DNA Alkylation

Streptozocin (NSC-85998) is an antibiotic that induces DNA methylation. Streptozocin is toxic to insulin-producing pancreatic islet B-cells and is commonly used in the construction of animal models of type 1 diabetes. The product is unstable in solution and is recommended to be dispensed now.

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

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

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.

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.

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

GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors.

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

Busulfan (Busulphan) is a synthetic derivative of dimethane-sulfonate with antineoplastic and cytotoxic properties. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription.

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

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

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

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).

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).

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.

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

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.

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

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

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.

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

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.

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.

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.

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

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