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 No. 1936529-65-5

Purity & Quality Control

YKL-05-099 Related Products

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy YKL-05-099 | YKL-05-099 supplier | purchase YKL-05-099 | YKL-05-099 cost | YKL-05-099 manufacturer | order YKL-05-099 | YKL-05-099 distributor