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Technical Data
| Formula | C22H26N6O2 |
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| Molecular Weight | 406.48 | CAS No. | 623152-17-0 | |
| Solubility (25°C)* | In vitro | DMSO | 81 mg/mL (199.27 mM) | |
| Water | Insoluble | |||
| Ethanol | 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 | BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38. | ||
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| In vitro | BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop[2]. | ||
| In vivo | The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And at an oral dose of 10 mg/kg, the mouse AUC0-8 h for BMS-582949 is 75.5 μM•h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively[1]. |
Protocol (from reference)
References
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Selleck's BMS-582949 has been cited by 13 publications
| ASK1 inhibitor NQDI‑1 decreases oxidative stress and neuroapoptosis via the ASK1/p38 and JNK signaling pathway in early brain injury after subarachnoid hemorrhage in rats [ Mol Med Rep, 2023, 27(2)47] | PubMed: 36633130 |
| Reciprocal priming between receptor tyrosine kinases at recycling endosomes orchestrates cellular signalling outputs [ EMBO J, 2021, e107182] | PubMed: 34086370 |
| The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
| The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] | PubMed: 32645325 |
| Melatonin protects mouse testes from palmitic acid-induced lipotoxicity by attenuating oxidative stress and DNA damage in a SIRT1-dependent manner [ J Pineal Res, 2020, 69(4):e12690] | PubMed: 32761924 |
| Melatonin Protects Mouse Testes from Palmitic Acid-Induced Lipotoxicity by Attenuating Oxidative Stress and DNA Damage in a SIRT1-Dependent Manner [ J Pineal Res, 2020, e12690] | PubMed: 32761924 |
| 5-HT7 Receptor Contributes to Proliferation, Migration and Invasion in NSCLC Cells. [ Onco Targets Ther, 2020, 13:2139-2151] | PubMed: 32210580 |
| Corticosteroids inhibit Mycobacterium tuberculosis-induced necrotic host cell death by abrogating mitochondrial membrane permeability transition. [ Nat Commun, 2019, 10(1):688] | PubMed: 30737374 |
| Curcuminoid WZ35 synergize with cisplatin by inducing ROS production and inhibiting TrxR1 activity in gastric cancer cells. [ J Exp Clin Cancer Res, 2019, 38(1):207] | PubMed: 31113439 |
| Piperlongumine potentiates the antitumor efficacy of oxaliplatin through ROS induction in gastric cancer cells. [ Cell Oncol (Dordr), 2019, 10.1007/s13402-019-00471-x] | PubMed: 31493144 |
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.