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Receptor interacting protein 2 (RIP2) is a serine/threonine kinase, is an adaptor molecule of NOD1 and NOD2, and genetic variation in this receptor is known to be associated with the severity of allergic asthma in children.


Receptor interacting protein kinase 2 (RIPK2) is critical for NOD-mediated NF-κB activation and cytokine production. WEHI-345, a selective RIPK2 kinase inhibitor, which delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement.



Receptor interacting protein kinase 3 (RIPK3) is a cytosolic master regulator of necroptosis. RIPK3 has an active serine/threonine kinase domain at the N-terminus, and a unique protein-protein interaction domain called the RIP homotypic interaction motif (RHIM) at the C-terminus. Both kinase activity and RHIM are indispensable for necroptosis. RIPK3 interacts with other RHIM-containing proteins such as RIPK1, Toll/interleukin-1 (IL-1) receptor domain-containing adaptor protein inducing TRIF or DAI. RIPK3 induces necroptosis, a type of regulated necrosis, through its kinase domain and RHIM.

Cat. No. Product Name CAS No. Information
GY02673

RIPK2-IN-2

1581270-11-2

A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor.

GY02539

RIP2 kinase inhibitor 1

1423186-80-4

A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor.

GY02422

WEHI-345

1354825-58-3

A potent and selective RIPK2 inhibitor with IC50/Kd of 130/46 nM; displays negligible activity (>10 uM) against RIPK1, RIPK4 and RIPK5; delays RIPK2 ubiquitylation and NF-κB activation downstream of NOD engagement; prevents cytokine production in vitro and in vivo and ameliorates experimental autoimmune encephalomyelitis in mice.

GY06957

RIPK2-IN-8

2141969-56-2

RIPK2-IN-8 is a potent, selective, orally available RIPK2 inhibitor with IC50 of 3 nM; displays 90% percent of kinases showed <50% inhibition in a broad 250 kinase panel; effectively suppresses IL6 secrection in mouse bone marrow derived macrophages with IC50 of 12 nM; significantly reverses MDP-induced pro-inflammatory cytokines in rat colon

GY10120

HS-1371

2158197-70-5

HS-1371 (HS1371) is a novel potent, ATP-competitive receptor-interacting protein kinase-3 (RIP3 or RIPK3 kinase) inhibitor with IC50 of 20.8 nM; binds to the ATP binding pocket of RIP3 and inhibits ATP binding to prevent RIP3 enzymatic activity in vitro; inhibits S227 auto-phosphorylation of RIP3 in treated HT-29 cells, blocks necrosome complex formation, rescues cells from RIP3-dependent necroptotic cell death but not apoptotic cell death.

GY10482

RIPK2 inhibitor OD36

1638644-62-8

RIPK2 inhibitor OD36 is a potent, specific, ATP-competitive inhibitor of RIPK2 with IC50 of 5.3 nM, inhibits Tyr and Ser/Thr-directed activities of RIPK2; inhibits both RIPK2 tyrosine autophosphorylation as well as downstream NF-κB and MAPK signaling induced by MDP, downregulates a panel of RIPK2 kinase-dependent genes; reduces cellular infiltration in an in vivo MDP-induced peritonitis model; also shows high affinity for cyclin G-associated kinase (GAK) with Ki of 3.8 nM.

GY10548

RIPGBM

355406-76-7

RIPGBM is a cell type-selective, small molecule inducer of apoptosis in GBM cancer stem cells (CSCs) with EC50 of 220 nM (GBM 1 cells); RIPGBM is converted to an apoptosis-inducing derivative (cRIPGBM/RIPGBM-18) selectively in GBM CSCs; cRIPGBM induces apoptosis in GBM CSCs by interacting with RIPK2; significantly suppress tumor formation in vivo in orthotopic intracranial GBM CSC tumor xenograft mouse model.

GY10549

cRIPGBM

cRIPGBM (RIPGBM derivative cRIPGBM, RIPGBM-18) is a metabolite of RIPGBM induces apoptosis in GBM CSCs (EC50=68 nM in GBM 1 cells) by interacting with RIPK2 (Kd=2.3 uM); induces caspase 1-dependent apoptosis, reduces the formation of a prosurvival RIPK2/TAK1 complex and increases the formation of a proapoptotic RIPK2/caspase 1 complex.

GY10551

GSK2593074A

1337531-06-2

GSK2593074A (GSK'074, GSK-2593074A) is novel potent, selective RIP1/RIP3 kinase dual inhibitor, directly binds to RIP1 and RIP3 with Kd of 130 and 12 nM, respectively; potently inhibits necroptosis in various cell types (IC50=3 nM both in MOVAS and L929 cells), blocks necroptosis signaling pathway; inhibits RIP3-dependent RIP1-independent necroptosis and inflammation, but does not induce apoptosis; attenuates cell death and inflammation in calcium phosphate injured aortae.

GY01922

GSK-481

1622849-58-4

A highly potent, monokinase selective and ATP-competitive inhibitor of RIP1 kinase with biochemical IC50 of 10 nM; displays complete specificity for RIP1 kinase over a panel of 456 kinases; exhibits excellent translation in the U937 cellular assay with IC50 of 10 nM, demonstrates significant blockage of the induced RIP1 autophosphorylation at Ser166 in HT29 cells; possesses good pharmacokinetic profiles in rodents.

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