Chemical Structure : CSLP43
货号: PC-35429Not For Human Use, Lab Use Only.
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.
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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.
CSLP43 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.
CSLP43 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.
分子量 | 511.641 | |
分子式 | C26H33N5O4S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Hrdinka M, et al. EMBO J. 2018 Jul 19. pii: e99372.
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