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Submit ReviewLomeguatrib
说明： MGMT inhibitor
别名： PaTrin-2
化学名： 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine
纯度： ≥98% (HPLC)
生物活性 for Lomeguatrib
Lomeguatrib (LomG) is a potent inhibitor of O6-methylguanine-DNA methyltransferase (MGMT); (IC50 = 0.009 μM in cell-free extracts from HeLa S3 cells); LomG attenuates MGMT activity in vitro and in vivo. LomG enhances the antitumor activity of temozolomide (Cat. No. 2706) in both human melanoma and MCF-7 xenografts. LomG acts as a pseudosubstrate for MGMT and can be used to induce rapid ubiquitin proteasome pathway degradation of proteins that have a MGMT fusion.
技术数据 for Lomeguatrib
| 分子量 | 326.17 |
| 公式 | C10H8BrN5OS |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 192441-08-0 |
| PubChem ID | 3025944 |
| InChI Key | JUJPKFNFCWJBCX-UHFFFAOYSA-N |
| Smiles | NC1=NC(OCC3=CC(Br)=CS3)=C2C(N=CN2)=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Lomeguatrib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 32.62 | 100 |
制备储备液 for Lomeguatrib
以下数据基于产品分子量 326.17。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.07 mL | 15.33 mL | 30.66 mL |
| 5 mM | 0.61 mL | 3.07 mL | 6.13 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.07 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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产品说明书 for Lomeguatrib
参考文献 for Lomeguatrib
参考文献是支持产品生物活性的出版物。
Reinhard et al (2001) Monosaccharide-linked inhibitors of O6-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J.Med.Chem. 44 4050 PMID: 11708909
Barvaux et al (2004) Sensitization of a human ovarian cancer cell line to temozol. by simultaneous attenuation of the Bcl-2 antiapoptotic protein and DNA repair by O6-alkylguanine-DNA alkyltransferase. Mol.Cancer Ther. 3 1215 PMID: 15486188
Clemons et al (2005) O6-(4-bromothenyl)guanine reverses temozol. resistance in human breast tumor MCF-7 cells and xenografts. Br.J.Cancer 93 1152 PMID: 16278661
Murawska et al (2022) Repurposing the damage repair protein methyl guanine methyl transferase as a ligand inducible fusion degron. ACS Chem.Biol. 17 24 PMID: 34982531
If you know of a relevant reference for Lomeguatrib, please let us know.
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关键词: Lomeguatrib, Lomeguatrib supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, inhibits, psuedosubstrates, epigenetics, PaTrin-2, DNA, Methyltransferases, 4359, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Epigenetics in Cancer Research Product Guide
This product guide reviews some of the main areas in cancer epigenetics research and lists around 120 products that can be used for the main epigenetic targets including:
- Histone Methylation
- Histone Acetylation
- DNA Methylation
- Ubiquitination
- Bromodomains
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.