YKL-05-099

SKU: orb1307595

Description

YKL-05-099 is a potent and selective salt-inducible kinase (SIK) inhibitor, with IC50 values of 10 nM, 40 nM, and 30 nM for SIK1, SIK2, and SIK3, respectively. This tool compound is widely used in biochemical and cellular research to investigate SIK signaling pathways in inflammation, metabolism, and bone homeostasis.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1936529-65-5
• MW: 600.11
• Purity: 99.89% (May vary between batches)
• Formula: C₃₂H₃₄ClN₇O₃
• SMILES: COc1ccc(nc1)N1C(=O)N(Cc2cnc(Nc3ccc(cc3OC)C3CCN(C)CC3)nc12)c1c(C)cccc1Cl
• Target: SIK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.33 mM);DMSO:45 mg/mL (74.99 mM)

Bioactivity

• Target IC50:
  SIK1:10 nM|SIK3:30 nM|SIK2:40 nM
• 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.
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, SIK3, SIK2, SIK1, YKL05099, YKL-05-099, YKL 05 099, Salt-inducible Kinase (SIK)

Compound Identifiers

PubChem CID

121596782