501010-06-6
501010-06-6 structure
- Name: GGTI 2418
- Chemical Name: (2S)-2-[[(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxopiperazine-1-carbonyl]amino]-4-methylpentanoic acid
- CAS Number: 501010-06-6
- Molecular Formula: C23H31N5O4
- Molecular Weight: 441.52
- Catalog: Research Areas Cancer
- Create Date: 2016-12-11 08:24:00
- Modify Date: 2025-09-20 16:52:10
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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].
| Name | (2S)-2-[[(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxopiperazine-1-carbonyl]amino]-4-methylpentanoic acid |
|---|---|
| Synonyms |
unii-m67g28k74k
GGTI 2418 |
| 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]. |
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| Related Catalog | |
| 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]. Western Blot Analysis[2] Cell Line: HeLa cells Concentration: 10-15 μM Incubation Time: 16 hours Result: Delocalized FBXL2 and stabilized IP3R3. |
| 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[1]. GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice[1]. 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[1]. Animal Model: Nude mice implanted with MDA-MB-231 breast cancer tumors[1] 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[1] 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. |
| References |
| Molecular Formula | C23H31N5O4 |
|---|---|
| Molecular Weight | 441.52 |
| Exact Mass | 441.23800 |
| PSA | 122.12000 |
| LogP | 2.26270 |
| Storage condition | 2-8℃ |