[CAS NO. 1936529-65-5] YKL-05-099
PRODUCTS SPECIFICATIONS [1936529-65-5]
DESCRIPTION [1936529-65-5]
Overview
| MDL | MFCD31382123 |
|---|---|
| Molecular Weight | 600.11 |
| Molecular Formula | C32H34ClN7O3 |
| SMILES | O=C1N(C2=NC=C(OC)C=C2)C3=NC(NC4=CC=C(C5CCN(C)CC5)C=C4OC)=NC=C3CN1C6=C(C)C=CC=C6Cl |
3 Publications Citing Use of MCE
Summary
YKL-05-099 is a salt-inducible kinase ( SIK ) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC 50 s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC 50 =40 nM) [1] .
IC50 & Target
IC50: 10 nM (SIK1), 30 nM (SIK3), 40 nM (SIK2) [1]
In Vitro
YKL-05-099 has slightly less potent SIK2-inhibitory (IC 50 =40 nM) and IL-10-enhancing activities (EC 50 =460 nM). YKL-05-099 binds to SIK1 and SIK3 with IC 50 s of 10 and 30 nM, respectively, in a competitive binding assay. Preincubating bone marrow-derived macrophages with YKL-05-099 reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259. YKL-05-099 suppresses 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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
YKL-05-099 is non-toxic at concentrations less than 10 μM and stable in mouse liver microsomes for more than 2 hours. YKL-05-099 is highly soluble (PBS solubility=428 μM) and present in an unbound state at appreciable levels in mouse plasma. YKL-05-099 dose dependently decreases phosphorylation of HDAC5 at the SIK-regulated site Ser259; reduced phosphorylation is observed at the lowest dose (5 mg/Kg) and is below the limit of detection by immunoblotting beginning at the 20 mg/Kg dose. YKL-05-099 dose-dependently reduces abundance of TNFα in serum beginning at 5 mg/Kg, and increases IL-10 levels at the 20 mg/Kg dose by more than 2-fold [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 75 mg/mL ( 124.98 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6664 mL | 8.3318 mL | 16.6636 mL |
| 5 mM | 0.3333 mL | 1.6664 mL | 3.3327 mL |
| 10 mM | 0.1666 mL | 0.8332 mL | 1.6664 mL |