Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), showing 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.
Pack Size | Availability | Price/USD | Quantity |
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2 mg | 5 days | $ 94.00 |
Description | GGTI-2418 is a highly potent, competitive, and selective inhibitor of geranylgeranyltransferase I (GGTase I), showing 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 | GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM.?GGTi-2418 (10-15 μM;?16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.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. |
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 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo.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. |
Molecular Weight | 441.52 |
Formula | C23H31N5O4 |
CAS No. | 501010-06-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (283.11 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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GGTI-2418 501010-06-6 Metabolism Transferase GGTI 2418 GGTI2418 inhibitor inhibit