Necroptosis
Necroptosis is a caspase-independent form of programmed cell death. It is involved in the pathology of many diseases involving cell death and inflammation. Necroptosis can be triggered by myriad signals including TNFα, TRAIL, TWEAK, genotoxic stress, PAMPS (pathogen-associated molecular patterns), and caspase 8 inhibition. The necroptotic signalling pathway begins with activation of Receptor-Interacting Protein 1(RIP1) kinase. In the absence of caspase 8 signalling, RIPK1 and RIPK3 form the necrosome (or complex IIb). This complex recruits mixed-lineage kinase domain-like protein (MLKL), which is phosphorylated by RIPK3. MLKL translocates to the plasma and cytoplasmic membranes starting the necroptotic process.
7-Cl-O-Necl
Necrostatin-1 analogue with superior potency (IC50 = 206nM vs 494nM), selectivity and metabolic stability in blocking RIP1.7-Cl-O-Nec1 shows no off-target inhibition of indolamine-2,3-deoxygenase (IDO) in contrast to Necrostatin-1 (Nec-1).7-Cl-O-Nec1 showed higher activity in inhibiting necroptosis in Jurkat cells than Necrostatin-1 (EC50 = 210 nM vs. EC50 = 490 nM), no non-specific cytotoxicity at high concentrations (100 µM) and reasonable pharmacokinetic characteristics when used in mice.7-Cl-O-Nec1 is recommended for cellular and in vivo use over Necrostatin-1.
Product Base Number: 10-4544 Size: 5mg Size: 25mg
RIPA-56
IPA-56 is a potent (IC50 = 13 nM, EC50 = 28nM for HT-29 cells) and selective inhibitor of Receptor-Interacting Protein 1 (RIP1) kinase with significant metabolic stability (t1/2 = 128min human liver microsomal stability assay). RIPA-56 showed excellent kinase selectivity and did not inhibit IDO at 200 µM.
Product Base Number: 10-4611 Size: 10mg Size: 50mg
GSK872
GSK872 is a potent (IC50 = 1.3 nM) and selective inhibitor of Receptor-Interacting Protein 3 (RIP3). It is able to block virus-induced and TLR3-induced necrosis.
Product Base Number: 10-4861 Size: 5mg Size: 25mg
Dabrafenib
SK872 is a potent (IC50 = 1.3 nM) and selective inhibitor of Receptor-Interacting Protein 3 (RIP3). It is able to block virus-induced and TLR3-induced necrosis.
Product Base Number: 10-1569 Size: 5mg Size: 25mg
Necrosulfonamide
Nerosulfonamide is an inhibitor (IC50 <200 nM) of human mixed lineage kinase domain-like protein (MLKL). It is able to block necroptosis downstream of RIP3 activation.12 MLKL has been found to be critical to the execution of necroptosis.