ProINDYCAS# 719277-30-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 719277-30-2 | SDF | Download SDF |
PubChem ID | 44633738 | Appearance | Powder |
Formula | C14H15NO3S | M.Wt | 277.34 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 100 mM in DMSO | ||
Chemical Name | [(2Z)-3-ethyl-2-(2-oxopropylidene)-1,3-benzothiazol-5-yl] acetate | ||
SMILES | CCN1C2=C(C=CC(=C2)OC(=O)C)SC1=CC(=O)C | ||
Standard InChIKey | RLEOCVDWLAYGRX-AUWJEWJLSA-N | ||
Standard InChI | InChI=1S/C14H15NO3S/c1-4-15-12-8-11(18-10(3)17)5-6-13(12)19-14(15)7-9(2)16/h5-8H,4H2,1-3H3/b14-7- | ||
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 | DYRK1A/B inhibitor; prodrug form of INDY. Cell permeable. Inhibits phosphorylation of tau protein and rescues repressed calcineurin/NFAT signaling. Recovers Xenopus embryos from head malformation induced by DYRK1A overexpression in vivo. |
ProINDY Dilution Calculator
ProINDY Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 3.6057 mL | 18.0284 mL | 36.0568 mL | 72.1137 mL | 90.1421 mL |
5 mM | 0.7211 mL | 3.6057 mL | 7.2114 mL | 14.4227 mL | 18.0284 mL |
10 mM | 0.3606 mL | 1.8028 mL | 3.6057 mL | 7.2114 mL | 9.0142 mL |
50 mM | 0.0721 mL | 0.3606 mL | 0.7211 mL | 1.4423 mL | 1.8028 mL |
100 mM | 0.0361 mL | 0.1803 mL | 0.3606 mL | 0.7211 mL | 0.9014 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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A chemical with proven clinical safety rescues Down-syndrome-related phenotypes in through DYRK1A inhibition.[Pubmed:27483355]
Dis Model Mech. 2016 Aug 1;9(8):839-48.
DYRK1A is important in neuronal development and function, and its excessive activity is considered a significant pathogenic factor in Down syndrome and Alzheimer's disease. Thus, inhibition of DYRK1A has been suggested to be a new strategy to modify the disease. Very few compounds, however, have been reported to act as inhibitors, and their potential clinical uses require further evaluation. Here, we newly identify CX-4945, the safety of which has been already proven in the clinical setting, as a potent inhibitor of DYRK1A that acts in an ATP-competitive manner. The inhibitory potency of CX-4945 on DYRK1A (IC50=6.8 nM) in vitro was higher than that of harmine, INDY or ProINDY, which are well-known potent inhibitors of DYRK1A. CX-4945 effectively reverses the aberrant phosphorylation of Tau, amyloid precursor protein (APP) and presenilin 1 (PS1) in mammalian cells. To our surprise, feeding with CX-4945 significantly restored the neurological and phenotypic defects induced by the overexpression of minibrain, an ortholog of human DYRK1A, in the Drosophila model. Moreover, oral administration of CX-4945 acutely suppressed Tau hyperphosphorylation in the hippocampus of DYRK1A-overexpressing mice. Our research results demonstrate that CX-4945 is a potent DYRK1A inhibitor and also suggest that it has therapeutic potential for DYRK1A-associated diseases.
Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A.[Pubmed:20981014]
Nat Commun. 2010 Oct 5;1:86.
Dyrk1A (dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A) is a serine/threonine kinase essential for brain development and function, and its excessive activity is considered a pathogenic factor in Down syndrome. The development of potent, selective inhibitors of Dyrk1A would help to elucidate the molecular mechanisms of normal and diseased brains, and may provide a new lead compound for molecular-targeted drug discovery. Here, we report a novel Dyrk1A inhibitor, INDY, a benzothiazole derivative showing a potent ATP-competitive inhibitory effect with IC(50) and K(i) values of 0.24 and 0.18 muM, respectively. X-ray crystallography of the Dyrk1A/INDY complex revealed the binding of INDY in the ATP pocket of the enzyme. INDY effectively reversed the aberrant tau-phosphorylation and rescued the repressed NFAT (nuclear factor of activated T cell) signalling induced by Dyrk1A overexpression. Importantly, ProINDY, a prodrug of INDY, effectively recovered Xenopus embryos from head malformation induced by Dyrk1A overexpression, resulting in normally developed embryos and demonstrating the utility of ProINDY in vivo.