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RIP1 kinase inhibitor 9 (compound SY-1) is a selective RIPkinase inhibitor. RIP1 kinase inhibitor 9 effectively suppresses the central inflammatory response induced by epilepsy. RIP1 kinase inhibitor 9 inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis in HT-29 cells with an EC50 of 7.04 nM .
RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2)kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders .
RIP1 kinase inhibitor 7 (compound 41) is a potent receptor interacting protein 1 kinase(RIP1) Inhibitor with an IC50 of <100 nM for human RIP1. RIP1 kinase inhibitor 7 has an EC50 of 1-100 nM in the cell necrosis assay .
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species .
RIP1 kinase inhibitor 6 is a potent and selective RIP1kinase inhibitor with an IC50 of < 100 nM in human R1P1 kinase assay. RIP1 kinase inhibitor 6 is extracted from patent WO2020103884, example 80 .
RIP1 kinase inhibitor 4 (Example 3) is a BBB-penetrable RIP1 kinase inhibitor (EC50: <100 nM). RIP1 kinase inhibitor 4 can be used for the research of cell programming necrosis-related diseases . RIP1 kinase inhibitor 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
RIP1 kinase inhibitor 5 (example 1) is a potent inhibitor of RIP1, which is used as a checkpoint kinase to control tumor immunity . RIP1 kinase inhibitor 5 is similar with SIR1-365 (compound 13), which inhibits necrosis and iron death activity .
RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α .
RIPK2-IN-2 (example 25) is a RIP2 kinasePROTAC inhibitor. RIPK2-IN-2 can block RIP2-dependent proinflammatory signaling, regulated RIP2 kinase activity in auto inflammatory diseases .
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1)kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase .
PROTAC RIPK degrader-6 (example 1) is a Cereblon-based PROTAC targeting RIPKinase degradation wherein the RIP2 kinase inhibitor is linked via a linker to a cereblon binder .
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM .
Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
GSK2982772 is a potent, orally active and ATP competitive RIP1kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
GSK-843 (GSK'843) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 8.6 nM, and inhibits kinase activity with an IC50 of 6.5 nM. GSK-843 can be used for the research of inflammation .
Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
(E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
Nec-3a is a Necrostatin-3 analogue. Nec-3a is a RIP1 inhibitor (IC50: 0.44 μM). Nec-3a inhibits the autophosphorylation activity of the RIP1 kinase domain .
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM .
GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro .
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
GSK2983559 is an orally active and potent receptor interacting protein 2(RIP2)kinase inhibitor. GSK2983559 blocks many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples .
(Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer .
GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2)kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.
Necroptosis-IN-4, a potent necroptosis inhibitor, is a RIPkinase 1 (RIPK1) inhibitor. Necroptosis-IN-4 has no inhibitory activity against RIPK3 and weak inhibitory activity against VEGFR1/2 and PDGFR-α .
GSK2983559 free acid (compound 3) is an orally active and potent receptor interacting protein 2(RIP2)kinase inhibitor. GSK2983559 free acid can block many proinflammatory cytokine responses in vivo and in human inflammatory bowel disease explant samples .
Necrostatin-1 (Nec-1) is a potent and cross the blood-brain barrier necroptosis inhibitor with an EC50 of 490 nM in Jurkat cells. Necrostatin-1 inhibits RIP1 kinase (EC50=182 nM). Necrostatin-1 is also an IDO inhibitor .
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity .
Tomatine hydrochloride is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine hydrochloride elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine hydrochloride promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine hydrochloride also inhibits 20S proteasome activity .
GSK-872 is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury .
GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury .
RIPK3-IN-3 (compound 20) is a selective inhibitor of RIPkinase RIPK3 (IC50=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion .
GSK223 is a quinazolinone NOD1 pathway inhibitor with potential anti-inflammatory activity. GSK223 can selectively inhibit IL-8 release under iE-DAP stimulation without affecting IL-8 secretion caused by TNF receptor, TLR2 or NOD2 agonists. GSK223 does not directly inhibit RIP2 kinase activity.
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity .
RIPK3 is a kinase that controls necroptosis and apoptosis. In necroptosis, activated by TNF-α and ZBP1, RIPK3 phosphorylates MLKL, leading to membrane damage. RIPK3 Protein, Human (P.pastoris, His) is the recombinant human-derived RIPK3 protein, expressed by P. pastoris , with N-6*His labeled tag.
RIPK3 Protein, participates in programmed necrosis (necroptosis) and apoptosis, contributing to diverse cellular processes. RIPK3 Protein, Mouse (P.pastoris, His) is the recombinant mouse-derived RIPK3 protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of RIPK3 Protein, Mouse (P.pastoris, His) is 486 a.a., with molecular weight of ~64 kDa.
RIPK2 is a multifunctional serine/threonine/tyrosine protein kinase that coordinates innate and adaptive immune responses. It is activated by bacterial peptidoglycan to form filaments in the NOD1 and NOD2 pathways, undergoing autophosphorylation and polyubiquitination. RIPK2 Protein, Human (P. pastoris, His) is the recombinant human-derived RIPK2 protein, expressed by P. pastoris , with C-6*His, C-6*His labeled tag. The total length of RIPK2 Protein, Human (P. pastoris, His) is 540 a.a., with molecular weight of 66 kDa.
RIPK1 protein is a serine-threonine kinase that centrally regulates TNF-mediated apoptosis, necroptosis, and inflammatory pathways. Functionally, it plays a kinase-dependent role in the regulation of cell death and a kinase-independent scaffolding function in the control of inflammatory signaling and cell survival.
RIPK1 protein is a serine-threonine kinase that centrally regulates TNF-mediated apoptosis, necroptosis, and inflammatory pathways. Functionally, it plays a kinase-dependent role in the regulation of cell death and a kinase-independent scaffolding function in the control of inflammatory signaling and cell survival. RIPK1 Protein, Human (Sf9, His, GST) is the recombinant human-derived RIPK1 protein, expressed by Sf9 insect cells , with N-8*His, N-GST labeled tag. The total length of RIPK1 Protein, Human (Sf9, His, GST) is 327 a.a., .
Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide. Necrosulfonamide is a necroptosis inhibitor acting by selectively targeting the mixed lineage kinase domain-like protein (MLKL). Necrosulfonamide prevents MLKL-RIP1-RIP3 necrosome complex from interacting with its downstream effectors. MLKL is a critical substrate of RIP3 during the induction of necrosis .
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