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GGTI-2418
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GGTI-2418图片
CAS NO:501010-06-6
规格:98%
分子量:441.52
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
GGTI-2418是一种高效,竞争性和选择性的香叶基香叶基转移酶I(GGTaseI)抑制剂。GGTI-2418抑制GGTaseI和FTase活性,IC50分别为9.5nM和53μM。GGTI-2418还增强p27(Kip1)并诱导乳腺肿瘤显着消退。
CAS:501010-06-6
分子式:C23H31N5O4
分子量:441.52
纯度:98%
存储:Store at -20°C

Background:

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors[1]. IC50: 9.5 nM (GGTase I), 53 μM (FTase)[1]


GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase. GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM[1].GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3[2]. Western Blot Analysis[2] Cell Line: HeLa cells


GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of breast tumor xenografts in nude mice with MDA-MB-231 xenografts[1].GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice[1]. GGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo[1]. Animal Model: Nude mice implanted with MDA-MB-231 breast cancer tumors[1]


[1]. Kazi A, et al. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009 Apr;29(8):2254-63. [2]. Kuchay S, et al. PTEN counteracts FBXL2 to promote IP3R3- and Ca2+-mediated apoptosis limiting tumour growth. Nature. 2017 Jun 22;546(7659):554-558.