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Selonsertib

Catalog No. T3350   CAS 1448428-04-3
Synonyms: GS-4997

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

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Selonsertib Chemical Structure
Selonsertib, CAS 1448428-04-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 45.00
5 mg In stock $ 72.00
10 mg In stock $ 93.00
25 mg In stock $ 159.00
50 mg In stock $ 202.00
100 mg In stock $ 363.00
200 mg In stock $ 522.00
500 mg In stock $ 847.00
1 mL * 10 mM (in DMSO) In stock $ 78.00
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Purity: 99.53%
Purity: 98.97%
Purity: 95.04%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.
Targets&IC50 ASK1:8.3(pIC50)
Kinase Assay Kinase assays mTOR.: Reagents are prepared as follows:"Simple Tor buffer": 10 mM Tris pH 7.4, 100 mM NaCl, 0.1% Tween-20, 1 mM DTT. Recombinant mTOR is diluted in this buffer to an assay concentration of 0.200ug/mL. ATP/Substrate solution: 0.075 mM ATP, 12.5 mM MnCl2, 50 mM Hepes, pH 7.4, 50 mM β-GOP, 250 nM Microcystin LR, 0.25 mM EDTA, 5 mM DTT, and 3.5 μg/mL GST-p70S6. Dilution Curve: A 10-point, 1:3 dilution of compounds are prepared in neat DMSO at 50 times the final assay concentration. Detection reagent mix: 50 mM HEPES, pH 7.4 0.01% Triton X-100, 0.01% BSA, 0.1 mM EDTA, 12.7 ug/mL Cy5-anti-GST antibody, 9 ng/ml anti-phospho p70S6 antibody (Thr389), 627ng/mL anti-mouse IgG labeled with Lance Eu. To 20 uL of the Simple Tor buffer is added 0.5 uL of the compound Dilution Curve in DMSO. The final concentration range for compound is 30 to 0.0015 μM. To initiate the reaction, 5 μL of the ATP/substrate solution is added to the above. The reaction is allowed to run for 60 minutes. The assay is stopped by adding 5 μL of 60 mM EDTA. Ten (10) μL of detection reagent mix is then added, and the mixture is allowed to sit at least 2 hours before reading on a Perkin Elmer Envision microplate reader set to detect Europium-based TR-FRET.
Synonyms GS-4997
Molecular Weight 445.49
Formula C24H24FN7O
CAS No. 1448428-04-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 34 mg/mL (76.3 mM)

Ethanol: 23 mg/mL (51.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Lin JH, et al. Nephron. 2015, 129(1):29-33.

TargetMolCitations

1. Yuan J, Yao C, Tang J, et al. Enhanced GRP78 protein expression via the IRE1α/ASK1/p38 MAPK pathway during As2O3-induced endoplasmic reticulum stress in BEAS-2B cells. Toxicology. 2021, 462: 152962.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Inhibitor Library Apoptosis Compound Library Anti-Metabolism Disease Compound Library Anti-Prostate Cancer Compound Library Pyroptosis Compound Library

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Keywords

Selonsertib 1448428-04-3 Apoptosis MAPK ASK Inhibitor GS-4997 inhibit MAP3K GS4997 MAP kinase kinase kinase, MEKK, MAPKKK GS 4997 inhibitor

 

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