PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. MM2 is the binding site of RMI complex on Fanconi anemia complementation group M protein (FANCM). PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics.

QBS10072S is a novel dual-function, BBB permeable chemotherapeutic agent with alkylating moiety and a selective large neutral amino acid transporter 1 (LAT1, SLC7A5) substrate, shows excellent BBB penetration and promising efficacy in vitro (U251 cell IC5

Treosulfan (NSC 39069, Treosulphan) is an alkylating agent used for conventional and high-dose chemotherapy regimens. Treosulfan is potently cytotoxic against pancreatic cancer cell lines.

NSC373981 (NSC 373981) is a CARD11 G-quadruplex (G4) stabilizing small molecule that downregulates CARD11 gene expression in DLBCL cells.

CDEAH is a monofunctional alkylating agent that selectively kills PARP1- and xeroderma pigmentosum A-deficient cells.

OBI-3424 S-isomer (TH-3424, OBI 3424) is a highly potent DNA alkylating prodrug that is converted by AKR1C3 to a potent DNA-alkylating agent.

Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.

Cisplatin is an inorganic platinum agent (cis-diamminedichloroplatinum) with antineoplastic activity.

AST-3424 (OBI-3424, TH-3424) is a first-in-class, novel prodrug that selectively targets cancers overexpressing the enzyme AKR1C3, OBI-3424 is a highly selective prodrug that is converted by AKR1C3 to a DNA alkylating agent.

Sibiromycin is a naturally produced glycosylated pyrrolobenzodiazepines (PBDs). Sibiromycin is also a potent antitumor antibiotic that binds covalently to DNA in the minor groove at the NH2 of guanine.

Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities.

SG2057 (DRG16) is a PBD dimer containing a pentyldioxy linkage which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts. SG2057 is a highly active antitumor agent.

TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM, demonstrates 270-fold enhanced cytotoxicity under hypoxia versus their potency under aerobic conditions, stable to cytochrome P450 metabolism.

Oxaliplatin is a second generation potent platinum-based anti-neoplastic agent that is believed to form inter- and intrastrand DNA adducts which activate signaling pathways culminating in apoptosis. The development of Oxaliplatin was inspired from the eff

N,N’N’-triethylenethiophosphoramide (ThioTEPA) is a cancer chemotherapeutic member of the alkylating agent group.

Mitomycin C is a DNA crosslinking agent that inhibits DNA synthesis and induces apoptosis in a variety of cells.

Methazolastone (Temozolomide, Temodar, Temodal) is a DNA damage inducer.

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

Carboplatin is a chemotherapy drug by binding to DNA and interfering with the cell's repair mechanism.

Bisantrene is a highly effective antitumor drug, targets eukaryotic type II topoisomerases.

Ranimustine (MCNU) is a nitrosourea alkylating agent, can be used for research of chronic myelogenous leukemia and polycythemia vera.

Prednimustine (Leo 1031;NSC 134087) is the ester formed from Prednisolone and Chlorambucil. Prednimustine can be used for leukemias and lymphomas research.

LP-284 is a potent DNA alkylating agent that kills solid tumours. LP-284 can be used in the studies of hematologic cancers with compromised DNA repair, such as mantle cell lymphoma (MCL).

Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide, with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response.

Phosphoramide mustard is the major metabolite for Cyclophosphamide, with anticancer activitiy. Phosphoramide mustard induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response.

Phenylacetic acid mustard is the major metabolite of the cancer chemotherapeutic agent Chlorambucil. Chlorambucil is an alkylating agent with antitumor activity.

Duocarmycin analog-2 is a potent DNA alkylating agent. Duocarmycin analog-2 can be used of synthetic immunoconjugate. Duocarmycin analog-2 has antitumor activity.

Methyl methanesulfonate (MMS), a DNA alkylating agent, modifies both guanine (to 7-methylguanine) and adenine (to 3-methlyladenine) to cause base mispairing and replication blocks, respectively.

Melphalan(Sarcolysin; L-PAM) is a chemotherapy drug belonging to the class of nitrogen mustard alkylating agents; attaches the alkyl group to the guanine base of DNA.

EC2629 is a highly potent folate receptor (FR)-targeted DNA crosslinking agent. EC2629 can be used for the research of FR-positive tumors, including those that are classified as drug resistant.