SML3813

YKL-05-099

≥98% (HPLC)

• Synonym(s): 3-(2-Chloro-6-methylphenyl)-7-((2-methoxy-4-(1-methylpiperidin-4-yl)phenyl)amino)-1-(5-methoxypyridin-2-yl)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one, YKL-05-99
• Empirical Formula (Hill Notation): C₃₂H₃₄ClN₇O₃
• CAS Number: 1936529-65-5
• Molecular Weight: 600.11
• MDL number: MFCD31382123
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: , Faint yellow to yellow-brown
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CC1=CC=CC(Cl)=C1N2C(N(C3=CC=C(OC)C=N3)C4=NC(NC5=C(OC)C=C(C6CCN(C)CC6)C=C5)=NC=C4C2)=O

Description

Biochem/physiol Actions

Potent and selective salt-inducible kinases (SIK1, SIK2, SIK3) inhibitor in vitro and in vivo.



YKL-05-099 is a potent and selective salt-inducible kinases inhibitor (SIK1/2/3 IC50 = 10/40/30 nM) with superior pharmacokinetic properties than HG-9-91-01. YKL-05-099 pre-treatment of murine BDMCs up-regulates Zymosan A-stimulated IL-10 (EC50 = 460 nM with 24h ), while suppresses inflammatory cytokines production (TNFα, IL-6 and IL-12p40). Likewise, YKL-05-099 intraperitoneal administration in mice (20 mg/kg i.p.) 15 min prior to LPS (0.5 mg/kg i.p.) enhances serum IL-10, while reduces HDAC5 pSer259 levels in total splenic leukocytes and serum TNFα level in vivo.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable