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QL-1200186

Chemical Structure : QL-1200186

CAS No.:

QL-1200186 (QL1200186)

Catalog No.: PC-21281Not For Human Use, Lab Use Only.

QL-1200186 is a potent, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 0.06 nM, targets pseudokinase regulatory domain (Janus homology 2, JH2) of the TYK2 protein.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

QL-1200186 is a potent, highly selective allosteric inhibitor of tyrosine kinase 2 (TYK2) with IC50 of 0.06 nM, targets pseudokinase regulatory domain (Janus homology 2, JH2) of the TYK2 protein.
QL-1200186 displays weak acitvity against JAK1 JH2 domain (IC50=9.85 nM, >160-fold), does not show inhibitory activity against TYK2 JAK1/2/3 JH1 kinases.
QL-1200186 shows dose-dependent inhibition of the JAK/STAT/ISGF3 pathway and IFNα-stimulated pSTAT5 levels in CD3+ T cells.
QL-1200186 inhibits the IL-23-induced pSTAT3 level in human Th17 cells in a dose-dependent manner.
QL-1200186 reduces IL-12/IL-18-driven IFNγ release, improves imiquimod-induced psoriasis-like skin inflammation in mice.

Physicochemical Properties

M.Wt
Formula
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

References

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