Cat. No.: HY-101147

YKL-05-099

Name: YKL-05-099
Brand: MedChemExpress
SKU: HY-101147
Price: 85.00 USD
Availability: InStock
Rating: 5 (9 reviews)

9 Cited Publications

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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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Pureté : 99.73%
CAS No.: 1936529-65-5
Formule: C₃₂H₃₄ClN₇O₃
Masse moléculaire:600.11

Stockage:

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 No.: 1936529-65-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

SIK1

QSK/SIK3

Voir tous les produits spécifiques à Isoform Salt-inducible Kinase (SIK) :

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 No. 1936529-65-5
Appearance Solid
Masse moléculaire 600.11
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (9)

All In Vivo Efficacy StudyCell Proliferation/Viability AssayIF

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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

YKL-05-099 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2026 Jun;27(6):1237-1252. [Abstract]

YKL-05–099 (6 mg/kg; I.P.; 5 times per week) significantly extended survival of OvCa-bearing mice.

YKL-05-099 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2026 Jun;27(6):1237-1252. [Abstract]

YKL-05–099 (6 mg/kg; I.P.; 5 times per week) significantly increased the expression of apoptosis marked by Cleaved Caspase 3 in PPM tumors.
Cancer Lett

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

2025 Jul 28:623:217726. PMID: 40250791

YKL-05-099 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2025 Jul 28:623:217726. [Abstract]

YKL-05–099 (1 μM; 72 h) inhibited cell viability in Panc05.04, MIA PaCa-2, AsPC-1 cells.

YKL-05-099 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2025 Jul 28:623:217726. [Abstract]

YKL-05–099 (15 mg/kg; three times a week for 30 days) decreased tumor volume and weight in nude mice.

YKL-05-099 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2025 Jul 28:623:217726. [Abstract]

YKL-05–099 (15 mg/kg; three times a week for 30 days) revealed a significant decrease in Ki67-positive cells in PDX tumor tissues.

YKL-05-099 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2025 Jul 28:623:217726. [Abstract]

YKL-05–099 (15 mg/kg; three times a week for 30 days)increased the expression of 4-HNE in PDX tumor tissues.
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

Solvant et solubilité

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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

Bioz

Keywords

YKL-05-099

9 Cited Publications

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YKL-05-099

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

Voir tous les produits spécifiques à Isoform Salt-inducible Kinase (SIK)