rip1

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).

Nec-4 is a potent inhibitor of receptor interacting protein 1 (RIP1)(IC50 of 2.6 μM),and is a tricyclic derivative.

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

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 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].

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.

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].

TRIP13-IN-1 (compound 20) is a potent ligand and inhibitor of TRIP13, demonstrating anticancer effects both in vivo and in vitro.

Rab8a GTPase-binding stapled peptide (Kd = 12.7 μM). Cell permeable; localizes to the endomembrane system. Cromm et al (2016) Protease-resistant and cell-permeable double-stapled peptides targeting the Rab8a GTPase. ACS Chem.Biol. 11 2375 PMID:27336832

RIPK1-IN-31 (Compound 36) is a selective allosteric modulator of RIPK1 (Receptor Interacting Protein Kinase 1) with an IC50 value of 16 nM. It holds potential for research in areas such as infections, autoimmune disorders, and neurodegenerative diseases.