ripk2

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.

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

cRIPGBM, a proapoptotic derivative of RIPGBM, selectively induces apoptosis in GBM cancer stem cells (CSCs) by targeting receptor-interacting protein kinase 2 (RIPK2), demonstrating an EC50 of 68 nM in GBM-1 cells [1].

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I.

OD36 is a selective and potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 inhibits ALK2 signaling and osteogenic differentiation (KD: 37 nM), and binds efficiently to the ALK2 kinase ATP pocket.

WEHI-345 is a potent and selective RIPK2 inhibitor that modulates NOD signaling events while preventing inflammatory cytokine production.

OD36 hydrochloride (OD-36 hydrochloride) is a potent RIPK2 inhibitor with an IC50 of 5.3 nM.OD36 hydrochloride is a macrocyclic inhibitor that binds efficiently to the ATP pocket of the ALK2 kinase and effectively antagonizes mutant ALK2 signaling and osteogenic differentiation.OD36 hydrochloride targets ALK2. OD36 hydrochloride targets ALK2 with a KD of 37 nM.

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.

Zharp2-1, a RIPK2 inhibitor, inhibits the transcription of inflammatory cytokines induced by MDP-induced or Listeria monocytogenes infection and alleviates MDP-induced peritonitis symptoms in mice, which can be used for the study of inflammatory bowel disease (IBD).

Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, with KDs of 0.2, 0.76, 13, and 1.2 nM for EGFR, HER2, BLK, and RIPK2, respectively, and exhibits anticancer activity.

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.

RIPK2/3 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.

RIPK2/3-IN-2 (29) is a dual inhibitor of RIPK2 and RIPK3, exhibiting IC50 values of 12 nM and 18 nM, respectively. It can induce necroptosis with an EC50 of 0.16 μM.

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-4 is a potent and specific inhibitor of RIPK2 with an IC50 value of 5 nM.

RIPK2-IN-8 is an orally active and highly selective RIPK2 inhibitor with an IC50 of 11 nM. It exhibits greater selectivity for RIPK2 over RIPK1 (IC50 > 30,000 nM) and has moderate inhibitory effects on RIPK3 (IC50 = 44.61 nM). RIPK2-IN-8 exerts anti-inflammatory effects by inhibiting the NOD2-RIPK2 signaling pathway and the expression of inflammatory cytokines IL-6 and TNFα. Additionally, in models of acute liver injury (ALI), RIPK2-IN-8 demonstrates both anti-inflammatory and hepatoprotective effects, making it useful for ALI research.

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.

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].

RIPK-IN-4 is a highly effective and selective small-molecule inhibitor of receptor-interacting protein kinase 2 (RIPK2) that demonstrates potent biochemical activity with an IC50 value of 3 nM, and it is further distinguished by excellent oral bioavailability, making it a valuable research tool for investigating RIPK2-mediated signaling pathways, innate immune responses, and inflammatory disease mechanisms in both in vitro and in vivo experimental systems.

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-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.

CSLP37 is a selective RIPK2 inhibitor with an IC50 of 16.3 nM and demonstrates no inhibitory activity against RIPK1 or RIPK3. Additionally, CSLP37 effectively suppresses cellular responses mediated by NOD1 and NOD2.

RIP2 Kinase Inhibitor 4 is a highly potent and selective RIPK2 PROTAC compound that efficiently degrades RIPK2 (pIC50 value of 8) and effectively inhibits the release of TNF-α.