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Product Infomation
Product Name

GGTI-2418

CAS No.501010-06-6
Molecular Weight441.52                                                                                    
FormulaC₂₃H₃₁N₅O₄
SMILESCC(C)C[C@@H](C(O)=O)NC(N1[C@@H](CC2=CC=CC=C2)C(N(CC3=C(C)N=CN3)CC1)=O)=O
Stock statusInstock




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Product description:




DescriptionGGTI-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 & Target

IC50: 9.5 nM (GGTase I), 53 μM (FTase)[1]

In VitroGGTI-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].



Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month







Peferences:


[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.