GGTI2417

For research use only. Not for therapeutic Use.

  • CAT Number: I028022
  • CAS Number: 501010-05-5
  • Molecular Formula: C24H33N5O4
  • Molecular Weight: 455.559
  • Purity: 98%
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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.


Catalog Number I028022
CAS Number 501010-05-5
Synonyms

GGTI2417; GGTI-2417; GGTI2417.

Molecular Formula C24H33N5O4
Purity 98%
Solubility Soluble in DMSO
Appearance Solid powder
Storage Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
IUPAC Name L-Leucine, N-[[(2S)-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxo-2-(phenylmethyl)-1-piperazinyl]carbonyl]-, methyl ester
InChI 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
InChIKey DWKYALWDWAYMTB-FPOVZHCZSA-N
SMILES 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
Reference

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.

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