ripk

RIPK1-IN-7 is a potent and selective inhibitor of RIPK1 (Kd of 4 nM and enzymatic IC50 of 11 nM), exhibiting excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.

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

PK68 is an effective and selective inhibitor of type II receptor-interacting kinase 1 (RIPK1, IC50 = 90 nM). PK68 can be used for research on the treatment of inflammatory disorders and cancer metastasis.

RIPA-56 is an inhibitor of RIP1

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM).

PROTAC RIPK degrader-6 (example 1) is a PROTAC engineered for RIP Kinase degradation, comprising a RIP2 kinase inhibitor linked to a cereblon binder[1].

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).

RIPK1-IN-9 is a potent and selective inhibitor of RIPK1, a dihydronaphthone compound, which inhibits U937 and L929 cells with an IC50 of 2 nM and 1.3 nM, respectively.

RIPK2-IN-3 (FCG806791773) is a receptor-interacting serine threonine protein kinase 2 (RIPK2) inhibitor with anti-inflammatory and anti-tumor activity. It can be used for research on immune diseases and cancer.

RIPK1-IN-3 is a RIPK1 inhibitor, with anti-inflammatory proprieties.

RIPK2-IN-6 (Compound 15a) is an inhibitor of RIPK that specifically targets the phosphorylation of RIPK2, thereby suppressing the NF-κB and MAPK signaling pathways. It has demonstrated anti-inflammatory and anti-fibrotic activities in a mouse model of colitis induced by Dextran sodium sulfate.

RIPK1-IN-18 (compound i) serves as a potent inhibitor of RIPK 1 and has applications in the research of autoimmune diseases [1].

RIPK1-IN-25 (WL8) is a RIPK1 inhibitor with blood-brain barrier permeability, displaying an EC50 of 19.9 nM and a Kd of 25 nM. It is utilized in the research of neurodegenerative diseases.

RIPK1-IN-24 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an IC50 of 1.3 μM. It is utilized in research on inflammatory diseases.

RIPK1-IN-26 is a potent inhibitor of Receptor-Interacting Serine Threonine Kinase 1 (RIPK1), exhibiting anti-necrotic properties in cells. This compound demonstrates good metabolic stability and binding specificity in mice. RIPK1-IN-26 holds potential for development as a PET imaging probe and in the research of neurodegenerative diseases.

RIPK1-IN-27 (compound 19) is an inhibitor of RIPK1.

NOD1-RIPK2-IN-1 (Compound 37) is an inhibitor of the NOD1-RIPK2 signaling pathway, displaying potent IC50 values of 42 nM and 1.52 nM against NOD1 and RIPK2, respectively. This compound effectively reduces the secretion of the pro-inflammatory cytokine IL-8, making it valuable for research in inflammation and immune disorders.

RIPK2 3 inhibitor 29 (compound 29) is a dual inhibitor of RIPK2 (IC50=12 nM) and RIPK3 (IC50=18 nM), which can directly bind to RIPK2 and RIPK3, effectively inhibiting NOD induced cytokine production and cell necrosis. Compound 29 has shown significant therapeutic effects in DSS induced colitis mouse models and has broad potential for dual inhibition of RIPK2 RIPK3 in the treatment of IBD.

The IC50 value of RIPK2 IN 10W for RIPK2 is 0.6 nM, which is more than 50000 times higher than RIPK1 (IC50>30 μ M). RIPK2 IN 10W has high kinase selectivity, inhibits RIPK2, and prevents NOD induced cytokine production after stimulation with muramyl dipeptide (MDP). RIPK2 as a therapeutic target has shown potential in treating inflammatory bowel disease.

RIPK1-IN-28 (compound 13) is an orally active inhibitor of RIPK1. It exhibits inhibitory effects on human I2.1 and Hepa1-6 cells, with IC50 values of 0.4 and 1.2 nM, respectively.

RIPK1-IN-15 (Compound 2.5) is a potent RIPK1 inhibitor with potential applications in research on neurodegenerative, autoimmune, and inflammatory diseases [1].

RIPK1-IN-13 (Compound 8) is an effective RIPK1 inhibitor (IC50=1139 nM) that can block the activation of the necrotic apoptosis pathway, holding research potential in inflammatory diseases.

RIPK1-IN-14 (Compound 41) is a potent RIPK1 inhibitor (IC50: 92 nM) with significant anti-necrotic apoptotic effects in a necrotic apoptosis model using U937 cells.