dnaalkylation

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.

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.

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.

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.

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.

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

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

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

DLK-IN-1 is a selective oral active inhibitor of bisleucine zipper kinase (DLK, MAP3K12) with Ki of 3 nM. DLK-IN-1 is active in the Alzheimer's disease model, retains excellent CNS permeability, and after multiple days of administration, its concentration

GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).

Seco-Duocarmycin SA is a highly potent DNA alkylator used as an ADC cytotoxin.

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.

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

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

Duocarmycin Analog is used as an DNA alkylator and ADC cytotoxin. Duocarmycin Analog is an analog of Duocarmycin.

Miriplatin hydrate (SM-11355 (hydrate)) (MPT) is a novel platinum complex used in TACE that shows promise for the treatment of hepatocellular carcinoma (HCC). Miriplatin hydrate is a lipophilic platinum complex that can be easily suspended in Lipiodol and gradually releases active platinum compounds in tumor tissue.

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.

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).

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).

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.

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.