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AdipoGen Life Sciences
Leucettinib-21
100
CHF
CHF 100.00
In stock
AG-MR-C0047-M0011 mgCHF 100.00
AG-MR-C0047-M0055 mgCHF 330.00
AG-MR-C0047-M02525 mgCHF 980.00
| Product Details | |
|---|---|
| Synonyms | LCTB-21; (R,Z)-5-(Benzo[d]thiazol-6-ylmethylene)-2-((1-methoxy-4-methylpentan-2-yl)amino)-3,5-dihydro-4H-imidazol-4-one |
| Product Type | Chemical |
| Properties | |
| Formula |
C18H22N4O2S |
| MW | 358.5 |
| CAS | 2732859-75-3 |
| Purity Chemicals | ≥99% (NMR) |
| Appearance | Pale yellow to off-white powder. |
| Solubility | Soluble in DMSO (10mM) or ethanol. |
| Reconstitution | Stock solutions can be made up to 10mM in DMSO. |
| Identity | Determined by 1H-NMR. |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice |
Keep cool and dry. Protect from light and moisture. |
| Use/Stability |
Stable for at least 2 years after receipt when stored at -20°C. Store solutions at -20°C in the dark. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Potent inhibitor of DYRK1A (IC50=2.4nM), DYRK1B (IC50=6.7nM), CLK1 (IC50=11.8nM) and CLK4 (IC50=5nM) kinases [2].
- Inhibits the phosphorylation of Tau at Thr212 and cyclin D1 at Thr286, native DYRK1A in HT-22 cells and triggers cell apoptotic cell death.
- Corrects cognitive deficits in Ts65Dn model of Down syndrome and other models.
- iso-Leucettinib-21 (Prod. No. AG-MR-C0048) is a kinase-inactive isomer and should be used as a negative control together with this compound.
Product References
- Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B: E. Deau, et al.; J. Med. Chem. 66, 10694 (2023)
- Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer’s Disease Drug Candidate: M.F. Lindberg, et al.; J. Med. Chem. 66, 15648 (2023)
- Leucettinib-21, a DYRK1A kinase inhibitor as a clinical drug candidate for Alzheimer’s disease and Down syndrome. In Therapeutic Trials in Alzheimer's Disease: Where Are We Now?: L. Meijer, et al.; J. Alzheim. Dis. (in press) (2024)
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