonate is a mild alkylating, non-volatile methanesulfonic diester of ethylene glycol. 

Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.

Methoxyamine HCl (Methoxyamine) covalently binds to apurinic apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER), which may result in an increase in DNA strand breaks and apoptosis. Methoxyamine is an orally bioavailable small molecule inhibitor with potential adjuvant activity. This agent may potentiate the anti-tumor activity of alkylating agents.

Carmustine (bis-chloroethylnitrosourea) is a cell-cycle phase nonspecific alkylating antineoplastic agent.

Satraplatin (BMS182751) is an orally available antineoplastic platinum(IV) complex.Satraplatin has a favorable toxicity profile and appears to have clinical activity against a variety of malignancies.

Aniline mustard (Mesylerythrol) is alkylating mustard with anti-neoplastic activity.

Aniline-MPB-amino-C3-PBD is a cytotoxic agent with a non-alkylating group and acts as a sequence-selective DNA minor-groove binding agent.

(+)-CBI-CDPI1, an enhanced functional analog of CC-1065, is a DNA alkylating agent and an antibody-drug conjugate (ADCs) toxin.

DC1 is an ADC cytotoxin, similar to the small groove-binding DNA alkylating agent CC-1065. DC1 can be used to synthesize antibody-drug conjugates targeted to the treatment of cancer. DC1Sme is a DC1 derivative with IC50 values of Ramos, Namalwa, HL60 s