Additional information:
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.|Product information|CAS Number: 501010-06-6|Molecular Weight: 441.52|Formula: C23H31N5O4|Chemical Name: (2S)-2-{[(2S)-2-benzyl-4-[(5-methyl-1H-imidazol-4-yl)methyl]-3-oxopiperazine-1-carbonyl]amino}-4-methylpentanoic acid|Smiles: CC1NC=NC=1CN1CCN([C@@H](CC2C=CC=CC=2)C1=O)C(=O)N[C@@H](CC(C)C)C(O)=O|InChiKey: COLCNDRDBCLVOC-ICSRJNTNSA-N|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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 125 mg/mL (283.11 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.{{Lebrikizumab} site|{Lebrikizumab} Interleukin Related|{Lebrikizumab} Biological Activity|{Lebrikizumab} Purity|{Lebrikizumab} supplier|{Lebrikizumab} Epigenetics} 5±2.{{Adapalene} site|{Adapalene} Apoptosis|{Adapalene} Technical Information|{Adapalene} Formula|{Adapalene} manufacturer|{Adapalene} Epigenetics} 0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase.PMID:24423657 GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM. GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes 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.|Products are for research use only. Not for human use.|