GGTI-297

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406421

CAS#: 181045-83-0

Description: GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).


Price and Availability

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GGTI-297 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406421
Name: GGTI-297
CAS#: 181045-83-0
Chemical Formula: C26H31N3O3S
Exact Mass: 465.20861
Molecular Weight: 465.60764
Elemental Analysis: C, 67.07; H, 6.71; N, 9.02; O, 10.31; S, 6.89


Synonym: GGTI297; GGTI-297; GGTI 297.

IUPAC/Chemical Name: (S)-2-(4-(((R)-2-amino-3-mercaptopropyl)amino)-2-(naphthalen-1-yl)benzamido)-4-methylpentanoic acid

InChi Key: PKMVDYSKPDHRLR-KOSHJBKYSA-N

InChi Code: InChI=1S/C26H31N3O3S/c1-16(2)12-24(26(31)32)29-25(30)22-11-10-19(28-14-18(27)15-33)13-23(22)21-9-5-7-17-6-3-4-8-20(17)21/h3-11,13,16,18,24,28,33H,12,14-15,27H2,1-2H3,(H,29,30)(H,31,32)/t18-,24+/m1/s1

SMILES Code: CC(C)C[C@H](NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O)C(O)=O


Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Patel CA, Rattan S. RhoA prenylation inhibitor produces relaxation of tonic smooth muscle of internal anal sphincter. J Pharmacol Exp Ther. 2007 May;321(2):501-8. Epub 2007 Feb 22. PubMed PMID: 17322025.

2: Lindholm MW, Nilsson J. Simvastatin stimulates macrophage interleukin-1beta secretion through an isoprenylation-dependent mechanism. Vascul Pharmacol. 2007 Feb;46(2):91-6. Epub 2006 Jul 25. PubMed PMID: 16942919.

3: Mraiche F, Cena J, Das D, Vollrath B. Effects of statins on vascular function of endothelin-1. Br J Pharmacol. 2005 Mar;144(5):715-26. PubMed PMID: 15678081; PubMed Central PMCID: PMC1576052.

4: Wickman G, Lan C, Vollrath B. Functional roles of the rho/rho kinase pathway and protein kinase C in the regulation of cerebrovascular constriction mediated by hemoglobin: relevance to subarachnoid hemorrhage and vasospasm. Circ Res. 2003 Apr 18;92(7):809-16. Epub 2003 Mar 13. PubMed PMID: 12637369.

5: Pollack IF, Bredel M, Erff M, Hamilton AD, Sebti SM. Inhibition of Ras and related guanosine triphosphate-dependent proteins as a therapeutic strategy for blocking malignant glioma growth: II--preclinical studies in a nude mouse model. Neurosurgery. 1999 Nov;45(5):1208-14; discussion 1214-5. PubMed PMID: 10549939.

6: Sun J, Blaskovich MA, Knowles D, Qian Y, Ohkanda J, Bailey RD, Hamilton AD, Sebti SM. Antitumor efficacy of a novel class of non-thiol-containing peptidomimetic inhibitors of farnesyltransferase and geranylgeranyltransferase I: combination therapy with the cytotoxic agents cisplatin, Taxol, and gemcitabine. Cancer Res. 1999 Oct 1;59(19):4919-26. PubMed PMID: 10519405.

7: Sun J, Qian Y, Hamilton AD, Sebti SM. Both farnesyltransferase and geranylgeranyltransferase I inhibitors are required for inhibition of oncogenic K-Ras prenylation but each alone is sufficient to suppress human tumor growth in nude mouse xenografts. Oncogene. 1998 Mar;16(11):1467-73. PubMed PMID: 9525745.

8: Vogt A, Qian Y, McGuire TF, Hamilton AD, Sebti SM. Protein geranylgeranylation, not farnesylation, is required for the G1 to S phase transition in mouse fibroblasts. Oncogene. 1996 Nov 7;13(9):1991-9. PubMed PMID: 8934546.