Chemical Structure
FRAX486 HCL, Inhibitor | FRAX486, inhibitor
FRAX486 HCL (1232030-35-1 free base)
Purity
0.9982
Synonyms
FRAX486 HCL; FRAX486 HCL (1232030-35-1 free base); FRAX486; inhibitor
Purity/Purification
0.9982
Form/Format
Solid
Solubility
DMSO: 10.3mg/mL (20mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
SMILES
FC1=CC(NC2=NC=C3C(N(C(C(C4=CC=C(C=C4Cl)Cl)=C3)=O)CC)=N2)=CC=C1N5CCNCC5.[H]Cl
Formula
C25H24Cl3FN6O
Cell Research
Cells are grown in 96-well plates (20,000 cells/well) for 24 h, before FRAX486, IPA3, or DMSO are added in indicated concentrations (1, 5, 10 uM). Subsequently, cells are grown for different periods (24, 48, 72 h). Separate controls are performed for each period. At the end of this period, 10uL of [2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium monosodium salt (WST-8) from CCK-8 is added, and absorbance in each well is measured at 450 after incubation for 2 h at 37degree C.
In vitro
FRAX486 crosses the blood-brain barrier and that therapeutically useful concentrations of FRAX486 are in the brain as early as 1 h and remain as long as 24 h after administration, with the maximum concentration in the target tissue at 8 h. Daily dosing results in steady-state levels of FRAX486 in the brain. FRAX486 specifically rescues the Fmr1 KO abnormality in which the spine phenotype is present in apical neurons and not simply decreasing spine density irrespective of genotype or existence of a phenotype. Also, FRAX486 reduces hyperactivity and stereotypical movements, both of which are phenotypes that characterize the mouse model of Fragile X syndrome[3].
Preparation and Storage
Store at 0-4 degree C for short term (days to weeks), or -20 degree C for long term (months).
Chemical Structure
Chemical Structure
Related Product Information for FRAX486, inhibitor
FRAX486 HCL is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14,33,39 and 575 for PAK1,PAK2,PAK3 and PAK4 respectively.
Product Categories/Family for FRAX486, inhibitor
References
Hayashi-Takagi A, et al. Proc Natl Acad Sci U S A. 2014, 111(17):6461-6.
Wang Y, et al. PLoS One. 2016, 11(4):e20153312.
Dolan BM, et al. Proc Natl Acad Sci U S A. 2013, 110(14):5671-6.
Wang Y, et al. PLoS One. 2016, 11(4):e20153312.
Dolan BM, et al. Proc Natl Acad Sci U S A. 2013, 110(14):5671-6.
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Product Notes
The FRAX486 (Catalog #AAA5764911) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "FRAX486 HCL, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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