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CCG-63808

Reversible RGS inhibitor CAS# 620113-73-7

CCG-63808

Catalog No. BCC1461----Order now to get a substantial discount!

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CCG-63808: 5mg $81 In Stock
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  • CCG-63802

    Catalog No.:BCC1460
    CAS No.:620112-78-9

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Chemical structure

CCG-63808

3D structure

Chemical Properties of CCG-63808

Cas No. 620113-73-7 SDF Download SDF
PubChem ID 5948316 Appearance Powder
Formula C25H15FN4O2S M.Wt 454.49
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 1 mg/mL (2.20 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name (E)-2-(1,3-benzothiazol-2-yl)-3-[2-(4-fluorophenoxy)-9-methyl-4-oxopyrido[1,2-a]pyrimidin-3-yl]prop-2-enenitrile
SMILES CC1=CC=CN2C1=NC(=C(C2=O)C=C(C#N)C3=NC4=CC=CC=C4S3)OC5=CC=C(C=C5)F
Standard InChIKey IPZHFKHGSYRBNT-DTQAZKPQSA-N
Standard InChI InChI=1S/C25H15FN4O2S/c1-15-5-4-12-30-22(15)29-23(32-18-10-8-17(26)9-11-18)19(25(30)31)13-16(14-27)24-28-20-6-2-3-7-21(20)33-24/h2-13H,1H3/b16-13+
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CCG-63808

DescriptionCCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.

References:
[1]. Levi L. Blazer et al.Reversible, Allosteric Small-Molecule Inhibitors of Regulator of G Protein Signaling Proteins. Molecular Pharmacology September 2010 vol.78 no.3 524-533

CCG-63808 Dilution Calculator

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CCG-63808 Molarity Calculator

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Preparing Stock Solutions of CCG-63808

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2003 mL 11.0013 mL 22.0027 mL 44.0054 mL 55.0067 mL
5 mM 0.4401 mL 2.2003 mL 4.4005 mL 8.8011 mL 11.0013 mL
10 mM 0.22 mL 1.1001 mL 2.2003 mL 4.4005 mL 5.5007 mL
50 mM 0.044 mL 0.22 mL 0.4401 mL 0.8801 mL 1.1001 mL
100 mM 0.022 mL 0.11 mL 0.22 mL 0.4401 mL 0.5501 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on CCG-63808

CCG-63808 is a selective inhibitor of RGS4 with IC50 value of 1.4 μM [1].
RGS (regulators of G protein signaling) are multi-functional, GTPase-accelerating proteins and plays an important role in promoting GTP hydrolysis via heterotrimeric G proteins α subunit. RGS 4 is also known as RGP4 and plays a pivotal role in negatively regulating signaling upstream or at the level of the heterotrimeric G protein [2].
CCG-63808 is a potent RGS4 inhibitor and is different from the reported RGS4 irreversibly inhibitor CCG-4986. Using the [32P] GTP single-turnover GAP assay, it was shown that CCG-63808 treatment inhibited GAP activity of RGS4 and the inhibition could be reversed by washing [1].
References:
[1].Blazer, L.L., et al., Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol, 2010. 78(3): p. 524-33.
[2].Dobrivojevic, M., et al., Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol, 2012. 303(12): p. C1260-8.

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Description

CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.

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