rip1 kinase

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

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.

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

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).

(E)-Necrosulfonamide ((E)-Necrosulfonamide) is an inhibitor of necroptosis. Blocks mixed lineage kinase domain-like protein (MLKL), a critical substrate of receptor-interacting serine-threonine kinase 3 (RIP3) during necrosis. Prevents MLKL-RIP1-RIP3 necrosome complex from interacting with downstream necrosis effectors. Binds and inhibits gasdermin D. Inhibits pyroptosis.

RIPA-56 is an inhibitor of RIP1

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

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).

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.

Nec-3a, an analogue of Necrostatin-3, acts as a RIP1 inhibitor with an inhibition concentration (IC50) of 0.44 μM. This compound successfully impedes the autophosphorylation activity within the RIP1 kinase domain.

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