CCG-63808Reversible RGS inhibitor CAS# 620113-73-7 |
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| 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. |
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| 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. |
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| 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. | ||
| Description | CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins. References: | |||||
CCG-63808 Dilution Calculator
CCG-63808 Molarity Calculator
| 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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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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CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
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