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Necrostatin-5 is an inhibitor of necroptosis (non-apoptotic cell death pathway) by indirect inhibition of RIP1 kinase. Necroptosis is defined as alternative active cell death pathway: Death-Domain Receptor (DRs, e.g. Fas/TNFR) mediated and caspase-inhibitor insensitive with specific morphology (nuclear condensation, organelle swelling, loss of plasma membrane integrity). The necrostatins have been discovered to inhibit this pathway by inhibition of the death domain receptor-associated adaptor kinase RIP1. Three distinct mechanisms appear to be involved: T-loop dependent inhibition by necrostatin-1; partially T-loop independent inhibition by necrostatin-3 and indirect inhibition of RIP1 by necrostatin-5, since necrostatin-5 is a potent inhibitor of immunnoprecipitated RIP1, but does not inhibit recombinant RIP1.
| Molecular Weight | 383.49 |
| Formula | C19H17N3O2S2 |
| CAS Number | 337349-54-9 |
| Solubility (25°C) | DMSO 5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related RIPK Products |
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| Necrostatin-1
Necrostatin-1 (NEC-1) is a potent inhibitor of necroptosis, with an EC50 of 490 nM in Jurkat cells. Necrostin-1 is the first identified RIPK1 inhibitor, EC50=182 nM, that reduces inflammation and inhibits colitis associated tumorigenesis. Necrostatin-1 (Nec-1) is also an inhibitor of IDO. |
| GSK481
GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM. |
| GSK583
GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM. |
| WEHI-345
WEHI-345 is a potent and selective RIPK2 inhibitor with IC50 of 0.13 μM. WEHI-345 delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation. |
| GSK872
GSK872 is a receptor interacting protein kinase-3 (RIP3) inhibitor, which inhibits kinase activity with an IC50 of 1.3 nM. |
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