AdipoGen Life Sciences

Leucettinib-92

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AG-MR-C0049-M0011 mgCHF 130.00

AG-MR-C0049-M0055 mgCHF 430.00

AG-MR-C0049-M02525 mgCHF 1’290.00

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Product Details
Synonyms	LCTB-92; (Z)-2-((Adamantan-1-yl)amino)-5-(benzo[d]thiazol-6-ylmethylene)-3,5-dihydro-4H-imidazol-4-one
Product Type	Chemical
Properties
Formula	C₂₁H₂₂N₄OS
MW	378.5
CAS	2732859-57-1
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=1.2nM), DYRK1B (IC₅₀=1.8nM), DYRK3 (IC₅₀=19.3nM) and CLK2 (IC₅₀=0.6nM) [1].
Inhibits the phosphorylation of Tau at Thr212 and cyclin D1 at Thr286.
Corrects cognitive deficits in animal models of Down syndrome.
iso-Leucettinib-92 (Prod. No. AG-MR-C0050) is a kinase-inactive isomer and should be used as a negative control together with this compound.

Product References

Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases: M.F. Lindberg, et al.; J. Med. Chem. 66, 4106 (2023)
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)
DYRK1A inhibition restores pancreatic functions and improves glucose metabolism in a preclinical model of type 2 diabetes: R. Bertrand, et al.; Mol. Metab. 101, 102242 (2025)

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