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Cat. No. Product Name CAS No. Information
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-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-35704

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.
PC-35429

CLSP43

CLSP43 (RIPK2 inhibitor CLSP43) 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

CLSP37

CLSP37 (RIPK2 inhibitor CLSP37) 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-63388

GSK-2982772

1622848-92-3 GSK-2982772 is a potent, selective, ATP competitive RIP1 kinase inhibitor with IC50 of 16 nM; inhibits RIP1-dependent inflammatory cytokine MIP-1β production in human whole blood with IC50 of 0.5 nM, reduces spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue; shows potential for the treatment of inflammatory diseases in vivo.

Psoriasis

Phase 2 Clinical

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.

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