ripk

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].

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

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

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.

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-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.

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].

RIPK2-IN-3 (FCG806791773) is a receptor-interacting protein kinase 2 (RIPK2) inhibitor with an IC50 of 6.39 μM against recombinant truncated RIPK2, applicable for studying inflammation and cancer [1].

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

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-19 (compound 10b), a selective RIPK1 inhibitor (IC50 = 15 nM), demonstrates significant protective activity in TNFα-induced systemic inflammatory response syndrome (SIRS) and Imiquimod (IMQ)-induced psoriasis models. This compound is suitable for research on inflammation and immune system diseases [1].

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.

RIPK1-IN-18 sulfate hydrate, a potent RIPK1 inhibitor, is suitable for autoimmune disease research (NZ748385A; compound i) [1].

RIPK1 3-IN-1 (Compound 10) is a selective inhibitor of RIPK1 and RIPK3, effectively preventing necroptosis by blocking the phosphorylation of RIPK1, RIPK3, and MLKL [1].

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage. It alleviates acute kidney injury by attenuating Cisplatin- and I R-induced kidney damage, along with associated inflammatory responses and necroptosis [1].

RIPK1-IN-8 is an aminoimidazolopyridine and is a selective and potent inhibitor of RIPK1 (IC50: 4 nM).RIPK1-IN-8 has research potential in inflammatory diseases.

RIPK2-IN-5 is a receptor-interacting protein kinase 2 (RIPK2) inhibitor with potential anti-inflammatory activity for the study of diseases caused by immune dysfunctions.

RIPK2-IN-2 (example 25) is a RIP2 kinase PROTAC inhibitor that effectively blocks RIP2-dependent pro-inflammatory signaling and regulates RIP2 kinase activity in autoinflammatory diseases [1].

RIPK1-IN-21 (Compound I-5), an inhibitor of RIPK1, manifests a potent EC 50 value of 14.8 nM. It is primarily utilized in researching neurodegenerative, autoimmune, and inflammatory diseases [1].

RIPK2 3-IN-1 is a potent inhibitor of both RIPK2 and RIPK3 kinases, exhibiting IC50 values of 3 nM for RIPK2 and 117 nM for RIPK3. Additionally, in a 14-TriLAN-Gly NOD1 THP-1 cell-based NF-κB reporter assay, RIPK2 3-IN-1 demonstrates an IC50 value of 14 ± 4 nM against RIPK2 [1].

RIPK2-IN-1 (compound 18f) is a potent inhibitor of RIPK2 with an IC50 of 51 nM, and also inhibits ALK2 with an IC50 of 5 nM.

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.

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

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

Necroptosis-IN-1 is a potent necroptosis inhibitor of RIPK1. It is an analog of Necrostatin-1.

GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor that binds to the RIP3 kinase domain (IC50: 0.9 nM) and inhibits kinase activity (IC50: 0.3 nM).

GSK-872 (GSK2399872A) is an effective and specific RIP3 kinase inhibitor. It binds RIP3 kinase domain with high affinity (IC50: 1.8 nM) and inhibits kinase activity (IC50: 1.3 nM).

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

RIPA-56 is an inhibitor of RIP1

ICCB-19 hydrochloride (ICCB-19 HCl) is an inhibitor of TRADD (TNFRSF1A Associated Via Death Domain). It binds to a pocket on the N-terminal TRAF2-binding domain of TRADD (TRADD-N), which interacts with the C-terminal domain (TRADD-C) and TRAF2 to modulate the ubiquitination of RIPK1 and beclin 1.

Necrostatin 2 racemate (Necrostatin-2 racemate) is an potent and specific inhibitor of RIPK1.

Necrostatin-34 (2-{[3-cyano-4-(4-methylphenyl)-6-oxo-1,4) is a RIPK1 kinase inhibitor, stabilizing RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain.

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

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

Eclitasertib is a potent inhibitor of receptor-interacting protein kinase 1 (RIPK1, IC50 of <1 µΜ).

GSK583 is a highly effective and specific RIP2 kinase inhibitor (IC50: 5 nM).

GSK3145095 is an orally active inhibitor of RIPK1 with IC50 of 5 nM, with potential immunomodulatory activities and antineoplastic.

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

GSK963 (Racemate), a structurally distinct, potent and selective inhibitor of RIP1 kinase(IC50=29 nM).

Apostatin-1 (Apt-1) is a novel TRADD inhibitor that binds to a pocket on the N-terminal TRAF2 binding domain of TRADD.

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.