ripk 1

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-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.

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

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-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-29 (Compound 22) is a RIPK1 inhibitor with an IC50 of 6.9 nM. It exhibits anti-necroptotic apoptosis activity by inhibiting RIPK1. In a TNF-α induced inflammatory in vivo model, a 10 mg/kg dose of RIPK1-IN-29 can protect mice from hypothermia and death. This compound is suitable for research in the field of inflammatory diseases.

RIPK1-IN-30 (compound 24) is a potent RIPK1 inhibitor with an IC50 of 2.01 μM. It demonstrates a protective effect in the HT-29 cell model of TSZ-induced necroptosis, with an EC50 of 6.77 μM.

RIPK1-IN-20 has strong RIPK1 kinase inhibitory activity with an IC50 value of 59.8 nM. It can block TNFα-induced necroptosis in both human and mouse cells, with an EC50 ranging from 1.06 to 4.58 nM.

RIPK1-IN-23 (compound 19) is an RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC50 = 1.7 nM). Additionally, RIPK1-IN-23 exhibits anti-inflammatory properties.

RIPK1-IN-13 (compound 28) is a selective inhibitor of receptor-interacting serine/threonine-protein kinase 1 (RIPK1), showing a pKi of 7.66 as measured by the ADP-Glo kinase assay. It exhibits inhibitory effects in human leukemia U937 cells with a pIC50 of 7.2.

RIPK1-IN-31 (Compound 36) is a selective allosteric modulator of RIPK1 (Receptor Interacting Protein Kinase 1) with an IC50 value of 16 nM. It holds potential for research in areas such as infections, autoimmune disorders, and neurodegenerative diseases.

RIPK1-IN-32 is an RIPK inhibitor with anti-inflammatory properties. It inhibits nitric oxide (NO) release, with an IC50 of 3.26 μM. Additionally, RIPK1-IN-32 disrupts the RIPK1/NF-κB/MAPK signaling pathway, preventing nuclear translocation of p65 and c-fos, leading to reduced expression of TNF-α and IL-6 and significantly alleviating acute liver injury related to sepsis. This compound is useful for studies on acute liver injury and sepsis.

RIPK1-IN-33 is an orally active RIPK1 inhibitor with excellent blood-brain barrier permeability, exhibiting an IC50 of 0.115 μM. It demonstrates significant anti-ferroptosis activity, radical scavenging capability (IC50= 123.3 μM), and anti-lipid peroxidation effects (IC50= 9.72 μM). In transient middle cerebral artery occlusion (tMCAO) models, it significantly reduces cerebral infarct volume and improves neurological scores. RIPK1-IN-33 is suitable for ischemic stroke research.

RIPK1-ligand-2 is an inhibitor of RIPK1, and it can be used in the synthesis of PROTAC[RIPK1]Degrader-1.

PROTACRIPK1Degrader-1 is a selective RIPK1 PROTAC degrader. This compound degrades RIPK1 in various cancer cell lines, such as A375 and B16F10 cells. It enhances the anticancer effects of radiotherapy in both syngeneic and humanized mouse models. PROTACRIPK1Degrader-1 is applicable for research in cancers like melanoma.

RIPK1ligand-Linker Conjugate-1 is a Target Protein Ligand-Linker Conjugate that consists of a RIPK1 ligand and a PROTAC linker, designed to recruit E3 ligase. It is utilized in the synthesis of PROTACRIPK1Degrader-1.

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.

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.

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.