ProINDY - CAS 719277-30-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C14H15NO3S
Molecular Weight:
277.34
COA:
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Targets:
Others
Description:
ProINDY, the prodrug form of INDY, is a cell permeable ATP-competitive DYRK1A/B inhibitor.
Purity:
≥98% by HPLC
Synonyms:
TG007; TG-007; TG 007; (1Z)-1-(5-Acetyloxy3-ethyl-2(3H)-benzothiazolylidene)-2-propanone
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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InChIKey:
RLEOCVDWLAYGRX-UHFFFAOYSA-N
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-
Canonical SMILES:
CCN1C2=C(C=CC(=C2)OC(=O)C)SC1=CC(=O)C
1.Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A.
Ogawa Y;Nonaka Y;Goto T;Ohnishi E;Hiramatsu T;Kii I;Yoshida M;Ikura T;Onogi H;Shibuya H;Hosoya T;Ito N;Hagiwara M Nat Commun. 2010 Oct 5;1:86. doi: 10.1038/ncomms1090.
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 μM, 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.
2.A chemical with proven clinical safety rescues Down-syndrome-related phenotypes in through DYRK1A inhibition.
Kim H;Lee KS;Kim AK;Choi M;Choi K;Kang M;Chi SW;Lee MS;Lee JS;Lee SY;Song WJ;Yu K;Cho S Dis Model Mech. 2016 Aug 1;9(8):839-48. doi: 10.1242/dmm.025668. Epub 2016 Jul 7.
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.
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CAS 719277-30-2 ProINDY

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