| Name | YKL-05-099 |
| 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] |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 45 mg/mL (74.99 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.33 mM), Sonication is recommended.
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| Keywords | YKL-05-099 | YKL05099 | YKL 05 099 | SIK3 | SIK2 | SIK1 | Salt-inducible Kinase (SIK) | Inhibitor | inhibit |
| Inhibitors Related | RSS0680 | YKL-06-061 | MRT 67307 dihydrochloride | Pterosin B | GLPG3970 | ARN-3236 | WH-4-025 | PF-07899895 | Phanginin A | GLPG3312 | YKL-06-062 | HG-9-91-01 |
| Related Compound Libraries | Glycolysis Compound Library | Reprogramming Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Kinase Inhibitor Library | Anti-Obesity Compound Library | Hematonosis Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
