Molecular structure of GGTI-286, CAS Number: 171744-11-9
GGTI-286 (CAS 171744-11-9)
Alternate Names:
N-4-[2(R)-Amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(L)-leucine methyl ester
Application:
GGTI-286 is a potent, selective, cell-permeable inhibitor of GGTase I
CAS Number:
171744-11-9
Molecular Weight:
429.57
Molecular Formula:
C23H31N3O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
GGTI-286 is a potent, cell-permeable, and selective inhibitor of GGTase I. This methyl ester derivative of GGTI-287 is about 25-fold more potent than FTI-277 in inhibiting the processing of the geranylgeranylated protein Rap1A. GGTI-286 has also been shown to have a significant antiproliferative effect in human malignant glioma cells. It also selectively antagonizes oncogenic K-Ras4B.
GGTI-286 (CAS 171744-11-9) References
- Simvastatin inhibits TGFβ1-induced fibronectin in human airway fibroblasts. | Schaafsma, D., et al. 2011. Respir Res. 12: 113. PMID: 21864337
- Atorvastatin inhibits CXCR7 induction to reduce macrophage migration. | Ma, W., et al. 2014. Biochem Pharmacol. 89: 99-108. PMID: 24582769
- A zebrafish chemical suppressor screening identifies small molecule inhibitors of the Wnt/β-catenin pathway. | Nishiya, N., et al. 2014. Chem Biol. 21: 530-540. PMID: 24684907
- Simvastatin aggravates impaired autophagic flux in NSC34-hSOD1G93A cells through inhibition of geranylgeranyl pyrophosphate synthesis. | Qi, W., et al. 2019. Neuroscience. 409: 130-141. PMID: 31051215
- Nuclear β-catenin translocation plays a key role in osteoblast differentiation of giant cell tumor of bone. | Kimura, A., et al. 2022. Sci Rep. 12: 13438. PMID: 35927428
- Disruption of oncogenic K-Ras4B processing and signaling by a potent geranylgeranyltransferase I inhibitor. | Lerner, EC., et al. 1995. J Biol Chem. 270: 26770-3. PMID: 7592913
- Inhibition of the prenylation of K-Ras, but not H- or N-Ras, is highly resistant to CAAX peptidomimetics and requires both a farnesyltransferase and a geranylgeranyltransferase I inhibitor in human tumor cell lines. | Lerner, EC., et al. 1997. Oncogene. 15: 1283-8. PMID: 9315095
- Selective inhibition of type-I geranylgeranyltransferase in vitro and in whole cells by CAAL peptidomimetics. | Qian, Y., et al. 1998. Bioorg Med Chem. 6: 293-9. PMID: 9568283
- Inhibition of Ras and related G-proteins as a therapeutic strategy for blocking malignant glioma growth. | Bredel, M., et al. 1998. Neurosurgery. 43: 124-31; discussion 131-2. PMID: 9657198
Inhibitor of:
GGTase, GGTase-Iβ, and K-Ras.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GGTI-286, 250 µg | sc-221670 | 250 µg | $209.00 |