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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 | 75 mg/mL (168.35 mM) | |
| Ethanol | 50 mg/mL (112.23 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 29 publications
| Multi-omic human pancreatic islet endoplasmic reticulum and cytokine stress response mapping provides type 2 diabetes genetic insights [ Cell Metab, 2024, 36(11):2468-2488.e7] | PubMed: 39383866 |
| CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer [ Cell Death Dis, 2024, 15(9):662] | PubMed: 39256356 |
| Cetylpyridinium chloride triggers paraptosis to suppress pancreatic tumor growth via the ERN1-MAP3K5-p38 pathway [ iScience, 2024, 27(8):110598] | PubMed: 39211547 |
| 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 |
| ABT‑737 increases cisplatin sensitivity through the ROS‑ASK1‑JNK MAPK signaling axis in human ovarian cancer cisplatin‑resistant A2780/DDP cells [ Oncol Rep, 2024, 52(3)122] | PubMed: 39054955 |
| Abrogating PDK4 activates autophagy-dependent ferroptosis in breast cancer via ASK1/JNK pathway [ J Cancer Res Clin Oncol, 2024, 150(4):218] | PubMed: 38678126 |
| Increasing expression of dual-specificity phosphatase 12 mitigates oxygen-glucose deprivation/reoxygenation-induced neuronal apoptosis and inflammation through inactivation of the ASK1-JNK/p38 MAPK pathway [ Autoimmunity, 2024, 57(1):2345919] | PubMed: 38721693 |
| 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 |
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.