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
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About This Item
Empirical Formula (Hill Notation):
C32H34ClN7O3
CAS Number:
Molecular Weight:
600.11
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
Quality Level
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
InChI key
VQINULODWGEVBB-UHFFFAOYSA-N
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.
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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