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YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. It can inhibit the activity of SIK1 (IC50: 10 nM) and SIK3 (IC50: 30 nM), and has a slightly weaker inhibitory effect on SIK2 (IC50: 40 nM). [1]

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $68 | In Stock | In Stock | |
| 5 mg | $123 | - | In Stock | |
| 10 mg | $189 | - | In Stock | |
| 25 mg | $328 | - | In Stock | |
| 50 mg | $488 | - | In Stock | |
| 100 mg | $689 | Inquiry | Inquiry | |
| 1 mL x 10 mM (in DMSO) | $162 | - | In Stock |
| Description | YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. It can inhibit the activity of SIK1 (IC50: 10 nM) and SIK3 (IC50: 30 nM), and has a slightly weaker inhibitory effect on SIK2 (IC50: 40 nM). [1] |
| Targets&IC50 | SIK1:10 nM, SIK2:40 nM, SIK3:30 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 | METHODS: YKL-05-099 (6, 18 mg/kg/d) was tested in surgically ovariectomized mice by intraperitoneal injection to see if it could increase cancellous bone mass in hypogonadal female mice. RESULTS YKL-05-099 treatment increased trabecular bone mass in the femur and L5 vertebrae of hypogonadal female mice, indicating that the agent does not cause significant defects in cortical bone mass. [1] |
| Molecular Weight | 600.11 |
| Formula | C32H34ClN7O3 |
| Cas No. | 1936529-65-5 |
| Smiles | COc1ccc(nc1)N1C(=O)N(Cc2cnc(Nc3ccc(cc3OC)C3CCN(C)CC3)nc12)c1c(C)cccc1Cl |
| Relative Density. | 1.311 g/cm3 (Predicted) |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (74.99 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.33 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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