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YKL-05-099

Chemical Structure : YKL-05-099

CAS No.: 1936529-65-5

YKL-05-099 (YKL 05-099)

Catalog No.: PC-42327Not For Human Use, Lab Use Only.

YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively
YKL-05-099 displays increased SIK selectivity and enhanced pharmacokinetic properties compared with HG-9-91-01.
YKL-05-099 reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259, increases expression of the CREB target genes Il10 and Nurr77, suppresses production of TNFα, IL-6 and IL-12p40 in BMDMs.
YKL-05-099 is a useful probe to investigate SIK function in vivo.

Physicochemical Properties

M.Wt 600.11046
Formula C32H34ClN7O3
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

DMSO: ≥ 103.33 mg/mL; PBS: 100 mM

Chemical Name/SMILES

Pyrimido[4,5-d]pyrimidin-2(1H)-one, 3-(2-chloro-6-methylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-1-(5-methoxy-2-pyridinyl)-

References

1. Sundberg TB, et al. ACS Chem Biol. 2016 Aug 19;11(8):2105-11.

2. Wein MN, et al. Nat Commun. 2016 Oct 19;7:13176.

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