Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
RIP kinase inhibitors act on receptor-interacting protein kinases (RIPKs), mainly RIPK1, RIPK2 and RIPK3. RIPK1 and RIPK3 control necroptosis, a regulated form of necrosis triggered by tumor necrosis factor alpha (TNF-α) and other death receptor signals. Necrostatin-1 was described in 2005 as an inhibitor of nonapoptotic cell death, and RIPK1 was identified as its cellular target in 2008. A 2009 study showed that RIPK3 determines whether cells die by necrosis in response to TNF-α. GSK481 and PK68 are further RIPK1 inhibitors, and GSK-843 inhibits RIPK3. GSK583 inhibits RIPK2, which relays signals from the bacterial sensors nucleotide-binding oligomerization domain-containing proteins 1 and 2 (NOD1, NOD2).
Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).
Necrosulfonamide is a pharmacological inhibitor of MLKL with IC50 values of 124 nM in human HT-29.
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.
GSK481 is a novel benzoxazepinone (BOAz) series of RIP1 inhibitors. Receptor Interacting Protein Kinase 1 (RIP1) has been implicated as a key contributor to inflammation through the regulation of programmed necrosis. Inhibition of this kinase has been shown to hinder cell necrotic death, thereby establishing RIP1 as a viable target for the potential treatment of multiple inflammatory diseases.
Synonyms: GSK 074
GSK2593074A (GSK??074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.
GSK583 is a highly potent and selective inhibitor of RIP2 Kinase.
GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
RIP2 kinase inhibitor 2 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043437 A1, compound example 9.
GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.
GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM.
PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis.
HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM.
RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a Kd of 4 nM and an enzymatic IC50 of 11 nM. RIPK1-IN-7 exhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
RIPK1-IN-3 (Example 38), a RIPK1 inhibitor, extracted from patent WO2018148626A1, possesses anti-inflammatory proprieties.
GSK547 (GSK-547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.
GSK3145095 is a RIP1 kinase inhibitor with an IC50 of 6.3 nM .
RIPK-IN-4 is a potent and selective RIPK2 inhibitor with excellent oral bioavailability, and has an IC50 of 3 nM.
GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM.
RIP2 Kinase Inhibitor 3 is a highly potent and selective inhibitor of receptor interacting protein-2 (RIP2) Kinase with an IC50 of 1 nM .
RIP1 kinase inhibitor 1 (compound 22) is a highly potent, orally available, and brain-penetrating RIP1 kinase inhibitor (pKi=9.04).
WEHI-345 is a potent and selective RIPK2 kinase inhibitor with an IC50 of 0.13 μM, which delays RIPK2 ubiquitylation and NF-κB activation on oligomerization domain (NOD) stimulation.
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase.
Nec-4, a tricyclic derivative, is a potent receptor interacting protein 1 (RIP1) inhibitor, with an IC50 of 2.6 μM, Ki of 0.46 μM.
GSK2983559 free acid (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor.
