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Selonsertib (GS-4997)

Name: Selonsertib (GS-4997)
Brand: Selleck Chemicals
SKU: S8292
Rating: 5 (22 reviews)

Catalog No.S8292 Purity: 99.40%

Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

Selonsertib (GS-4997) Chemical Structure

CAS: 1448428-04-3

Selleck's Selonsertib (GS-4997) has been cited by 22 publications

Purity & Quality Control

Batch: Purity: 99.40%

99.40

Selonsertib (GS-4997) Related Products

Related Targets	ASK1	Click to Expand
Related Compound Libraries	Autophagy Compound Library Apoptosis Compound Library Ferroptosis Compound Library Pyroptosis Compound Library Mitochondria-Targeted Compound Library	Click to Expand

Choose Selective ASK Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Sf21	Function assay		60 mins		Inhibition of recombinant human N-terminal GST-tagged ASK1 catalytic domain (654 to 971 residues) expressed in baculovirus infected sf21 cells using STK3 as substrate after 60 mins by HTRF assay, IC50 = 0.005012 μM.	28337323
Click to View More Cell Line Experimental Data

Biological Activity

Description

Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

Targets

ASK1 ^[3]
(Cell-free assay)

8.3(pIC50)

In vitro
In vitro	Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor with pIC50 of 8.3.

In Vivo
In vivo	An orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Upon oral administration, ASK1 inhibitor GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. This prevents the phosphorylation of downstream kinases, such as c-Jun N-terminal kinases (JNKs) and p38 mitogen-activated protein kinase (p38 MAPK). By preventing the activation of ASK1-dependent signal transduction pathways, GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation^[2].

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02509624	Completed	Diabetic Kidney Disease	Gilead Sciences	August 18 2015	Phase 1

References

[4] Lou G, et al. Cell Biosci. 2021 Jan 7;11(1):9.

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Chemical Information & Solubility

Molecular Weight	445.49	Formula	C₂₄H₂₄FN₇O
CAS No.	1448428-04-3	SDF	Download Selonsertib (GS-4997) SDF
Smiles	CC1=CC(=C(C=C1N2C=C(N=C2)C3CC3)C(=O)NC4=CC=CC(=N4)C5=NN=CN5C(C)C)F
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 75 mg/mL ( (168.35 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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