1. Immunology/Inflammation
  2. Salt-inducible Kinase (SIK)

YKL-05-099 

Cat. No.: HY-101147 Purity: 99.76%
Handling Instructions

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

For research use only. We do not sell to patients.

YKL-05-099 Chemical Structure

YKL-05-099 Chemical Structure

CAS No. : 1936529-65-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 555 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2220 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Protocol

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  • References

Description

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

IC50 & 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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 75 mg/mL (124.98 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6664 mL 8.3318 mL 16.6636 mL
5 mM 0.3333 mL 1.6664 mL 3.3327 mL
10 mM 0.1666 mL 0.8332 mL 1.6664 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.17 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

600.11

Formula

C₃₂H₃₄ClN₇O₃

CAS No.

1936529-65-5

SMILES

O=C1N(C2=NC=C(OC)C=C2)C3=NC(NC4=CC=C(C5CCN(C)CC5)C=C4OC)=NC=C3CN1C6=C(C)C=CC=C6Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.76%

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Product Name:
YKL-05-099
Cat. No.:
HY-101147
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YKL-05-099

Cat. No.: HY-101147