YKL-05-099
Based on 9 publication(s) in Google Scholar
YKL-05-099 is a salt-inducible kinase (SIK) inhibitor. YKL-05-099 binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent SIK2-inhibitory (IC50=40 nM).
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 1936529-65-5
- Formula: C32H34ClN7O3
- Molecular Weight:600.11
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
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Kinase Inhibitor Library
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Targeted Diversity Library
HY-L099
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Heterocyclic Compound Library
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Multi-Target Compound Library
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Bioactive Compound Library Max
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Kinase Inhibitor Library Mini
HY-L009M
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
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High-Throughput Bioactive Compound Library
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Posttranslational Modification Library
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Publications Citing Use of MedChemExpress (MCE) YKL-05-099
More- Nat Immunol. 2026 Jun;27(6):1237-1252. [Abstract]
- Cancer Lett. 2025 Apr 16:217726. [Abstract]
- Proc Natl Acad Sci U S A. 2024 May 21;121(21):e2403685121. [Abstract]
- Br J Pharmacol. 2026 Apr 29. [Abstract]
- JCI Insight. 2022 May 10;e150363. [Abstract]
- bioRxiv. 2025 March 10.
- bioRxiv. 2023 Oct 20:2023.10.19.563158. [Abstract]
- Patent. US20200246435A1.
- Harvard Medical School LINCS LIBRARY
Biological Activity
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SIK1 |
SIK3 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1936529-65-5
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Appearance Solid
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Molecular Weight 600.11
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Formula C32H34ClN7O3
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Color White to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Nat Immunol
Inhibition of salt-inducible kinases reprograms T cells and antitumor immunity in ovarian cancer. [Abstract]2026 Jun;27(6):1237-1252. PMID: 42162294 -
Cancer Lett
2025 Apr 16:217726. PMID: 40250791 -
Proc Natl Acad Sci U S A
Genome-wide CRISPR screens in spheroid culture reveal that the tumor suppressor LKB1 inhibits growth via the PIKFYVE lipid kinase. [Abstract]2024 May 21;121(21):e2403685121. PMID: 38743625 -
Br J Pharmacol
Dual pharmacological targeting of coactivator-associated arginine methyltransferase 1 (CARM1) and salt inducible kinase (SIK) drives ketogenesis in both hepatocytes and mice. [Abstract]2026 Apr 29. PMID: 42055601 -
JCI Insight
2022 May 10;e150363. PMID: 35536646 -
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bioRxiv
LKB1 suppresses growth and promotes the internalization of EGFR through the PIKFYVE lipid kinase. [Abstract]2023 Oct 20:2023.10.19.563158. PMID: 37904985 -
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Harvard Medical School LINCS LIBRARY
Solvent & Solubility
DMSO : ≥ 75 mg/mL (124.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6664 mL | 8.3318 mL | 16.6636 mL | 41.6590 mL |
| 5 mM | 0.3333 mL | 1.6664 mL | 3.3327 mL | 8.3318 mL | |
| 10 mM | 0.1666 mL | 0.8332 mL | 1.6664 mL | 4.1659 mL | |
| 15 mM | 0.1111 mL | 0.5555 mL | 1.1109 mL | 2.7773 mL | |
| 20 mM | 0.0833 mL | 0.4166 mL | 0.8332 mL | 2.0830 mL | |
| 25 mM | 0.0667 mL | 0.3333 mL | 0.6665 mL | 1.6664 mL | |
| 30 mM | 0.0555 mL | 0.2777 mL | 0.5555 mL | 1.3886 mL | |
| 40 mM | 0.0417 mL | 0.2083 mL | 0.4166 mL | 1.0415 mL | |
| 50 mM | 0.0333 mL | 0.1666 mL | 0.3333 mL | 0.8332 mL | |
| 60 mM | 0.0278 mL | 0.1389 mL | 0.2777 mL | 0.6943 mL | |
| 80 mM | 0.0208 mL | 0.1041 mL | 0.2083 mL | 0.5207 mL | |
| 100 mM | 0.0167 mL | 0.0833 mL | 0.1666 mL | 0.4166 mL |
YKL-05-099 Related Classifications
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