O6-Benzylguanine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
O6-Benzylguanine(BG)是一种强效的MGMT抑制剂和抗肿瘤剂[1].
O6甲基鸟嘌呤DNA甲基转移酶(MGMT,也称为O6-烷基鸟嘌呤-DNA烷基转移酶,或AGT)是一种DNA修复蛋白,消除位于DNA鸟嘌呤O6位点上的烷基并恢复DNA完整性.MGMT被烷基化并不可逆地灭活.
O6-Benzylguanine是一种强效的MGMT抑制剂.在HT29细胞中,O6-Benzylguanine显著降低MGMT的稳定性和MGMT对DNA的亲和力,增加其对蛋白酶的敏感性. O6-Benzylguanine也增加烷化剂BCNU的细胞毒性作用[1].在SF767细胞中,BG(25 μM,作用1小时)降低超过95％的MGMT活性,而33％的活性在24小时内恢复.当用BG预处理(2.5 μM,作用24小时)的细胞随后用相同的低剂量治疗24小时,MGMT活性完全去除[2].在HCT116和HCT15细胞中,BG和BCNU处理灭活MGMT,并将70-80％的细胞阻滞在G2/M期,以响应BCNU 诱导的DNA损伤[3].
在带有SF767人脑肿瘤异种移植的裸鼠中,与单独使用BCNU相比,BCNU之前用O6-Benzylguanine处理显著抑制肿瘤生长[1].在异种移植SF767肿瘤中,前处理和后处理(8 mg/kg,作用24小时以上)与静脉内大剂量(80 mg/kg)BG联合用药抑制超过95％的MGMT活性[2].
参考文献：
[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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 241.2 |
| Cas No. | 19916-73-5 |
| Formula | C12H11N5O |
| Solubility | insoluble in H2O; ≥11.3 mg/mL in EtOH with gentle warming; ≥56.2 mg/mL in DMSO |
| Chemical Name | 6-(benzyloxy)-9H-purin-2-amine |
| SDF | Download SDF |
| Canonical SMILES | [H]N1C2=NC(N)=NC(OCC3=CC=CC=C3)=C2N=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
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质量控制和MSDS
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化学结构
