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GGTI-2418

Catalog No. T11396   CAS 501010-06-6

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.

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GGTI-2418 Chemical Structure
GGTI-2418, CAS 501010-06-6
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2 mg 5 days $ 94.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 125 mg/mL (283.11 mM), sonification is recommended.

TargetMolReferences and Literature

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 Ca

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Keywords

GGTI-2418 501010-06-6 Metabolism Transferase GGTI 2418 GGTI2418 inhibitor inhibit

 

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