RIP kinase

Necrostatin-1 (Nec-1) is a necrotic apoptosis inhibitor and RIP1 inhibitor with specificity. Necrostatin-1 inhibits TNF-α-induced necrotic apoptosis. Necrostatin-1 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.

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.

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

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

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

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

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

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.GSK-843 has potential analgesic activity, inhibits the expression of RIP3 and NLRP3 in the SDH of CFA mice, and can be used as an adjunctive therapy for the treatment of inflammation.

RIP2 Kinase Inhibitor 3 is a potent and selective inhibitor of RIP2 with an IC50 of 1 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).

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.

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

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.

RIPA-56 is an inhibitor of RIP1

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

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.

RIPK1/3-IN-1 (Compound 10) is a selective inhibitor of both 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-16 is an orally active, potent RIPK1 inhibitor that mitigates excessive inflammation via inhibition of RIPK1-mediated necroptosis in vivo. It shields mice from TNF-induced systemic inflammatory response syndrome and sepsis [1].

RIPK2-IN-3 (FCG806791773) is a receptor-interacting protein kinase 2 (RIPK2) inhibitor with an IC50 value of 6.39 μM against recombinant truncated RIPK2. It is applicable in the study of inflammation and cancer [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.

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

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

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].

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

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

RIPK1-IN-7 is a potent and selective inhibitor of RIPK1(Kd of 4 nM and an enzymatic IC50 of 11 nM),andexhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.

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

RIP1 kinase inhibitor 5 (example 1) serves as a potent regulator of tumor immunity by inhibiting RIP1, functioning similarly to SIR1-365 (compound 13) in suppressing necrosis and ferroptosis [2].

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].

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].

WEHI-345 is a potent and selective RIPK2 inhibitor which shows NOD signalling events yet prevents inflammatory cytokine production.

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

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.

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).

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.

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.

RIP1 Kinase Inhibitor 6 is a potent and selective inhibitor of RIP1 kinase, demonstrating inhibitory activity with an IC50 of less than 100 nM in a human R1P1 kinase assay[1].

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).

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

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.

RI-962 is a potent and selective inhibitor of receptor-interacting protein kinase 1 (RIPK1), exhibiting an IC50 of 35.0 nM. It is utilized for the investigation of nervous system disorders and inflammatory diseases [1].

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.

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

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.