alkylation

N-Ethylmaleimide (NEM) is a reagent for alkylation of free sulfhydryl groups, a cysteine protease inhibitor used in experimental biochemistry. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor that specifically inhibits phosphate transport in mitochondria.

Procarbazine hydrochloride (NSC-77213 HCl) is the hydrochloride salt of a methylhydrazine derivative with antineoplastic and mutagenic activities. Although the exact mode of cytotoxicity has not been elucidated, procarbazine, after metabolic activation, appears to inhibit the trans-methylation of methionine into transfer RNA (t-RNA), thereby preventing protein synthesis and consequently DNA and RNA synthesis. This agent may also undergo auto-oxidation, resulting in the formation of cytotoxic free radicals which damage DNA through an alkylation reaction.

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.

Menadione (Vitamin K3) is a synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo.

4-Octyl Itaconate, a cell-permeable derivative of Itaconate, is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 and inhibits phosphorylation of STING.

BIO-013077-01 is a potent TGFbeta family type I receptors antagonist.

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

Busulfan-d8 is a deuterated compound of Busulfan. Busulfan has a CAS number of 55-98-1. Busulfan 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.

Masticadienolic acid is a specific competitive inhibitor of secreted phospholipase A2, it not only protects the active site histidine from alkylation but also inhibits the action of secreted from pancreas, synovial fluid, and bee venom. Masticadienolic ac

1-Methyladenine is a DNA alkylation product that undergoes damage reversal through oxidative demethylation for repair purposes.

Antiproliferative Agent-38 (COM 18), a tetracyclic compound, features a reactive ring nitrogen (likely the quinoline moiety) that resists N-alkylation. Despite its classification, it neither exhibits anti-malarial properties nor inhibits cancer cell proliferation [1].

JH295 is a highly potent and selective inhibitor of NIMA-related kinase 2 (Nek2), exhibiting irreversible inhibition activity with an IC 50 value of 770 nM. This compound effectively inhibits cellular Nek2 using the alkylation of Cys22. Importantly, JH295 does not exhibit any inhibitory effects toward Cdk1, Aurora B, or Plk1, which are kinases involved in mitotic processes. Furthermore, JH295 has no impact on bipolar spindle assembly or the spindle assembly checkpoint mechanism.

DM-CHOC-PEN is a DNA alkylation agent that may be used to treat brain cancer.

Vitamin K3-d3 is a deuterated compound of Vitamin K3. Vitamin K3 has a CAS number of 58-27-5. Menadione is a synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo.

RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting cancer cell proliferation and inducing p53-dependent apoptosis. Furthermore, RUNX-IN-2 suppresses tumor development in PANC-1 xenograft mice and demonstrates notable alkylation efficiency and specificity [1].

JH295 hydrate is a potent, irreversible, and selective NIMA-related kinase 2 (Nek2) inhibitor that inhibits cellular Nek2 by Cys22 alkylation (IC50 = 770 nM). JH295 hydrate is not active against the mitotic kinases Cdk1, Aurora B, or Plk1, and does not interfere with bipolar spindle assembly or the spindle assembly checkpoint [1].

Duocarmycin SA is an extremely potent cytotoxic agent and antitumor antibiotic that induces sequence-selective alkylation of duplex DNA, with an IC50 of 10 pM. It demonstrates synergistic cytotoxicity against glioblastoma multiforme (GBM) cells when combined with proton radiation in vitro.

DC41SMe is a DC1 derivative that is cytotoxic to Ramos, Namalwa and HL60 / s with IC50s ranging from 18-25 pM. DC1 is a simplified analogue of CC-1065, an antibody conjugate of cytotoxic DNA alkylation molecules, used for targeted treatment of cancer.

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