Chemical Structure : BAL-0598
货号: PC-25460Not For Human Use, Lab Use Only.
BAL-0598 is a potent and selective, non-covalent inhibitor of human NLRP3, binds NLRP3 NACHT with a steady-state KD of 193 nM in SPR assays.
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BAL-0598 is a potent and selective, non-covalent inhibitor of human NLRP3, binds NLRP3 NACHT with a steady-state KD of 193 nM in SPR assays.
BAL-0598 inhibits LPS and nigericin-induced NLRP3 signaling in a range of human cell types, including THP-1, monocytes, iMacs, and HMDM.
BAL-0598 also inhibits NLRP3 activation by stimuli such as MSU and prevents NLRP3-dependent ASC speck formation.
BAL-0598 does not inhibit NLRP3 activation in mouse macrophages.
BAL-0598 inhibit NLRP3 activation in mouse macrophages expressing human NLRP3 in a nanomolar range.
BAL-0598 has IC50 of 63.9 nM in IL-1β release assay from PMA-differentiated THP-1 cells.
BAL-0598 reduces the IL-1β response in mice model of peritonitis with ED50 of 28.6 mg/kg.
BAL-0598 inhibits disease-associated NLRP3 mutations, potently inhibits A352V, K565E, E567G, K568N, and G569R at levels similar to WT NLRP3.
分子量 | 434.47 | |
分子式 | C24H23FN4O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Wilhelmsen K, et al. Discovery of potent and selective inhibitors of human NLRP3 with a novel mechanism of action. J Exp Med. 2025 Nov 3;222(11):e20242403.
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