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AdipoGen Life Sciences
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CHF 95.00
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AG-CR1-3665-M0055 mgCHF 95.00
Specifications / Handling
| Product Details | |
|---|---|
| Synonyms | (1Z)-1-(3-Ethyl-5-hydroxy-2(3H)-benzothiazolylidene)-2-propanone |
| Product Type | Chemical |
| Properties | |
| Formula |
C12H13NO2S |
| MW | 235.3 |
| CAS | 1169755-45-6 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | White to off-white solid. |
| Solubility | Soluble in DMSO (10mg/ml). |
| Identity | Determined by 1H-NMR. |
| InChi Key | GCSZJMUFYOAHFY-SDQBBNPISA-N |
| Smiles | OC1=CC=C(S/C(N2CC)=C\C(C)=O)C2=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Keep cool and dry. |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| Safety Data Sheet |
Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Scientific Background Information
Product Description
- Potent and selective ATP-competitive DYRK1A and DYRK1B inhibitor (IC50=240nM and 230nM respectively). Binds at the ATP-binding cleft of the enzyme.
- Inhibits also DYRK2, DYRK3, CLK1, CLK4, casein kinase 1 (CSNK1D) and PIM1 (>90% inhibition at the same concentration).
- Reverses aberrant tau-phosphorylation and rescues repressed calcineurin/NFAT signaling.
- Impairs the self-renewal capacity of neural stem cells and glioblastoma tumor-initiating cells.
- Shown to induce regeneration and expansion of rat and adult human β-cells in vivo or ex vivo.
Product-specific References
- Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A: Y. Ogawa, et al.; Nat. Commun. 1, 86 (2010)
- Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastoma growth: N. Pozo, et al.; J. Clin. Invest. 123, 2475 (2013)
- A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication: P. Wang, et al.; Nat. Med. 21, 383 (2015)
- Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases: M.F. Lindberg, et al.; J. Med. Chem. ahead of print (2023)
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