YKL-05-099

Catalog No.S9646 Batch:S964601

Print

Technical Data

Formula

C32H34ClN7O3
Molecular Weight 600.11 CAS No. 1936529-65-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (166.63 mM)
Ethanol 100 mg/mL (166.63 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description YKL-05-099 is an inhibitor of salt-inducible kinase (SIK) with IC50 of ~10 nM, ~40 nM and ~30 nM for SIK1, SIK2 and SIK3, respectively.
Targets
SIK1 [1]
(Cell-free assay)		 SIK3 [1]
(Cell-free assay)		 SIK2 [1]
(Cell-free assay)
10 nM 30 nM 40 nM
In vitro

YKL-05-099 displays cell-based activities consistent with SIK inhibition. Pre-treatment with the indicated concentrations of YKL-05-099 for 24 hr potentiates IL-10 production by Zymosan A-stimulated BMDCs.[1]
In vivo

Well-tolerated doses of YKL-05-099 achieve free serum concentrations above its IC50 for SIK2 inhibition for > 16 hours and reduce phosphorylation of a known SIK substrate in vivo. While in vivo active doses of YKL-05-099 recapitulate the effects of SIK inhibition on inflammatory cytokine responses, they do not induce metabolic abnormalities observed in Sik2 knockout mice. These results identify YKL-05-099 as a useful probe to investigate SIK function in vivo, and further support the development of SIK inhibitors for treatment of inflammatory disorders.[1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    bone marrow-derived dendritic cells (BMDCs)

  • Concentrations

    1 μM

  • Incubation Time

    24 hr

  • Method

    --
Animal Study:

[1]
  • Animal Models

    male 8–10 week-old C57BL/6 mice

  • Dosages

    5 mg/kg-50 mg/kg

  • Administration

    IP

Selleck's YKL-05-099 has been cited by 2 publications

Salt-Inducible Kinase 1 is a potential therapeutic target in Desmoplastic Small Round Cell Tumor [ Oncogenesis, 2022, 11(1):18] PubMed: 35443736
Salt-inducible kinase inhibition sensitizes human acute myeloid leukemia cells to all-trans retinoic acid-induced differentiation [ Int J Hematol, 2020, 10.1007/s12185-020-03026-1] PubMed: 33074481

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.