Art. -Nr.: HY-101147

YKL-05-099

9 Cited Publications

Kundenbewertung

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).

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Reinheit: 99.73%
CAS. Nr.: 1936529-65-5
Formel: C₃₂H₃₄ClN₇O₃
Molecular Weight:600.11

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

YKL-05-099 Chemical Structure

CAS. Nr.: 1936529-65-5

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

SIK1

SIK3

Alle Salt-inducible Kinase (SIK) Isoform-spezifische Produkte anzeigen :

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].

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

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].

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

Chemical Information

CAS. Nr. 1936529-65-5
Appearance Solid
Molecular Weight 600.11
Formel C₃₂H₃₄ClN₇O₃
Color White to light yellow
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

SIK1 promotes ferroptosis resistance in pancreatic cancer via HDAC5-STAT6-SLC7A11 axis. [Abstract]

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

MEF2C opposes Notch in lymphoid lineage decision and drives leukemia in the thymus. [Abstract]

2022 May 10;e150363. PMID: 35536646
bioRxiv

2025 March 10.
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
Patent

US20200246435A1.
Harvard Medical School LINCS LIBRARY

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 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

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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

YKL-05-099

9 Cited Publications

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YKL-05-099

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Pyroptosis Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) YKL-05-099

Alle Salt-inducible Kinase (SIK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YKL-05-099

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Pyroptosis Compound Library

Targeted Diversity Library

Heterocyclic Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) YKL-05-099

Alle Salt-inducible Kinase (SIK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (9)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YKL-05-099 Related Classifications

HY-101147 Related Classifications