RIP kinase

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

Oditrasertib (DNL-788) is a potent RIPKl inhibitor with an IC50 value of less than 100 nM.Oditrasertib can be used for the study of immune and neurological disorders such as multiple sclerosis and Alzheimer's disease.

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.

RIPA-56 is an inhibitor of RIP1

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

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

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).

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

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

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).

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.

GSK2593074A (GSK'074) is a programmed necrosis inhibitor that displays inhibitory effects on RIP1 and RIP3.

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.

GSK2982772 is an inhibitor of receptor interacting serine/threonine kinase 1 (RIPK1)with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.

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.

GSK-843 (GSK'843) is a selective and potent RIP3 inhibitor with an IC50 value of 8.6 nM for the structural domain of RIP3 kinase. It has potential analgesic activity, inhibits the expression of RIP3 and NLRP3 in the SDH of CFA mice, and can be used as adjunctive therapy for treating inflammation.

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

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

Necrostatin 2 is a necrotic protein and receptor-interacting protein kinase 1 (RIPK1) inhibitor used to study inner ear disorders such as sudden deafness, dizziness and tinnitus.

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.

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

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

GSK872 HCl（1346546-69-7 free base） (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).

Cpd27 (TIE-2 VEGFR-2 kinase-IN-2) is a TIE-2 and VEGFR-2 inhibitor that inhibits RIPK1 and protects RGCs from TNF-stimulated cell death and can be used to study glaucoma.

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

Necrostatin-5 (Nec-5) is a selective RIP1 kinase inhibitor and cell necrosis inhibitor that prevents the death of Fadd-deficient Jurkat cells treated with TNF-α, with an EC50 of 240 nM.

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

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

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

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2, demonstrating an IC50 of 1 nM.

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

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.

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).

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.

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].

RIP1 Kinase Inhibitor 4 (Compound 3) is an effective inhibitor of RIP1K, exhibiting an EC50 of ≤ 1000 nM [1].

RIP1 Kinase Inhibitor 7 (Compound 41) serves as a potent inhibitory agent for receptor interacting protein 1 kinase (RIP1) with an IC50 of under 100 nM. Additionally, it demonstrates an EC50 ranging from 1 to 100 nM in cell necrosis assays [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].

SZM-1209 is a potent and specific RIPK1 inhibitor with oral activity, displaying a dissociation constant (Kd) of 85 nM. It demonstrates substantial anti-necroptotic efficacy with an EC50 of 22.4 ± 8.1 nM and possesses therapeutic effects against systemic inflammatory response syndrome (SIRS) and acute lung injury (ALI) [1].

RIP1 kinase inhibitor 5 (example 1) is a potent regulator of tumor immunity, inhibiting RIP1 and similarly to SIR1-365 (compound 13), suppresses necrosis and ferroptosis [2].

SZM679 is an orally active, selective RIPK1 inhibitor displaying potent affinity with a dissociation constant (Kd) of 8.6 nM for RIPK1, while exhibiting minimal activity towards RIPK3, with a Kd of >5000 nM. It effectively counteracts tumor necrosis factor-induced systemic inflammation, reduces Tau hyperphosphorylation, diminishes neuroinflammation, and lowers RIPK1 phosphorylation in the hippocampus and cortex. SZM679 is utilized in Alzheimer’s disease (AD) research [1].

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-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 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].