Home Immunology & Inflammation SIK inhibitor YKL-05-099

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YKL-05-099 SIK inhibitor

Cat.No.S9646

YKL-05-099 is an inhibitor of salt-inducible kinase (SIK) with IC50 of ~10 nM, ~40 nM and ~30 nM for SIK1, SIK2 and SIK3, respectively.
YKL-05-099 SIK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 600.11

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Quality Control

Batch: Purity: 99.88%
99.88

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (166.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 600.11 Formula

C32H34ClN7O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1936529-65-5 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C(=CC=C1)Cl)N2CC3=CN=C(N=C3N(C2=O)C4=NC=C(C=C4)OC)NC5=C(C=C(C=C5)C6CCN(CC6)C)OC

Mechanism of Action

Targets/IC50/Ki
SIK1
(Cell-free assay)
10 nM
SIK3
(Cell-free assay)
30 nM
SIK2
(Cell-free assay)
40 nM
In vitro

YKL-05-099 displays cell-based activities consistent with SIK inhibition. Pre-treatment with the indicated concentrations of this compound for 24 hr potentiates IL-10 production by Zymosan A-stimulated BMDCs.
In vivo

Well-tolerated doses of YKL-05-099 achieve free serum concentrations above its IC50 for SIK2 inhibition for > 16 hours and reduce phosphorylation of a known SIK substrate in vivo. While in vivo active doses of this compound recapitulate the effects of SIK inhibition on inflammatory cytokine responses, they do not induce metabolic abnormalities observed in Sik2 knockout mice. These results identify this chemical as a useful probe to investigate SIK function in vivo, and further support the development of SIK inhibitors for treatment of inflammatory disorders.
References

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