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GGTI-2418

GGTI-2418
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GGTI-2418

Catalog No. T11396Cas No. 501010-06-6
GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors.
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Pack SizePriceAvailabilityQuantity
1 mg$485 days
5 mg$1137-10 days
10 mg$1897-10 days
25 mg$3727-10 days
50 mg$5627-10 days
100 mg$7907-10 days
500 mg$1,6707-10 days
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Product Introduction

Bioactivity
Description
GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), exhibiting inhibitory activities with IC50 values of 9.5 nM for GGTase I and 53 μM for FTase, respectively. Additionally, it enhances p27(Kip1) expression and induces significant regression of breast tumors.
Targets&IC50
GGTase I:9.5 nM, FTase:53 μM
In vitro
In HeLa cells, GGTI-2418 (10-15 μM; 16 hours) can delocalize FBXL2 and stabilize IP3R3[2].
In vivo
GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice. GGTI-2418 inhibits the geranylgeranylation of Rap1, significantly reduces Akt S473 phosphorylation, and upregulates p27 levels in vivo. Additionally, GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of MDA-MB-231 breast tumor xenografts in nude mice.
AliasGGTI2418, GGT 2418
Chemical Properties
Molecular Weight441.52
FormulaC23H31N5O4
Cas No.501010-06-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (226.49 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2649 mL11.3245 mL22.6490 mL113.2452 mL
5 mM0.4530 mL2.2649 mL4.5298 mL22.6490 mL
10 mM0.2265 mL1.1325 mL2.2649 mL11.3245 mL
20 mM0.1132 mL0.5662 mL1.1325 mL5.6623 mL
50 mM0.0453 mL0.2265 mL0.4530 mL2.2649 mL
100 mM0.0226 mL0.1132 mL0.2265 mL1.1325 mL

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