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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G648049-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $140.90 | |
G648049-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $230.90 | |
G648049-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $450.90 | |
G648049-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $770.90 | |
G648049-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,350.90 |
Synonyms | GGTI-2418|501010-06-6|CHEMBL3218390|GGTI 2418|PTX-100|M67G28K74K|501010-06-6 (free acid)|(2S)-2-[[(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxopiperazine-1-carbonyl]amino]-4-methylpentanoic acid|(S)-2-((S)-2-benzyl-4-((4-methyl-1H-imidazol-5-y |
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Specifications & Purity | ≥98% |
Biochemical and Physiological Mechanisms | GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I ( GGTase I ) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC 50 s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces si |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I ( GGTase I ) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC 50 s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors In Vitro GGTI-2418 inhibits GGTase I and FTase activities with IC 50 s 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 K i of 4.4±1.6 nM. GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:IC50: 9.5 nM (GGTase I), 53 μM (FTase) |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | (2S)-2-[[(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxopiperazine-1-carbonyl]amino]-4-methylpentanoic acid |
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INCHI | InChI=1S/C23H31N5O4/c1-15(2)11-18(22(30)31)26-23(32)28-10-9-27(13-19-16(3)24-14-25-19)21(29)20(28)12-17-7-5-4-6-8-17/h4-8,14-15,18,20H,9-13H2,1-3H3,(H,24,25)(H,26,32)(H,30,31)/t18-,20-/m0/s1 |
InChi Key | COLCNDRDBCLVOC-ICSRJNTNSA-N |
Canonical SMILES | CC1=C(N=CN1)CN2CCN(C(C2=O)CC3=CC=CC=C3)C(=O)NC(CC(C)C)C(=O)O |
Isomeric SMILES | CC1=C(N=CN1)CN2CCN([C@H](C2=O)CC3=CC=CC=C3)C(=O)N[C@@H](CC(C)C)C(=O)O |
PubChem CID | 11539477 |
Molecular Weight | 441.5 |
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Solubility | DMSO : 125 mg/mL (283.11 mM; Need ultrasonic) |
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