For research use only
Product Infomation | |
Product Name | GGTI-2418 |
---|---|
CAS No. | 501010-06-6 |
Molecular Weight | 441.52
|
Formula | C₂₃H₃₁N₅O₄ |
SMILES | CC(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 status | Instock |
Product description:
Description | 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 & Target | IC50: 9.5 nM (GGTase I), 53 μM (FTase)[1] | |
In Vitro | 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]. | |
Powder | -20°C | 3 years |
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 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.