YKL-05-099

Modify Date: 2024-01-18 14:34:03

YKL-05-099 Structure
YKL-05-099 structure
Common Name YKL-05-099
CAS Number 1936529-65-5 Molecular Weight 600.110
Density 1.3±0.1 g/cm3 Boiling Point 761.0±70.0 °C at 760 mmHg
Molecular Formula C32H34ClN7O3 Melting Point N/A
MSDS N/A Flash Point 414.1±35.7 °C

 Use of YKL-05-099


YKL-05-099 is a salt-inducible kinase (SIK) probe; inhibits SIK2 with an IC50 of 40 nM.

 Names

Name YKL-05-099
Synonym More Synonyms

 YKL-05-099 Biological Activity

Description YKL-05-099 is a salt-inducible kinase (SIK) probe; inhibits SIK2 with an IC50 of 40 nM.
Related Catalog
Target

IC50: 40 nM (SIK2)[1]

In Vitro 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 with IC50s of 10 and 30 nM, respectively, in a competitive binding assay. Preincubating bone marrow-derived macrophages with YKL-05-099 reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259. YKL-05-099 suppresses 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[1].
In Vivo YKL-05-099 is non-toxic at concentrations less than 10 μM and stable in mouse liver microsomes for more than 2 hours. YKL-05-099 is highly soluble (PBS solubility=428 μM) and present in an unbound state at appreciable levels in mouse plasma. YKL-05-099 dose dependently decreases phosphorylation of HDAC5 at the SIK-regulated site Ser259; reduced phosphorylation is observed at the lowest dose (5 mg/Kg) and is below the limit of detection by immunoblotting beginning at the 20 mg/Kg dose. YKL-05-099 dose-dependently reduces abundance of TNFα in serum beginning at 5 mg/Kg, and increases IL-10 levels at the 20 mg/Kg dose by more than 2-fold[1].
Animal Admin Mice: YKL-05-099 is diluted in 5% N-methyl-2-pyrrolidinone, 5% Solutol HS15 and 90% normal saline and administered IP to male 8–10 week-old C57BL/6 mice. Serum and tissue samples are collected after euthanizing mice by CO2 inhalation overdose followed by cervical dislocation[1].
References

[1]. Sundberg TB, et al. Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo. ACS Chem Biol. 2016 Aug 19;11(8):2105-11.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 761.0±70.0 °C at 760 mmHg
Molecular Formula C32H34ClN7O3
Molecular Weight 600.110
Flash Point 414.1±35.7 °C
Exact Mass 599.241150
LogP 3.12
Vapour Pressure 0.0±2.6 mmHg at 25°C
Index of Refraction 1.647
Storage condition 2-8℃

 Synonyms

Pyrimido[4,5-d]pyrimidin-2(1H)-one, 3-(2-chloro-6-methylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-1-(5-methoxy-2-pyridinyl)-
3-(2-Chloro-6-methylphenyl)-7-{[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino}-1-(5-methoxy-2-pyridinyl)-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one
Top Suppliers:I want be here



Get all suppliers and price by the below link:

YKL-05-099 suppliers


Price: $555/10mM*1mLinDMSO

Reference only. check more YKL-05-099 price