CSLP43 

CSLP43 is a selective RIPK2 and XIAP inhibitor with an IC₅₀ of 19.9 nM against human RIPK2. CSLP43 binds to the ATP-binding pocket of RIPK2 and disrupts the interaction between RIPK2 and the BIR2 domain of XIAP or cIAP1. CSLP43 inhibits RIPK2 ubiquitination, NOD1-dependent inflammatory signaling pathways, NOD2-dependent inflammatory signaling pathways, as well as NF-κB activation associated with NOD agonists. CSLP43 is selective for the NOD1/NOD2 signaling pathway and does not inhibit the kinase activity of RIPK1 or RIPK3. CSLP43 is applicable to research related to Crohn's disease, Blau syndrome, early-onset sarcoidosis and early-onset inflammatory bowel disease^[1].

CSLP43 inhibits NOD2-mediated NF-κB activation in HEKBlue hNOD2 cells with an IC₅₀ of 1.3 nM^[1].
CSLP43 binds to intracellular RIPK2 in HEKBlue cells, with an IC₅₀ of 10.1 nM and a residence time of 106.9 min^[1].
CSLP43 (0-1 μM; 4 h) inhibits L18-MDP (HY-148690)-induced CXCL8 production in U2OS/NOD2 cells^[1].
CSLP43 inhibits MDP-induced TNF release in RAW264.7 macrophages with an IC₅₀ of 1.2 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

511.64

C₂₆H₃₃N₅O₄S

2244988-80-3

O=S(=O)(NC=1C=C(C=C(OC)C1OC)C2=CC(=CN=C2N)C=3C=CC(=CC3)N4CCNCC4)CCC

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hrdinka M, et al. Small molecule inhibitors reveal an indispensable scaffolding role of RIPK2 in NOD2 signaling. EMBO J. 2018;37(17):e99372.  [Content Brief]