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YKL-05-099

Catalog No. T17271 CAS 1936529-65-5

YKL-05-099 is an inhibitor of the salt-inducible kinase(SIK1 and SIK3 ; IC50s: 10 and 30 nM, respectively). It has a slightly less potent SIK2-inhibitory (IC50:40 nM).

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YKL-05-099, CAS 1936529-65-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 68.00
5 mg	In stock	$ 147.00
10 mg	In stock	$ 228.00
25 mg	In stock	$ 397.00
50 mg	In stock	$ 589.00
100 mg	In stock	$ 843.00
500 mg	In stock	$ 1,730.00
1 mL * 10 mM (in DMSO)	In stock	$ 195.00

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Purity: 99.89%

Purity: 99.22%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	YKL-05-099 is an inhibitor of the salt-inducible kinase(SIK1 and SIK3 ; IC50s: 10 and 30 nM, respectively). It has a slightly less potent SIK2-inhibitory (IC50:40 nM).
Targets&IC50	SIK1:10 nM, SIK2:40 nM, SIK3:30 nM
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	YKL-05-099 exhibits high solubility (PBS solubility=428 μM) and is predominantly in an unbound state in mouse plasma, displaying non-toxic characteristics at concentrations below 10 μM. This compound is metabolically stable, showing more than 2 hours of stability in mouse liver microsomes. Functionally, YKL-05-099 effectively modulates immune response by reducing TNFα levels in a dose-dependent manner, starting at 5 mg/Kg, and significantly enhancing IL-10 secretion at a 20 mg/Kg dose, achieving a more than two-fold increase. Furthermore, it inhibits phosphorylation of HDAC5 at the SIK-regulated site (Ser259) in a dose-responsive manner, with notable reduction starting at 5 mg/Kg and becoming undetectable by immunoblotting from the 20 mg/Kg dose onwards [1].

Molecular Weight	600.11
Formula	C32H34ClN7O3
CAS No.	1936529-65-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 75 mg/mL (124.98 mM)

References and Literature

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.

Citations

1. Wan J, He Z, Zhao Y, et al.Novel strategy of senescence elimination via toxicity-exempted kinome perturbations by nanoliposome-based thermosensitive hydrogel for osteoarthritis therapy.Advanced Composites and Hybrid Materials.2023, 6(3): 104.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Inhibitor Library Oxidation-Reduction Compound Library Anti-Prostate Cancer Compound Library Bioactive Compounds Library Max Anti-Liver Cancer Compound Library Metabolism Compound Library Immunology/Inflammation Compound Library Glycolysis Compound Library Anti-Obesity Compound Library

Related Products

Related compounds with same targets

MRT 67307 dihydrochloride ARN-3236 YKL-06-062 HG-9-91-01 YKL-06-061 WH-4-025

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Keywords

YKL-05-099 1936529-65-5 PI3K/Akt/mTOR signaling SIK YKL05099 YKL 05 099 inhibit Salt-inducible Kinase (SIK) Inhibitor inhibitor

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