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.

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].

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).

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.

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

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.

RIPK3-IN-1 is a selective and potent RIPK3 inhibitor (IC50: 9.1 nM) that inhibits the activities of c-Met kinase, RIPK1 and RIPK2.RIPK3-IN-1 has potential tumorigenic activity and can be used to study apoptosis.

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-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-19 is a selective and potent bimodal RIPK1 inhibitor with IC50=15 nM that protects against cell necrosis and works well in the tnf α-induced Systemic Inflammatory Response Syndrome (SIRS) model and imiquimod (IMQ)-induced psoriasis model.

RIPK3-IN-3 (compound 20) is a selective RIPK3 inhibitor with a potent IC50 value of 10 nM, effectively blocking RIPK3-mediated phosphorylation of MLKL, preventing oligomerization and necroptosis induction. Moreover, RIPK3-IN-3 suppresses CXCL5 secretion and impedes AsPC-1 cell migration and invasion [1].

RIPK1-IN-11 is an orally active RIPK1 inhibitor with a Kd value of 9.2 nM and an IC50 value of 67 nM. RIPK1-IN-11 inhibits necrosis in human and mouse cells and exhibits anti-inflammatory effects.

RIPK1-IN-10 is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1).

RIPK1-IN-16 is an orally active, potent RIPK1 inhibitor that mitigates excessive inflammation via inhibition of RIPK1-mediated necroptosis in vivo, protecting mice from TNF-induced systemic inflammatory response syndrome and sepsis [1].

RIPK1-IN-12 is a potent inhibitor of RIPK1, exhibiting an inhibitory effect on necroptosis in human and mouse cells with EC50 values of 1.6 and 2.9 nM, respectively.

RIPK3-IN-2, a RIP3 inhibitor, is utilized in studies of diseases caused by or associated with activated necrotic pathways.

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.