Home Apoptosis ASK inhibitor Selonsertib (GS-4997) For research use only.

Selonsertib (GS-4997)

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

Selonsertib (GS-4997) Chemical Structure

CAS No. 1448428-04-3

Purity & Quality Control

Selonsertib (GS-4997) Related Products

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
NCT02509624 Completed
Diabetic Kidney Disease
Gilead Sciences
 August 18 2015 Phase 1

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)

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

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Selonsertib (GS-4997) | Selonsertib (GS-4997) supplier | purchase Selonsertib (GS-4997) | Selonsertib (GS-4997) cost | Selonsertib (GS-4997) manufacturer | order Selonsertib (GS-4997) | Selonsertib (GS-4997) distributor