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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.


References:


1.Zhang D,et al. Cell Mol Immunol. 2010;7(4):243–249.

Cat. No. Product Name CAS No. Information
H9240

GSK962

 		2049872-86-6

GSK'962 is a negative control for GSK'963, a highly potent and selective RIP1 inhibitor.
H9130

Eclitasertib

 		2125450-76-0

Eclitasertib is a potent RIPK1 protein inhibitor useful in treatment of RIPK1-​mediated diseases.
H1746

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.
H1745

Sibiriline

 		1346526-26-8

A specific competitive RIPK1 inhibitor with IC50 of 1.03 uM, 100-fold less potent for RIPK3; inhibits both TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis in FADD-deficient Jurkat cells (EC50=1.2 uM); selectively inhibits necroptotic cell death induced by various death ligands in human or mouse cells while not protecting from caspase-dependent apoptosis; protects mice from concanavalin A-induced hepatitis.
H1744

RIPK2-IN-8

 		2141969-56-2

A potent, selective, orally available RIPK2 inhibitor with IC50 of 3 nM; displays 90% percent of kinases showed

H1743

RIPK2-IN-2

 		1581270-11-2

A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor.
H1742

RIPK2-IN-1

 		1423186-80-4

A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor.
H1741

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.
H1740

RIPK2 inhibitor 1

 		1290490-78-6

RIPK2 inhibitor 1 is a novel potent, selective RIPK2 inhibitor with IC50 of 5-10 nM; potently inhibits the proliferation of cancer cells by > 70% and also inhibits NF-κB activity.
H1739

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.

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