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MedKoo CAT#: 407805
Description: GGTI2417 is a potent and selective Geranylgeranyltransferase I inhibitor that targets RalB to inhibit anchorage-dependent growth and induce apoptosis and RalA to inhibit anchorage-independent growth. By expressing farnesylated, GGTI-resistant RalA and RalB in Cos7 cells and human pancreatic MiaPaCa2 cancer cells followed by GGTI-2417 treatment, it was demonstrated that farnesylated RalB, but not RalA, confers resistance to the proapoptotic and anti-anchorage-dependent growth effects of GGTI-2417.
MedKoo Cat#: 407805
Chemical Formula: C24H33N5O4
Exact Mass: 455.2533
Molecular Weight: 455.559
Elemental Analysis: C, 63.28; H, 7.30; N, 15.37; O, 14.05
Related CAS #: 501010-05-5 501010-06-6
Synonym: GGTI2417; GGTI-2417; GGTI2417.
IUPAC/Chemical Name: L-Leucine, N-[[(2S)-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxo-2-(phenylmethyl)-1-piperazinyl]carbonyl]-, methyl ester
InChi Key: DWKYALWDWAYMTB-FPOVZHCZSA-N
InChi Code: InChI=1S/C24H33N5O4/c1-16(2)12-19(23(31)33-4)27-24(32)29-11-10-28(14-20-17(3)25-15-26-20)22(30)21(29)13-18-8-6-5-7-9-18/h5-9,15-16,19,21H,10-14H2,1-4H3,(H,25,26)(H,27,32)/t19-,21-/m0/s1
SMILES Code: CC(C)C[C@@H](C(OC)=O)NC(N1[C@@H](CC2=CC=CC=C2)C(N(CC3=C(C)NC=N3)CC1)=O)=O
Geranylgeranyltransferase I inhibitors (GGTIs) are presently undergoing advanced preclinical studies and have been shown to disrupt oncogenic and tumor survival pathways, to inhibit anchorage-dependent and -independent growth, and to induce apoptosis.
1: Kazi A, Carie A, Blaskovich MA, Bucher C, Thai V, Moulder S, Peng H, Carrico
D, Pusateri E, Pledger WJ, Berndt N, Hamilton A, Sebti SM. 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. doi: 10.1128/MCB.01029-08. Epub 2009 Feb 9.
PubMed PMID: 19204084; PubMed Central PMCID: PMC2663293.
2: Falsetti SC, Wang DA, Peng H, Carrico D, Cox AD, Der CJ, Hamilton AD, Sebti
SM. Geranylgeranyltransferase I inhibitors target RalB to inhibit
anchorage-dependent growth and induce apoptosis and RalA to inhibit
anchorage-independent growth. Mol Cell Biol. 2007 Nov;27(22):8003-14. Epub 2007
Sep 17. PubMed PMID: 17875936; PubMed Central PMCID: PMC2169159.