Name: O6-Benzylguanine
Price: 180.00 USD

- Overview
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    Background
    
    O6-Benzylguanine (BG) is a potent inhibitor of MGMT and an antineoplastic agent [1]. O6-methylguanine DNA methyltransferase (MGMT, also known as O6-Alkylguanine-DNA alkyltransferase, or AGT) is a DNA repair protein that removes the alkyl group located on the O6-position of guanine from DNA and restores DNA integrity. MGMT is alkylated and irreversibly inactivated. O6-Benzylguanine is a potent MGMT inhibitor. In HT29 cells, O6-Benzylguanine significantly reduced MGMT stability and the affinity of MGMT for DNA, increased its sensitivity to proteases. O6-Benzylguanine also increased the cytotoxic effect of alkylating agent BCNU [1]. In SF767 cells, BG (25 μM for 1 h) reduced >95% of MGMT activity, while 33% of the activity recovered within 24 h. When cells pretreated with BG (2.5 μM for 24 h) followed by the same low-dose treatment for 24 h completely depleted MGMT activity [2]. In HCT116 and HCT15 cells, treatment with BG and BCNU inactivated MGMT and arrested 70-80% of cells in G2/M phase in response to the DNA damages induced by BCNU [3]. In nude mice bearing SF767 human brain tumor xenografts, treatment with O6-Benzylguanine prior to BCNU significantly inhibited tumor growth as compared to BCNU alone [1]. In xenograft SF767 tumors, pre- and post-treatments (8 mg/kg over 24 h) combined with an i.p. bolus dose (80 mg/kg) of BG inhibited >95% of MGMT activity [2].
    
    [1]. Dolan ME, Pegg AE. O6-benzylguanine and its role in chemotherapy. Clin Cancer Res, 1997, 3(6): 837-847.
    [2]. Kreklau EL, Kurpad C, Williams DA, et al. Prolonged inhibition of O(6)-methylguanine DNA methyltransferase in human tumor cells by O(6)-benzylguanine in vitro and in vivo. J Pharmacol Exp Ther, 1999, 291(3): 1269-1275.
    [3]. Yan L, Donze JR, Liu L. Inactivated MGMT by O6-benzylguanine is associated with prolonged G2/M arrest in cancer cells treated with BCNU. Oncogene, 2005, 24(13): 2175-2183.
- Properties
  - Alternative Name
    
    6-(benzyloxy)-9H-purin-2-amine
    
    CAS Number
    
    19916-73-5
    
    Molecular Formula
    
    C12H11N5O
    
    Molecular Weight
    
    241.2
    
    Appearance
    
    A solid
    
    Purity
    
    99.65%
    
    Solubility
    
    insoluble in H2O; ≥11.3 mg/mL in EtOH with gentle warming; ≥56.2 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

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O6-Benzylguanine

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Background

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