S84033 |
GGTI-298 |
源叶(MedMol) | 96% |
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- 产品描述: GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
- 靶点: IC50: 3 μM (Rap1A, in vivo), > 20 μM (Ha-Ras, in vivo);Others
- 体内研究:
The vivo mouse ileal loop experiments show fluid accumulation is reduced in a dose-dependent manner by TRAM-34, GGTI298, or H1152 when injected together with cholera toxin into the loop
- 参考文献:
1. Sheikh IA, et al. The Epac1 signaling pathway regulates Cl- secretion via modulation of apical KCNN4c channels in diarrhea. J Biol Chem. 2013 Jul 12;288(28):20404-15 2. Chen S, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis. Mol Cancer. 2010 Jan 29;9:23. 3. McGuire TF, et al. Platelet-derived growth factor receptor tyrosine phosphorylation requires protein geranylgeranylation but not farnesylation. J Biol Chem. 1996 Nov 1;271(44):27402-7.
- 溶解性: Soluble in DMSO
- 保存条件: RT
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.684 ml 8.422 ml 16.845 ml 5 mM 0.337 ml 1.684 ml 3.369 ml 10 mM 0.168 ml 0.842 ml 1.684 ml 50 mM 0.034 ml 0.168 ml 0.337 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)