GGTI 2147 | CAS#191102-87-1 | prenylation inhibior

MedKoo Cat#: 597451 | Name: GGTI 2147

Description:

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

GGTI 2147 is an inhibitors of protein geranylgeranyltransferase-I and protein prenylation. Increases prelamin A accumulation by inhibiting ZMPSTE24 protein in human fibroblast and increases cytosolic accumulation of Rac1 and elicites significant inhibition of GSIS from INS 832/13 cells.

Chemical Structure

GGTI 2147

CAS#191102-87-1

Theoretical Analysis

MedKoo Cat#: 597451

Name: GGTI 2147

CAS#: 191102-87-1

Chemical Formula: C28H30N4O3

Exact Mass: 470.2318

Molecular Weight: 470.57

Elemental Analysis: C, 71.47; H, 6.43; N, 11.91; O, 10.20

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

GGTI 2147; GGTI-2147; GGTI2147; Geranylgeranyl transferase inhibitor-2147;

IUPAC/Chemical Name

methyl (4-(((1H-imidazol-4-yl)methyl)amino)-2-(naphthalen-1-yl)benzoyl)-L-leucinate

InChi Key

TUQRZGWNDBXSNP-SANMLTNESA-N

InChi Code

InChI=1S/C28H30N4O3/c1-18(2)13-26(28(34)35-3)32-27(33)24-12-11-20(30-16-21-15-29-17-31-21)14-25(24)23-10-6-8-19-7-4-5-9-22(19)23/h4-12,14-15,17-18,26,30H,13,16H2,1-3H3,(H,29,31)(H,32,33)/t26-/m0/s1

SMILES Code

CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NCC2=CNC=N2)C=C1C3=C4C=CC=CC4=CC=C3)=O

Appearance

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

Shelf Life

>3 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).

HS Tariff Code

2934.99.03.00

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 470.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Yuan M, Gao S, Sun C, Chen L, Shi Q, Hu J, Yu R, Zhou X. Inhibiting geranylgeranyltransferase I activity decreases spine density in central nervous system. Hippocampus. 2015 Mar;25(3):373-84. doi: 10.1002/hipo.22379. Epub 2014 Nov 25. PubMed PMID: 25330763. 2: Appels NM, Bolijn MJ, van Eijndhoven MA, Stephens TC, Beijnen JH, Schellens JH. Characterization of the in vitro activity of AZD3409, a novel prenyl transferase inhibitor. Cancer Chemother Pharmacol. 2011 Jan;67(1):137-45. doi: 10.1007/s00280-010-1300-6. Epub 2010 Mar 13. PubMed PMID: 20229082. 3: Subasinghe W, Syed I, Kowluru A. Phagocyte-like NADPH oxidase promotes cytokine-induced mitochondrial dysfunction in pancreatic β-cells: evidence for regulation by Rac1. Am J Physiol Regul Integr Comp Physiol. 2011 Jan;300(1):R12-20. doi: 10.1152/ajpregu.00421.2010. Epub 2010 Oct 13. PubMed PMID: 20943855; PubMed Central PMCID: PMC3023281. 4: Okamoto S, Jiang Y, Kawamura K, Shingyoji M, Tada Y, Sekine I, Takiguchi Y, Tatsumi K, Kobayashi H, Shimada H, Hiroshima K, Tagawa M. Zoledronic acid induces apoptosis and S-phase arrest in mesothelioma through inhibiting Rab family proteins and topoisomerase II actions. Cell Death Dis. 2014 Nov 13;5:e1517. doi: 10.1038/cddis.2014.475. PubMed PMID: 25393473; PubMed Central PMCID: PMC4260733. 5: Amin RH, Chen HQ, Veluthakal R, Silver RB, Li J, Li G, Kowluru A. Mastoparan-induced insulin secretion from insulin-secreting betaTC3 and INS-1 cells: evidence for its regulation by Rho subfamily of G proteins. Endocrinology. 2003 Oct;144(10):4508-18. Epub 2003 Jun 19. PubMed PMID: 12960065. 6: Veluthakal R, Kaur H, Goalstone M, Kowluru A. Dominant-negative alpha-subunit of farnesyl- and geranyltransferase inhibits glucose-stimulated, but not KCl-stimulated, insulin secretion in INS 832/13 cells. Diabetes. 2007 Jan;56(1):204-10. PubMed PMID: 17192483. 7: Rung E, Friberg PA, Bergh C, Billig H. Depletion of substrates for protein prenylation increases apoptosis in human periovulatory granulosa cells. Mol Reprod Dev. 2006 Oct;73(10):1277-83. PubMed PMID: 16868926. 8: Amin R, Chen HQ, Tannous M, Gibbs R, Kowluru A. Inhibition of glucose- and calcium-induced insulin secretion from betaTC3 cells by novel inhibitors of protein isoprenylation. J Pharmacol Exp Ther. 2002 Oct;303(1):82-8. PubMed PMID: 12235236. 9: Kowluru A, Chen HQ, Tannous M. Novel roles for the rho subfamily of GTP-binding proteins in succinate-induced insulin secretion from betaTC3 cells: further evidence in support of the succinate mechanism of insulin release. Endocr Res. 2003 Aug;29(3):363-76. PubMed PMID: 14535637.