Leucettinib-92

Cat. No.: HY-155723: FAQs
Data Sheet Handling Instructions

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Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC₅₀s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3).

For research use only. We do not sell to patients.

Leucettinib-92 Chemical Structure

CAS No. : 2732859-57-1

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DYRK1 DYRK2 DYRK3 DYRK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-22	IC₅₀	6.3 μM Compound: 22	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]

In Vitro

Leucettinib-92 (0.1-10 μM; 3 min) binds to DYRK1A in SH-SY5Y cells and induces it to stabilize until melting temperature above 52°C. Leucettinib-92 (1 μM) inhibits phosphorylation of two DYRK1A substrates (Thr212-Tau and Thr286-cyclin D1)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

378.49

Formula

C₂₁H₂₂N₄OS

CAS No.

2732859-57-1

SMILES

O=C(N1)/C(N=C1NC2(C3)C[C@H]4C[C@@H]3C[C@@H](C2)C4)=C/C5=CC=C(N=CS6)C6=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Deau E, et al. Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B. J Med Chem. 2023 Aug 10;66(15):10694-10714. [Content Brief]

Leucettinib-92 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Leucettinib-922732859-57-1Leucettinib92Leucettinib 92CDKDYRKCyclin dependent kinaseDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseInhibitorinhibitorinhibit

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