Art. -Nr.: HY-15776

HG-9-91-01

(Synonyms: SIK inhibitor 1)

26 Cited Publications

Kundenbewertung

Based on 26 publication(s) in Google Scholar

HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC₅₀s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.

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Reinheit: 99.77%
CAS. Nr.: 1456858-58-4
Formel: C₃₂H₃₇N₇O₃
Molecular Weight:567.68

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

HG-9-91-01 Chemical Structure

CAS. Nr.: 1456858-58-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (26)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC₅₀s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.

IC₅₀ & Target

SIK1

SIK2

SIK3

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

In Vitro

HG-9-91-01 inhibits a number of protein tyrosine kinases that possess a threonine residue at the gatekeeper site, such as Src family members (Src, Lck, and Yes), BTK, and the FGF and Ephrin receptors^[1]. HG-9-91-01 demonstrates a strong correlation between the potency of SIK2 inhibition and enhanced IL-10 production. In agreement with these reports, pretreating BMDCs with HG-9-91-01, a recently described inhibitor of SIK1-3, along with several other kinases, results in concentration-dependent potentiation of zymosan-induced IL-10 production with an EC₅₀ ~200 nM and a maximum effect similar to that observed with PGE₂^[2]. HG-9-91-01 has more than a 100-fold greater potency against SIKs than AMPK (IC₅₀=4.5 μM) in a cell-free assay. HG-9-91-01 treatment dose dependently increased mRNA expression of Pck1 and G6pc and that effect is similar in cells treated with 4 μM HG-9-91-01. Consistent with this observation, there is also a dose-dependent increase in glucose production following HG-9-91-01 treatment^[3].

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

Chemical Information

CAS. Nr. 1456858-58-4
Appearance Solid
Molecular Weight 567.68
Formel C₃₂H₃₇N₇O₃
Color White to yellow
SMILES

CC1=CC=CC(C)=C1NC(N(C2=NC=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=C2)C5=CC=C(OC)C=C5OC)=O
Synonyms

SIK inhibitor 1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (26)

All WB

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Journal Impact Factor

Nat Cancer

Genome-scale functional genomics identify genes preferentially essential for multiple myeloma cells compared to other neoplasias. [Abstract]

2023 May;4(5):754-773. PMID: 37237081
Nat Metab

In vivo screen identifies a SIK inhibitor that induces β cell proliferation through a transient UPR. [Abstract]

2021 May;3(5):682-700. PMID: 34031592
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Mol Cell

LKB1 controls inflammatory potential through CRTC2-dependent histone acetylation. [Abstract]

2023 Jun 1;83(11):1872-1886.e5. PMID: 37172591
Cell Death Dis

Salt-inducible kinases inhibitor HG-9-91-01 targets RIPK3 kinase activity to alleviate necroptosis-mediated inflammatory injury. [Abstract]

2022 Feb 25;13(2):188. PMID: 35217652
Cell Death Dis

SIK2 enhances synthesis of fatty acid and cholesterol in ovarian cancer cells and tumor growth through PI3K/Akt signaling pathway. [Abstract]

2020 Jan 13;11(1):25. PMID: 31932581
Cell Death Dis

Salt-inducible kinase 1 regulates bone anabolism via the CRTC1-CREB-Id1 axis. [Abstract]

2019 Oct 31;10(11):826. PMID: 31672960
Oncogene

SIK2 maintains breast cancer stemness by phosphorylating LRP6 and activating Wnt/β-catenin signaling. [Abstract]

2022 Apr;41(16):2390-2403. PMID: 35277657
Cell Rep

The metabolic sensor LKB1 regulates ILC3 homeostasis and mitochondrial function. [Abstract]

2025 Mar 21;44(4):115456. PMID: 40120107
Cell Rep

A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin. [Abstract]

2017 Jun 13;19(11):2177-2184. PMID: 28614705
JCI Insight

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

2022 May 10;e150363. PMID: 35536646
Inflamm Bowel Dis

HG-9-91-01 Attenuates Murine Experimental Colitis by Promoting Interleukin-10 Production in Colonic Macrophages Through the SIK/CRTC3 Pathway. [Abstract]

2021 Oct 20;27(11):1821-1831. PMID: 33988718
Mediators Inflamm

Inhibition of SIK1 Alleviates the Pathologies of Psoriasis by Disrupting IL-17 Signaling. [Abstract]

2025 Feb 7:2025:3540219. PMID: 39959414
Cell Signal

JUP/plakoglobin is regulated by salt-inducible kinase 2, and is required for insulin-induced signalling and glucose uptake in adipocytes. [Abstract]

2020 Dec:76:109786. PMID: 32966883
FASEB J

Activation of SIK2 inhibits gluconeogenesis and alleviates lipogenesis-induced inflammatory response by SIK2-CRTC2-ACC1 in hepatocytes of large yellow croaker (Larimichthys crocea). [Abstract]

2025 Mar 31;39(6):e70393. PMID: 40067199
J Biol Chem

The structures of salt inducible kinase 3 in complex with pharmacological inhibitors reveal determinants for binding and selectivity. [Abstract]

2024 May;300(5):107201. PMID: 38508313
J Biol Chem

Salt-inducible Kinase 3 Signaling Is Important for the Gluconeogenic Programs in Mouse Hepatocytes. [Abstract]

2015 Jul 17;290(29):17879-17893. PMID: 26048985

HG-9-91-01 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2015 Jul 17;290(29):17879-17893. [Abstract]

Pterosin B does not inhibit SIK3 kinase activity up to 1 mM, whereas the strong pan-SIK inhibitor HG9-91-01 completely inhibits SIK3 kinase activity even at 1 μM. The GST-SIK3 enzyme is expressed in HEK293 cells, purified with a glutathione resin, and incubated with compounds, the coumarin-labeled CRTC2 peptide, and 1 mM ATP for 1 h. The phosphorylated and nonphosphorylated peptides are separated by electrophoresis.
J Cell Sci

Activation of IRE1, PERK and salt-inducible kinases leads to Sec body formation in Drosophila S2 cells. [Abstract]

2021 Sep 1;134(17):jcs258685. PMID: 34350957
J Gen Physiol

Methodological improvements for fluorescence recordings in Xenopus laevis oocytes. [Abstract]

2019 Feb 4;151(2):264-272. PMID: 30606741
Biochem Biophys Res Commun

Salt-inducible kinase 2 regulates TFEB and is required for autophagic flux in adipocytes. [Abstract]

2019 Jan 15;508(3):775-779. PMID: 30528240

HG-9-91-01 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 15;508(3):775-779. [Abstract]

Differentiated 3T3-L1 adipocytes are treated with different doses of HG-9-91-01, western analysis of protein expression is showed.
Heliyon

Salt-inducible kinase 1 deficiency promotes vascular remodeling in pulmonary arterial hypertension via enhancement of yes-associated protein-mediated proliferation. [Abstract]

2022 Oct 10;8(10):e11016. PMID: 36276742
Patent

US20200246435A1.
bioRxiv

2020 Apr.
Technical University of Munich

2017 Oct.
Kansai University

2017 Mar.

HG-9-91-01 purchased from MedChemExpress. Usage Cited in: Kansai University. 2017 Mar.

Pterosin B quickly induces the dephosphorylation of CRTC2 in AML-12 cells, which is also observed in Fsk- and HG9-91-01-treated cells.
Elife

Salt-inducible kinases mediate nutrient-sensing to link dietary sugar and tumorigenesis in Drosophila. [Abstract]

2015 Nov 17:4:e08501. PMID: 26573956

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (440.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.7616 mL

8.8078 mL

17.6156 mL

5 mM

0.3523 mL

1.7616 mL

3.5231 mL

10 mM

0.1762 mL

0.8808 mL

1.7616 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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: ≥ 2.08 mg/mL (3.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Cell Assay^[2]

Bone marrow is harvested from femurs and tibias of C57BL/6 mice. Bone-marrow-derived dendritic cells (BMDCs) are differentiated DMEM. Cultures are differentiated for 7 d and routinely analyzed for >90% CD11c (allophycocyanin (APC) anti-CD11c clone HL3) positivity by flow cytometry before use in experiments. Lentiviral transduction of bone marrow cultures is conducted by addition of 293T culture supernatants containing lentiviral particles encoding the CREB-dependent luciferase reporter construct or CRTC3 targeting or control shRNAs 1 d postisolation. Stable integration of lentiviral shRNA constructs is selected by addition of puromycin (3 μg/mL) on day 4 posttransduction. After 2 d, stably transduced BMDCs are released from selection and used in subsequent assays. Unless otherwise indicated, cells are treated for 2 d with PGE2 (5 μM) or HG-9-91-01 (0.5 μM) or an equivalent concentration of DMSO (≤0.5%) and then stimulated for 18 h with LPS (100 ng/mL), R848 (10 μg/mL), or Zymosan (4 μg/mL)^[2].

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 (280 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]. Clark K, et al. Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated andregulatory macrophages. Proc Natl Acad Sci U S A. 2012 Oct 16;109(42):16986-91. [Content Brief]

[2]. Sundberg TB, et al. Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells. Proc Natl Acad Sci U S A. 2014 Aug 26;111(34):12468-73. [Content Brief]

[3]. Patel K, et al.The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver. Nat Commun. 2014 Aug 4;5:4535. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7616 mL	8.8078 mL	17.6156 mL	44.0389 mL
	5 mM	0.3523 mL	1.7616 mL	3.5231 mL	8.8078 mL
	10 mM	0.1762 mL	0.8808 mL	1.7616 mL	4.4039 mL
	15 mM	0.1174 mL	0.5872 mL	1.1744 mL	2.9359 mL
	20 mM	0.0881 mL	0.4404 mL	0.8808 mL	2.2019 mL
	25 mM	0.0705 mL	0.3523 mL	0.7046 mL	1.7616 mL
	30 mM	0.0587 mL	0.2936 mL	0.5872 mL	1.4680 mL
	40 mM	0.0440 mL	0.2202 mL	0.4404 mL	1.1010 mL
	50 mM	0.0352 mL	0.1762 mL	0.3523 mL	0.8808 mL
	60 mM	0.0294 mL	0.1468 mL	0.2936 mL	0.7340 mL
	80 mM	0.0220 mL	0.1101 mL	0.2202 mL	0.5505 mL
	100 mM	0.0176 mL	0.0881 mL	0.1762 mL	0.4404 mL

Keywords

HG-9-91-01

26 Cited Publications

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HG-9-91-01

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors 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

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Publications Citing Use of MedChemExpress (MCE) HG-9-91-01

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

Biologische Aktivität

Chemical Information

Publications (26)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HG-9-91-01

Chemical Probe Library

Targeted Diversity Library

Heterocyclic Compound Library

Highly Selective Inhibitors 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

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Publications Citing Use of MedChemExpress (MCE) HG-9-91-01

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

Biologische Aktivität

Chemical Information

Publications (26)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HG-9-91-01 Related Classifications

HY-15776 Related Classifications