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Submit ReviewGGTI 298
说明： Geranylgeranyltransferase I (GGTase I) inhibitor
化学名： N-[4-[2(R)-Amino-3-mercaptopropyl]amino-2-(1-naphthalenyl)benzoyl]-L-leucine methyl ester trifluoroacetate salt
纯度： ≥95% (HPLC)
生物活性 for GGTI 298
GGTI 298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor. Strongly inhibits the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras (IC50 values are 3 and > 10 μM respectively). Causes G0-G1 cell cycle block and apoptosis in A549 cells and inhibits cell invasion and migration in COLO 320CM cells.
技术数据 for GGTI 298
| 分子量 | 593.66 |
| 公式 | C27H33N3O3S.CF3CO2H |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 1217457-86-7 |
| PubChem ID | 16078971 |
| InChI Key | WALKWJPZELDSKT-UFABNHQSSA-N |
| Smiles | SC[C@H](N)CNC1=CC=C(C(N[C@H]([C@@](OC)=O)CC(C)C)=O)C(C2=CC=CC3=C2C=CC=C3)=C1.FC(F)(C(O)=O)F |
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 GGTI 298
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 14.84 | 25 |
制备储备液 for GGTI 298
以下数据基于产品分子量 593.66。 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 |
|---|---|---|---|
| 0.25 mM | 6.74 mL | 33.69 mL | 67.38 mL |
| 1.25 mM | 1.35 mL | 6.74 mL | 13.48 mL |
| 2.5 mM | 0.67 mL | 3.37 mL | 6.74 mL |
| 12.5 mM | 0.13 mL | 0.67 mL | 1.35 mL |
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产品说明书 for GGTI 298
参考文献 for GGTI 298
参考文献是支持产品生物活性的出版物。
McGuire et al (1996) Platelet-derived growth factor receptor tyrosine kinase phosphorylation requires protein geranylgeranylation but not farnesylation. J.Biol.Chem. 271 27402 PMID: 8910319
Miquel et al (1997) GGTI-298 induces G0-G1 block and apoptosis whereas FTI-227 causes G2-M enrichment in A549 cells. Cancer Res. 57 1846 PMID: 9157972
Porcu et al (2010) A yeast-based genomic strategy highlights the cell protein networks altered by FTase inhibitor peptidomimetics. Mol.Cancer 9 197 PMID: 20653956
Kusama et al (2003) Selective inhibition of cancer cell invasion by a geranylgeranyltransferase inhibitor. Clin.Exp.Meta. 20 561
If you know of a relevant reference for GGTI 298, please let us know.
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关键词: GGTI 298, GGTI 298 supplier, GGTI298, geranylgeranyltransferase, GGTase1, Protein, Prenyltransferases, Post-translational, Modifications, 2430, Tocris Bioscience
2 篇 GGTI 298 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GGTI 298 的部分引用包括：
Luttman et al (2021) ABL allosteric inhibitors synergize with statins to enhance apoptosis of metastatic lung cancer cells. ABL allosteric inhibitors synergize with statins to 37 109880 PMID: 34706244
Domingue et al (2016) Chenodeoxycholic Acid Requires Activation of EGFR, EPAC and Ca2+ to Stimulate CFTR-dependent Cl-Secretion in Human Colonic T84 Cells. American Journal of Physiology - Cell Physiology PMID: 27558159
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GGTI 298 的评论
平均评分: 5 (Based on 1 Review.)
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Geranylgeranyltransferase I (GGTase I) inhibitor.
By
Anonymous on 03/26/2018
分析类型： In Vitro
种属： Rat
Geranylgeranyltransferase I (GGTase I) inhibitor
