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Cat. No. Product Name CAS No. Information
PC-35429

CSLP43

2244988-80-3

CSLP43 (RIPK2 inhibitor CSLP43) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 19.9 nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling; exhibits inhibition of TNF release from RAW264.7 cells with EC50 of 1.2 nM, inhibits NF-κB reporter activity with IC50 of 1.34 nM; antagonizes NOD2 signaling by interfering with the XIAP-RIPK2 interaction, selectively inhibits NOD responses in cells (HEKBlue NOD2 IC50=1.3 nM) and displays potent activity in vivo, does not attenuates the TNF release following an unrelated pro-inflammatory stimulation mediated through TLR4 activation by LPS at 1 uM.

PC-35428

CSLP37

2244984-64-1

CSLP37 (RIPK2 inhibitor CSLP37) is a novel potent, ATP pocket-binding RIPK2 inhibitor with IC50 of 16.3 nM in ADPGlo assay, demonstrates inhibition of both the RIPK2-XIAP interaction, and of cellular and in vivo NOD2 signaling; exhibits inhibition of TNF release from RAW264.7 cells with EC50 of 12.6 nM, inhibits NF-κB reporter activity with IC50 of 22.5 nM; antagonizes NOD2 signaling by interfering with the XIAP-RIPK2 interaction, selectively inhibits NOD responses in cells (HEKBlue NOD2 IC50=26.3 nM) and displays potent activity in vivo, does not attenuates the TNF release following an unrelated pro-inflammatory stimulation mediated through TLR4 activation by LPS at 1 uM.

PC-63258

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.

PC-62661

GSK-872

1346546-69-7

GSK-872 (GSK'872) is a potent and selective RIPK3 (receptor-interacting protein kinase-3) inhibitor; interferes with receptor-mediated endocytosis, entry of HIV, and synaptic vesicle recycling; attenuates rat nucleus pulposus (NP) cells death.

PC-42102

GSK-583

1346547-00-9

A potent, selective and orally bioavailable RIPK2 kinase inhibitor with IC50 of 5 nM and 2 nM for human and rat RIP2, respectively; displays robust selectivity against p38α and VEGFR2, and shows little or no inhibition of RIP3-dependent necroptotic cell death; potently and dose dependently inhibits MDP-stimulated TNFα production in human monocytes and human whole bolld with IC50 of 8 nM and 237 nM, respectively; inhibits MDP-induced inflammatory responses in vivo.

PC-36135

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.
PC-36066

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.

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