Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 uM. It specifically blocks necrosis downstream of receptor-interacting serine-threonine kinase 3 (RIP3) activation. RIP3 is a key signaling molecule in the programmed necrosis pathway. Treating cells with NSA arrested necrosis at a specific step at which RIP3 formed discrete punctae in cells.
Different from Necrostatin-1, NSA does not inhibit the necrosis-induced RIP1 and RIP3 interactions. NSA targets MLKL, a critical substrate of RIP3 during induction of necrosis. It binds the N-terminal of MLKL, covalently modifies Cys86 of human MLKL, and prevents necrosome from interacting with its downstream effectors.
Technical information:
Chemical Formula: | C18H15N5O6S2 | |
CAS #: | 432531-71-0 | |
Molecular Weight: | 461.47 | |
Purity: | >96% | |
Appearance: | Light yellow solid | |
Chemical Name: | (E)-N-[4-[N-(3-methoxypyrazin-2-yl)sulfamoyl]phenyl]-3-(5-nitrothiophene-2-yl)acrylamide | |
Solubility: | Up to 50 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Sun L., et al. Mixed Lineage Kinase Domain-like Protein Mediates Necrosis Signaling Downstream of RIP3 Kinase. Cell (2012), 148(1):213-227. |
2. | Wang Z., et al. The mitochondrial phosphatase PGAM5 functions at the convergence point of multiple necrotic death pathways. Cell (2012), 148(1):228-243 |
Other Information:
Product Specification (pdf)
MSDS (pdf)