rip 1

RIP1 kinase inhibitor 1 is an orally available and brain-penetrating inhibitor of RIP1 kinase with pKi of 9.04.

RIP1 kinase inhibitor 9 (compound SY-1) is a selective inhibitor of RIP kinase. It effectively reduces central inflammatory responses caused by seizures. RIP1 kinase inhibitor 9 also obstructs Z-VAD-FMK-induced necroptosis in HT-29 cells, with an EC50 of 7.04 nM.

RIP1-IN-1 is an orally bioavailable RIP1 inhibitor with a high binding affinity (Kd: 110 nM). This compound exhibits significant activity against necroptosis and effectively suppresses necrosome formation by inhibiting the phosphorylation of RIP1, RIP3, and MLKL pathways. RIP1-IN-1 can inhibit necroptosis and is applicable in research on acute liver injury.

RIP1 Kinase Inhibitor 4 (Compound 3) is an effective inhibitor of RIP1K, exhibiting an EC50 of ≤ 1000 nM [1].

RIP1 kinase inhibitor 5 (example 1) is a potent regulator of tumor immunity, inhibiting RIP1 and similarly to SIR1-365 (compound 13), suppresses necrosis and ferroptosis [2].

RIP1 Kinase Inhibitor 6 is a potent and selective inhibitor of RIP1 kinase, demonstrating inhibitory activity with an IC50 of less than 100 nM in a human R1P1 kinase assay[1].

RIP1 Kinase Inhibitor 7 (Compound 41) serves as a potent inhibitory agent for receptor interacting protein 1 kinase (RIP1) with an IC50 of under 100 nM. Additionally, it demonstrates an EC50 ranging from 1 to 100 nM in cell necrosis assays [1].

RIP1 Kinase Inhibitor 8 (Compound 77), a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor, exhibits an IC50 of 20 nM and effectively prevents necrotic cell death. It also demonstrates a favorable pharmacokinetic profile across multiple species [1].

Necrostatin-1 (Nec-1) is a specific RIP1 inhibitor and necrotic apoptosis inhibitor, which inhibits TNF-α-induced necrotic apoptosis and also inhibits IDO.

Necrostatin-5 (Nec-5) is a selective RIP1 kinase inhibitor and cell necrosis inhibitor that prevents the death of Fadd-deficient Jurkat cells treated with TNF-α, with an EC50 of 240 nM.

RIPK1-IN-4 is a potent and selective type II kinase receptor interacting protein 1 (RIP1) kinase inhibitor and binds to a DLG-out inactive form of RIP1 (IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase).

GSK2593074A (GSK'074) is a programmed necrosis inhibitor that displays inhibitory effects on RIP1 and RIP3.

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.

GSK583 is a highly effective and specific RIP2 kinase inhibitor (IC50: 5 nM).

GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).

GSK481 (GSK'481) is a RIP1(Receptor Interacting Protein Kinase1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.

GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1)with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.

GSK547 (GSK'547) is a highly selective and potent RIP1 kinase inhibitor that disrupts macrophage-mediated adaptive immune tolerance in pancreatic cancer.

RIPA-56 is an inhibitor of RIP1

GNE684 is a potent inhibitor of receptor interacting protein 1 (RIP1) with average Ki app values of 21 nM for human, 189 nM for mouse, and 691 nM for rat RIP1, respectively [1].

RIP2 kinase inhibitor 1 is a potent and selective receptor interacting inhibitor of protein 2 (RIP2) kinase(RIP2 FP with an IC50 of 0.03 μM ),and is used for autoinflammatory disorders.

RIP3 Activator 1 (compound C8) is an effective RIP3 activator that inhibits cell growth and induces necroptotic cell death (necroptosis) and autophagy through the RIP3/p62/Keap1 signaling pathway. Additionally, this compound enhances the expression of p-MLKL and promotes the accumulation of LC3-II and p62 proteins.

ZBP1/RIP3/MLKL activator 1 (compound 3a) is a synthesized quinoline derivative that can induce DNA damage, elevate intracellular reactive oxygen species (ROS) levels, and trigger apoptosis through the caspase pathway. Furthermore, when apoptosis is inhibited, it facilitates necroptosis via the ZBP1-RIP3-MLKL pathway. This compound is useful in cancer research, particularly for targeting cells with impaired apoptotic mechanisms.

DCZ0415 induces antimyeloma activity in vitro, in vivo and in primary cells of drug-resistant myeloma patients. DCZ0415 is a potent TRIP13 inhibitor that can impair the repair of non-homologous end junctions and inhibit NF-κB activity.