RIP Kinase

Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).

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.

GSK583 is a highly potent and selective inhibitor of RIP2 Kinase.

RIP2 kinase inhibitor 1 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.

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.