DNA Alkylation

Streptozotocin (Streptozocin, NSC-85998) is an antibiotic that enters pancreatic β-cells via the glucose transporter (GLUT2) and induces DNA methylation, leading to β-cell apoptosis. It is toxic to insulin-producing cells and commonly used to establish diabetic animal models. This product is unstable in solution and is recommended to be prepared freshly before use.

Duocarmycin TM is a DNA alkylator. Duocarmycin TM is an exceptionally potent antitumor antibiotic.

IACS-52825 is a selective and potent dual leucine zipper kinase (DLK) inhibitor that reverses para-mechanical aberrant pain in a CIPN mouse model for the study of neurological disorders.

Lomeguatrib (PaTrin-2), a modified guanine base, inhibits the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) .

Phosphoramide mustard is a toxic metabolite of cyclophosphamide with anticancer activity and ovarian toxicity that induces DNA damage.

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.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

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

Treosulfan (NSC 39069) is a bifunctional alkylating agent used in the treatment of advanced ovarian cancer.[2]

Thio-TEPA (Tiofosyl) is a polyfunctional, organophosphorus alkylating agent with antineoplastic activity.

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.

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

VAL-083 is an alkylating agent with antitumor activity that produces N7 methylation on DNA.

O6-Benzylguanine is a guanine analog with antineoplastic activity,and is a potent O6-alkylguanine DNA alkyltransferase (AGT) inactivator.

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.

Chlorambucil (CB-1348) is an orally-active antineoplastic aromatic nitrogen mustard. Chlorambucil alkylates and cross-links DNA during all phases of the cell cycle, resulting in disruption of DNA function, cell cycle arrest, and apoptosis.

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

Methyl methanesulfonate is a DNA alkylator that modifies adenine (3-methyladenine) and guanine (7-methyladenine) respectively, resulting in base mismatch and replication disorders.

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

Palifosfamide (Isophosphamide mustard) lysine (ZIO-201) is a stable form of palifosfamide. Palifosfamide lysine has broad activity in sarcoma lines in vitro. The IC50 ranges from 2.25 to 6.75 μM for most cell lines except OS222 (IC50=31.5 μM).

DN-1289 is an orally available, blood-brain barrier-crossing, selective and potent inhibitor with an IC50 value of 17 nM for di-leucine zipper kinase (DLK) and 40 nM for leucine zipper-bearing kinase (LZK).DN-1289 significantly inhibited optic nerve crush (ONC)-induced p-c-Jun in a mouse model.

Lobaplatin (D-19466) (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin (D-19466) is a third-generation platinum anti-neoplastic agent which shows activity for a variety of tumour types and is a promising antitumour chemotherapeutic agent[1][2]. It is a platinum complex with DNA alkylating activity.

CB1954(Tretazicar (NSC-115829)), an anticancer prodrug, is activated by NAD(P)H quinone oxidoreductase 2. It is converted in the presence of the enzyme NQO2 and co-substrate caricotamide ( EP-0152R) (EP) into a potent cytotoxic bifunctional alkylating agent.

Methyl methanesulfonate (Standard) is a reference standard for research and analysis in studies involving Methyl methanesulfonate. Methyl methanesulfonate is a DNA alkylating agent that modifies adenine (to 3-methyladenine) and guanine (to 7-methylguanine), inducing base mismatches and replication errors.