Home Immunology & Inflammation SIK inhibitor YKL-05-099 For research use only.

YKL-05-099

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 Chemical Structure

YKL-05-099 Chemical Structure

CAS: 1936529-65-5

Selleck's YKL-05-099 has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.88%
99.88

YKL-05-099 Related Products

Choose Selective SIK Inhibitors

Biological Activity

Description 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.
Targets
SIK1 [1]
(Cell-free assay)		 SIK3 [1]
(Cell-free assay)		 SIK2 [1]
(Cell-free assay)
10 nM 30 nM 40 nM
In vitro
In vitro

YKL-05-099 displays cell-based activities consistent with SIK inhibition. Pre-treatment with the indicated concentrations of YKL-05-099 for 24 hr potentiates IL-10 production by Zymosan A-stimulated BMDCs.[1]
Cell Research Cell lines bone marrow-derived dendritic cells (BMDCs)
Concentrations 1 μM
Incubation Time 24 hr
Method

--
In Vivo
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 YKL-05-099 recapitulate the effects of SIK inhibition on inflammatory cytokine responses, they do not induce metabolic abnormalities observed in Sik2 knockout mice. These results identify YKL-05-099 as a useful probe to investigate SIK function in vivo, and further support the development of SIK inhibitors for treatment of inflammatory disorders.[1]
Animal Research Animal Models male 8–10 week-old C57BL/6 mice
Dosages 5 mg/kg-50 mg/kg
Administration IP

Chemical Information & Solubility

Molecular Weight 600.11 Formula

C32H34ClN7O3
CAS No. 1936529-65-5 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (166.63 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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