GGTI-2418

Research use only, not for human use.

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.

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.

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.GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3.Western Blot Analysis Cell Line:HeLa cells Concentration:10-15 μM Incubation Time:16 hours Result:Delocalized FBXL2 and stabilized IP3R3.

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.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.Animal Model:Nude mice implanted with MDA-MB-231 breast cancer tumors Dosage:100 mg/kg daily or 200 mg/kg every third day Administration:Injected intraperitoneally; 15 days Result:Inhibited the growth of breast tumor xenografts.Animal Model:ErbB2 transgenic mice Dosage:100 mg/kg/day Administration:Subcutaneously; 5 days Result:Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.

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Metabolic Enzyme/Protease

Transferase

Transferase

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501010-06-6

441.52

C23H31N5O4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (283.11 mM; Ultrasonic )

CC(C)C[C@H](NC(=O)N1CCN(Cc2nc[nH]c2C)C(=O)[C@@H]1Cc1ccccc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years