Selonsertib (GS-4997)

Catalog No.S8292

For research use only.

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 No. 1448428-04-3

Selleck's Selonsertib (GS-4997) has been cited by 16 publications

Purity & Quality Control

Choose Selective ASK Inhibitors

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)
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf21 NWTvbXRsTnWwY4Tpc44h[XO|YYm= MX:2NEBucW6| M2Lsb2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iTj30[ZJucW6jbDDHV3QufGGpZ3XkJGFUUzFiY3H0ZYx6fGmlIHTvcYFqdiBqNkW0JJRwKDl5MTDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIIPmNlEh[2WubIOgeZNqdmdiU2TLN{BieyC|dXLzeJJifGViYX\0[ZIhPjBibXnud{BjgSCKVGLGJIF{e2G7LDDJR|UxKD1iMD6wNFUxOTJizszNMi=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN|N{OyN{c,Ojh|M{ezNlM9N2F-
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].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 445.49
Formula

C24H24FN7O

CAS No. 1448428-04-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C=C1N2C=C(N=C2)C3CC3)C(=O)NC4=CC=CC(=N4)C5=NN=CN5C(C)C)F

In vivo Formulation Calculator (Clear solution)

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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.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02509624 Completed Drug: Selonsertib Diabetic Kidney Disease Gilead Sciences August 18 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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