Catalog Number
ACM1139889932
Description
Golgicide A is a Potent, selective and reversible inhibitor of GBF1 ArfGEF. Golgicide A inhibited HSV-1 entry via beta-galactosidase reporter assay and impaired incoming virus transport to the nuclear periphery. Inhibition of GBF1 via golgicide A can result in rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network
IUPAC Name
(3aR,9bS)-6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
Molecular Formula
C17H14F2N2
Canonical SMILES
FC4=CC([C@]3([H])[C@]([H])2CC=C3)=C(C(F)=C4)NC2C1=CN=CC=C1
InChI
InChI=1S/C17H14F2N2/c18-11-7-14-12-4-1-5-13(12)16(10-3-2-6-20-9-10)21-17(14)15(19)8-11/h1-4,6-9,12-13,16,21H,5H2/t12-,13+,16?/m0/s1
InChI Key
NJZHEQOUHLZCOX-FTLRAWMYSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 71.82; H, 4.96; F, 13.36; N, 9.85
HS Tariff Code
2934.99.9001
In Vitro Activity
The effect of GCA on toxin trafficking and on intracellular organelle morphology was examined. Immunofluoresence experiments demonstrated dramatic effects of GCA on the Golgi and TGN. Whereas the Golgi remains as a tightly organized perinuclear ribbon in untreated cells, GCA caused complete dispersal of the medial-Golgi markers giantin and the cis-Golgi marker GM130. Treatment with GCA resulted in a diffuse and punctate distribution of the medial-Golgi marker giantin. The punctate structures were in contact with Sec31-positive foci, indicative of their association with ER exit sites. GCA also caused the TGN to disperse into small vesicles that subsequently disseminated throughout the cell.
Reference: Nat Chem Biol. 2009 Mar;5(3):157-65. https://pubmed.ncbi.nlm.nih.gov/19182783/
Shipping
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.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).
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