Art. -Nr.: HY-18938

Selonsertib

(Synonyms: GS-4997)

25 Cited Publications

Kundenbewertung

Based on 25 publication(s) in Google Scholar

Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC₅₀ of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.05%
CAS. Nr.: 1448428-04-3
Formel: C₂₄H₂₄FN₇O
Molecular Weight:445.49

Speicherung:

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

Selonsertib Chemical Structure

CAS. Nr.: 1448428-04-3

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (25)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ASK1

8.3 (pIC₅₀)

Alle MAP3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	20 nM Compound: 4; GS-4997	Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr Inhibition of V5 tagged human ASK1 expressed in HEK-293T cells assessed as reduction in T838 autophosphorylation incubated for 1 hr	[PMID: 31710475]
HEK-293T	IC₅₀	20 nM Compound: 3	Inhibition of V5 tagged human ASK1 expressed in HEK293T cells assessed as reduction in T848 autophosphorylation incubated for 1 hr by MSD assay Inhibition of V5 tagged human ASK1 expressed in HEK293T cells assessed as reduction in T848 autophosphorylation incubated for 1 hr by MSD assay	[PMID: 32292554]
HepG2	IC₅₀	20 μM Compound: 1; GS-4997	Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth Cytotoxicity against human HepG2 cells assessed as inhibition of cell growth	[PMID: 32289582]

In Vitro

Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis^[1]. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1448428-04-3
Appearance Solid
Molecular Weight 445.49
Formel C₂₄H₂₄FN₇O
Color White to light yellow
SMILES

O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F
Synonyms

GS-4997
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 (25)

All Histological Imaging/StainingELISAIFCell Imaging/StainingIHCOthersCell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

Acta Pharm Sin B

Palmitoylated SARM1 targeting P4HA1 promotes collagen deposition and myocardial fibrosis: A new target for anti-myocardial fibrosis. [Abstract]

2025 Sep;15(9):4789-4806. PMID: 41049740

Selonsertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4789-4806. [Abstract]

Immunofluorescence in determining the expression of P4HA1 after treated with Berberine (BBC; p.o.; 20 mg/kg for 7 days ) and Selonsertib (p.o.; 20 mg/kg for 7 days ) in the heart tissue of MI mice. n=3. *P < 0.05, **P < 0.01 vs. Sham, #P < 0.05, ##P < 0.01 vs. MI. Scale bar, 200 µm.

Selonsertib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Sep;15(9):4789-4806. [Abstract]

Echocardiographic detection of cardiac function changes in MI mice and treated with Berberine (BBC; p.o.; 20 mg/kg for 7 days ) and Selonsertib (p.o.; 20 mg/kg for 7 days ) . n=3-4. *P < 0.05 vs. Sham, #P < 0.05 vs. MI.
Biomaterials

Modelling fatty liver disease with mouse liver-derived multicellular spheroids. [Abstract]

2022 Nov:290:121817. PMID: 36208587

Selonsertib purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Nov:290:121817. [Abstract]

Selonsertib (Selon; 10 μM; 10 days) slightly decreased the lipid uptake in the MCLS culture.

Selonsertib purchased from MedChemExpress. Usage Cited in: Biomaterials. 2022 Nov:290:121817. [Abstract]

Selonsertib (Selon; 10 μM; 48 h) slightly decreased the expression of Collagen 1 and lipid accumulation in the MCLS culture.
Cell Death Dis

Targeted inhibition of protein synthesis renders cancer cells vulnerable to apoptosis by unfolded protein response. [Abstract]

2023 Aug 26;14(8):561. PMID: 37626037
Phytomedicine

Apigenin ameliorates non-eosinophilic inflammation, dysregulated immune homeostasis and mitochondria-mediated airway epithelial cell apoptosis in chronic obese asthma via the ROS-ASK1-MAPK pathway. [Abstract]

2023 Mar:111:154646. PMID: 36645975
J Hazard Mater

Combined exposure of alumina nanoparticles and chronic stress exacerbates hippocampal neuronal ferroptosis via activating IFN-γ/ASK1/JNK signaling pathway in rats. [Abstract]

2021 Jun 5:411:125179. PMID: 33858114
Acta Pharmacol Sin

Targeting PPARα activation sensitizes glioblastoma cells to temozolomide and reverses acquired resistance by inhibiting H3K18 lactylation. [Abstract]

2025 Jun 11. PMID: 40500345
Basic Res Cardiol

Deubiquitinase USP43 exacerbates myocardial ischemia-reperfusion injury by stabilizing ASK1 and activating the JNK/P38 MAPK pathway. [Abstract]

2026 Jun;121(3):459-479. PMID: 42012501
Apoptosis

The GATA3-RFPL3-ASK1 axis suppresses breast cancer growth and lung metastasis. [Abstract]

2026 Apr 17;31(4):127. PMID: 41995771
Phytother Res

Perilla frutescens L. alleviates trimethylamine N-oxide-induced apoptosis in the renal tubule by regulating ASK1-JNK phosphorylation. [Abstract]

2023 Apr;37(4):1274-1292. PMID: 36420586

Selonsertib purchased from MedChemExpress. Usage Cited in: Phytother Res. 2023 Apr;37(4):1274-1292. [Abstract]

Selonsertib (5 µM) alleviates TMAO-induced morphological changes and improve cellular viability in RTEC cells.
Cell Biosci

Selonsertib, a potential drug for liver failure therapy by rescuing the mitochondrial dysfunction of macrophage via ASK1-JNK-DRP1 pathway. [Abstract]

2021 Jan 7;11(1):9. PMID: 33413667
Life Sci

Galectin-9 in human trophoblast cells: Implications for maternal-fetal immune balance and pregnancy complications. [Abstract]

2026 Mar 1:388:124173. PMID: 41544754
Commun Biol

NOD1 deficiency promotes inflammation via autophagic degradation of ASK1. [Abstract]

2025 May 21;8(1):781. PMID: 40399666

Selonsertib purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 May 21;8(1):781. [Abstract]

Selonsertib (15 mg/kg; IP; daily) reduced exaggerated inflammation in NOD1-KO mice.

Selonsertib purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 May 21;8(1):781. [Abstract]

Selonsertib (15 mg/kg; IP; daily) reduced plasma IL-1β levels in the NOD1-KO mice.

Selonsertib purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 May 21;8(1):781. [Abstract]

Selonsertib (15 mg/kg; IP; daily) reduced IL-1β (magenta) and DAPI (blue) in the coronary arteries of NOD-KO mice.
Int Immunopharmacol

Monocrotaline induces liver injury via TRX1-ASK1-JNK Axis-mediated mitochondrial damage in hepatocytes. [Abstract]

2026 Mar 1:172:116121. PMID: 41519004
Int Immunopharmacol

PIM1 attenuates renal ischemia-reperfusion injury by inhibiting ASK1-JNK/P38. [Abstract]

2023 Jan:114:109563. PMID: 36513021
Biochim Biophys Acta Mol Basis Dis

PUMA overexpression dissociates thioredoxin from ASK1 to activate the JNK/BCL-2/BCL-XL pathway augmenting apoptosis in ovarian cancer. [Abstract]

2022 Dec 1;1868(12):166553. PMID: 36122664
Sci Rep

Digital pathology with artificial intelligence analysis provides insight to the efficacy of anti-fibrotic compounds in human 3D MASH model. [Abstract]

2024 Mar 11;14(1):5885. PMID: 38467661
Cancers (Basel)

Coxsackievirus Group B3 Has Oncolytic Activity against Colon Cancer through Gasdermin E-Mediated Pyroptosis. [Abstract]

2022 Dec 15;14(24):6206. PMID: 36551691
Neurochem Res

Anti-neuroinflammatory Effects and Brain Pharmacokinetic Properties of Selonsertib, an Apoptosis signal-regulating Kinase 1 Inhibitor, in mice. [Abstract]

2022 Dec;47(12):3829-3837. PMID: 36309631
FASEB J

E3 Ubiquitin Ligase TRIM21 Exacerbates Pathological Cardiac Hypertrophy Through ASK1 K63-Linked Polyubiquitination. [Abstract]

2025 Dec 15;39(23):e71311. PMID: 41359290
Animal Model Exp Med

Targeting ASK1 by CS17919 alleviates kidney- and liver-related diseases in murine models. [Abstract]

2025 Jan;8(1):102-113. PMID: 38873818
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
bioRxiv

2026 Jan 25.
University of Oxford

2023 Oct.
Research Square Print

2022 Aug.
Research Square Preprint

2021 Jul.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 66.67 mg/mL (149.66 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

2.2447 mL

11.2236 mL

22.4472 mL

5 mM

0.4489 mL

2.2447 mL

4.4894 mL

10 mM

0.2245 mL

1.1224 mL

2.2447 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: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.62 mg/mL (5.88 mM); Clear solution

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (4.67 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 3

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

Solubility: ≥ 2.08 mg/mL (4.67 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

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

Solubility: ≥ 2.08 mg/mL (4.67 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 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]. Lanier M, et al. Structure-Based Design of ASK1 Inhibitors as Potential Agents for Heart Failure. ACS Med Chem Lett. 2017 Feb 8;8(3):316-320. [Content Brief]

[2]. Lin JH, et al. Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron. 2015;129(1):29-33. [Content Brief]

[3]. Loomba R, et al. The ASK1 inhibitor selonsertib in patients with nonalcoholic steatohepatitis: A randomized, phase 2trial. Hepatology. 2018 Feb;67(2):549-559. [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	2.2447 mL	11.2236 mL	22.4472 mL	56.1180 mL
	5 mM	0.4489 mL	2.2447 mL	4.4894 mL	11.2236 mL
	10 mM	0.2245 mL	1.1224 mL	2.2447 mL	5.6118 mL
	15 mM	0.1496 mL	0.7482 mL	1.4965 mL	3.7412 mL
	20 mM	0.1122 mL	0.5612 mL	1.1224 mL	2.8059 mL
	25 mM	0.0898 mL	0.4489 mL	0.8979 mL	2.2447 mL
	30 mM	0.0748 mL	0.3741 mL	0.7482 mL	1.8706 mL
	40 mM	0.0561 mL	0.2806 mL	0.5612 mL	1.4029 mL
	50 mM	0.0449 mL	0.2245 mL	0.4489 mL	1.1224 mL
	60 mM	0.0374 mL	0.1871 mL	0.3741 mL	0.9353 mL
	80 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7015 mL
	100 mM	0.0224 mL	0.1122 mL	0.2245 mL	0.5612 mL

Keywords

Selonsertib

25 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Selonsertib

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Selonsertib

Alle MAP3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (25)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Selonsertib

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Selonsertib

Alle MAP3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (25)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Selonsertib Related Classifications

HY-18938 Related Classifications