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YKL-05-099

YKL-05-099
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Purity:99.89%
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YKL-05-099

Catalog No. T17271Cas No. 1936529-65-5
YKL-05-099 is an inhibitor of the salt-inducible kinase(SIK1 and SIK3 ; IC50s: 10 and 30 nM, respectively). It has a slightly less potent SIK2-inhibitory (IC50:40 nM).
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Pack SizePriceAvailabilityQuantity
1 mg$68In Stock
5 mg$123In Stock
10 mg$189In Stock
25 mg$328In Stock
50 mg$488In Stock
100 mg$689In Stock
1 mL x 10 mM (in DMSO)$162In Stock
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Product Introduction

Bioactivity
Description
YKL-05-099 is an inhibitor of the salt-inducible kinase(SIK1 and SIK3 ; IC50s: 10 and 30 nM, respectively). It has a slightly less potent SIK2-inhibitory (IC50:40 nM).
In vitro
YKL-05-099 inhibits the production of the inflammatory cytokines TNFα, IL-6 and IL-12p40, and only modestly enhances IL-1β release in BMDCs stimulated with the yeast cell wall extract Zymosan A. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM) and IL-10-enhancing activities (EC50=460 nM). YKL-05-099 binds to SIK1 and SIK3 (IC50s: 10 and 30 nM, respectively, in a competitive binding assay). Preincubating bone marrow-derived macrophages with YKL-05-099 decreases LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259 [1].
In vivo
YKL-05-099 exhibits high solubility (PBS solubility=428 μM) and is predominantly in an unbound state in mouse plasma, displaying non-toxic characteristics at concentrations below 10 μM. This compound is metabolically stable, showing more than 2 hours of stability in mouse liver microsomes. Functionally, YKL-05-099 effectively modulates immune response by reducing TNFα levels in a dose-dependent manner, starting at 5 mg/Kg, and significantly enhancing IL-10 secretion at a 20 mg/Kg dose, achieving a more than two-fold increase. Furthermore, it inhibits phosphorylation of HDAC5 at the SIK-regulated site (Ser259) in a dose-responsive manner, with notable reduction starting at 5 mg/Kg and becoming undetectable by immunoblotting from the 20 mg/Kg dose onwards [1].
Chemical Properties
Molecular Weight600.11
FormulaC32H34ClN7O3
Cas No.1936529-65-5
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 45 mg/mL (74.99 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.6664 mL8.3318 mL16.6636 mL83.3181 mL
5 mM0.3333 mL1.6664 mL3.3327 mL16.6636 mL
10 mM0.1666 mL0.8332 mL1.6664 mL8.3318 mL
20 mM0.0833 mL0.4166 mL0.8332 mL4.1659 mL
50 mM0.0333 mL0.1666 mL0.3333 mL1.6664 mL

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