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                同义名:
                    
                        
                            
                                GGTI 298 (trifluoroacetate salt); GGTI 298 TFA salt
                            
                        
                    
                
                
                
                    
                     
                    
                     
                
            
GGTI298 Trifluoroacetate是一种 geranylgeranyltransferase I 抑制剂,能够抑制 G1 期细胞周期并诱导凋亡。
 
                                 
                                
                            

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| 产品名称 | Transferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Tipifarnib | +++ FTase, IC50: 0.6 nM | 99%+ | |||||||||||||||||
| Tolcapone | + COMT, Ki: 30 nM | 99%+ | |||||||||||||||||
| Lonafarnib | +++ H-ras, IC50: 1.9 nM K-ras-4B, IC50: 2.8 nM | 99%+ | |||||||||||||||||
| (E)-Daporinad | ++++ NMPRTase, Ki: 0.4 nM | 99%+ | |||||||||||||||||
| FTI-277 HCl | ++++ FTase, IC50: 500 pM | 98% | |||||||||||||||||
| A 922500 | ++ human DGAT-1, IC50: 7 nM mouse DGAT-1, IC50: 24 nM | 98% | |||||||||||||||||
| Lomeguatrib | ++ O6-alkylguanine-DNA-alkyltransferas, IC50: 5 nM | 99%+ | |||||||||||||||||
| PF-04620110 | + DGAT1, IC50: 19 nM | 99% | |||||||||||||||||
| LB42708 | +++ FTase (K-Ras), IC50: 0.8 nM FTase (N-ras), IC50: 1.2 nM | 98% | |||||||||||||||||
| GGTI298 Trifluoroacetate | ✔ | 98%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 | 
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| 描述 | GGTI298 trifluoroacetate is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis. | 
| Concentration | Treated Time | Description | References | |
| T84WT cells | 1 μg/ml | 4 h | inhibited FSK-stimulated IK(ap) | J Biol Chem. 2013 Jul 12;288(28):20404-15. | 
| RAW264.7 cells | 10 μM | GGTI298 reversed the inhibition of osteoclast differentiation induced by compression by inhibiting the Rap1a/ERK signaling pathway, thereby accelerating tooth movement. | Int J Oral Sci. 2024 Feb 4;16(1):12. | |
| RAW264.7 cells | 2.5 µM | 2, 4, and 6 days | To evaluate the effect of GGTI298 on autophagic vesicle formation, it was found that GGTI298 significantly reduced the number of autophagic vesicles | Autophagy. 2019 Dec;15(12):2063-2075. | 
| Administration | Dosage | Frequency | Description | References | ||
| C57/BL6 mice | Orthodontic tooth movement model | Local injection | 50 μg/mL | Every 2 days for 7 days | GGTI298 increased osteoclast activity by inhibiting the Rap1a/ERK signaling pathway, thereby accelerating tooth movement. | Int J Oral Sci. 2024 Feb 4;16(1):12. | 
| Mouse | Ileal loop model | Ileal loop injection | 100 μM | Single dose, 6 hours duration | Reduced CT-induced fluid accumulation | J Biol Chem. 2013 Jul 12;288(28):20404-15. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 1.68mL 0.34mL 0.17mL | 8.42mL 1.68mL 0.84mL | 16.84mL 3.37mL 1.68mL | |
| CAS号 | 1217457-86-7 | 
| 分子式 | C29H34F3N3O5S | 
| 分子量 | 593.66 | 
| SMILES Code | CC(C)C[C@H](NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O)C(OC)=O.O=C(O)C(F)(F)F | 
| MDL No. | MFCD06409252 | 
| 别名 | GGTI 298 (trifluoroacetate salt); GGTI 298 TFA salt | 
| 运输 | 蓝冰 | 
| InChI Key | WALKWJPZELDSKT-UFABNHQSSA-N | 
| Pubchem ID | 16078971 | 
| 存储条件 | In solvent -20°C:3-6个月-80°C:12个月 | 
| 溶解方案 | DMSO: 105 mg/mL(176.87 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 
 
 
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