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Technical Data
| Formula | C24H24FN7O |
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| Molecular Weight | 445.49 | CAS No. | 1448428-04-3 | |
| Solubility (25°C)* | In vitro | DMSO | 89 mg/mL (199.78 mM) | |
| Ethanol | 40 mg/mL (89.78 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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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. | ||
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| In vitro | Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor with pIC50 of 8.3. |
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| 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)
References
Selleck's Selonsertib (GS-4997) has been cited by 23 publications
| ER Stress-Activated HSF1 Governs Cancer Cell Resistance to USP7 Inhibitor-Based Chemotherapy through the PERK Pathway [ Int J Mol Sci, 2024, 25(5)2768] | PubMed: 38474017 |
| Co-targeting ASK1 and THRβ synergistically improves steatohepatitis and fibrosis in a MASH animal model [ Biochem Biophys Res Commun, 2024, 705:149739] | PubMed: 38460439 |
| Nitric oxide-induced ribosome collision activates ribosomal surveillance mechanisms [ Cell Death Dis, 2023, 14(7):467] | PubMed: 37495584 |
| Nitric oxide-induced ribosome collision activates ribosomal surveillance mechanisms [ Cell Death Dis, 2023, 14(7):467] | PubMed: 37495584 |
| Metabolic improvement and liver regeneration by inhibiting CXXC5 function for non-alcoholic steatohepatitis treatment [ Exp Mol Med, 2022, 54(9):1511-1523] | PubMed: 36114279 |
| Systematic analysis of the MAPK signaling network reveals MAP3K-driven control of cell fate [ Cell Syst, 2022, 13(11):885-894.e4] | PubMed: 36356576 |
| CCN6 improves hepatic steatosis, inflammation, and fibrosis in non-alcoholic steatohepatitis [ Liver Int, 2022, 10.1111/liv.15430] | PubMed: 36156376 |
| Glutathione S-transferase Mu 2 inhibits hepatic steatosis via ASK1 suppression [ Commun Biol, 2022, 5(1):326] | PubMed: 35388144 |
| Distinct developmental and degenerative functions of SARM1 require NAD+ hydrolase activity [ PLoS Genet, 2022, 18(6):e1010246] | PubMed: 35737728 |
| Proteasome dysfunction under compromised redox metabolism dictates liver injury in NASH through ASK1/PPARγ binodal complementary modules [ Redox Biol, 2021, 45:102043] | PubMed: 34144391 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.