RIP kinase Inhibitor

Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC₅₀ of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC₅₀=182 nM). Necrostatin-1 is also an IDO inhibitor.

GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC₅₀ of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC₅₀ value of 200 nM.

Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.

Primidone (Standard) is the analytical standard of Primidone. This product is intended for research and analytical applications. Primidone is the orally active inhibitor for TRPM3 (IC₅₀ = 0.6 μM), RIP kinase and voltage-gated sodium channel, and the antagonist for GABA receptor. Primidone can be used as the analgesic and anticonvulsant agent.

RIPK3-IN-7 is a RIPK3 inhibitor that suppresses the RIPK3-mediated necroptosis pathway. RIPK3-IN-7 can be used for research on necroptosis and inflammation-related diseases.

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.

RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC₅₀ of 13 nM. RIPA-56 can be used for the treatment of systemic inflammatory response syndrome.

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.

CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC₅₀ values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease.

Ponicidin (Rubescensine B) is an orally active RIPK1 inhibitor with a K_d value of 135 nM. Ponicidin inhibits the JAK2/STAT3 pathway to induce apoptosis, activates the PI3K/Akt pathway, upregulates SIRT1 expression, alleviates oxidative stress, suppresses inflammatory responses and necroptosis, and blocks cell cycle progression. Ponicidin induces ROS production to exert antiproliferative and antiviral effects, while also improving cognitive function and reducing Aβ plaque deposition. Ponicidin can be used in studies related to hepatocellular carcinoma, Alzheimer's disease, and gastric cancer.

GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.

GSK2593074A (GSK’074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.

HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC₅₀ of 20.8 nM.

RIPK2-IN-5 (compound 14) is a high affinity and excellent selectivity RIPK2 inhibitor with an IC₅₀ value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases.

RIPK1-IN-7 is a potent and selective RIPK1 inhibitor with a K_d 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.

Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis.

GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC₅₀ of 1.3 nM, which inhibits Ser¹⁶⁶ phosphorylation in wild-type human RIP1 (IC₅₀=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC₅₀ of 10 nM.

RIPK1 Human Pre-designed siRNA Set A contains three designed siRNAs for RIPK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC₅₀=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion.

TP-030-2, a chemical probe, is a RIPK1 inhibitor (human K_i=0.43 nM; mouse IC₅₀=100 nM).