R-Spondin4 Inhibitors
Chemical inhibitors of R-Spondin4 can disrupt its functional activity by targeting various components of the Wnt/β-catenin signaling pathway, a pathway that R-Spondin4 is known to enhance. For instance, IWP-2 and LGK-974 act upstream in the Wnt signaling cascade: IWP-2 impairs the production of Wnt proteins themselves, while LGK-974 inhibits the enzyme porcupine, crucial for Wnt protein maturation and secretion. With diminished Wnt levels, R-Spondin4's role in amplifying the signaling pathway is inherently suppressed. Further downstream, XAV-939, JW55, and KY1220 obstruct the pathway at the level of β-catenin and its co-activators. XAV-939 promotes the degradation of β-catenin by stabilizing Axin, negating the effect of R-Spondin4 on enhancing β-catenin stability. JW55 and KY1220 prevent the essential interactions between β-catenin and TCF or its coactivator BCL9, respectively, which are critical for the transcriptional activity driven by Wnt signaling. These inhibitors collectively attenuate the potentiation of the signaling by R-Spondin4 by either removing its targets or by rendering the interactions that drive signal transduction ineffective.
CGP049090 and CCT251545 directly inhibit TCF, a transcription factor that is essential to the transcriptional activation of Wnt target genes. FH535, ICRT3, PKF118-310, and LF3 also function to inhibit the interactions between β-catenin and TCF, which is a critical step for the activation of Wnt-responsive genes. By blocking this interaction, these chemicals effectively prevent R-Spondin4 from fulfilling its role in enhancing Wnt/β-catenin signaling.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
IWP-2 | 686770-61-6 | sc-252928 sc-252928A | 5 mg 25 mg | $94.00 $286.00 | 27 | |
IWP-2 inhibits the production of Wnt proteins, which R-Spondin4 is known to potentiate by stabilizing the Frizzled/LRP6 complex. Inhibition of Wnt production reduces R-Spondin4 activity by decreasing the availability of its target signaling components. | ||||||
LGK 974 | 1243244-14-5 | sc-489380 sc-489380A | 5 mg 50 mg | $352.00 $1270.00 | 2 | |
LGK-974 functions as an inhibitor of the enzyme porcupine, which is involved in the palmitoylation and secretion of Wnt proteins. By inhibiting porcupine, LGK-974 reduces Wnt signaling, thereby limiting the ability of R-Spondin4 to enhance Wnt signaling. | ||||||
XAV939 | 284028-89-3 | sc-296704 sc-296704A sc-296704B | 1 mg 5 mg 50 mg | $35.00 $115.00 $515.00 | 26 | |
XAV-939 inhibits tankyrase 1 and 2, leading to stabilization of Axin and degradation of β-catenin. As R-Spondin4 acts to amplify Wnt signaling by preventing Axin-mediated LRP6 degradation, XAV-939 reduces the functional impact of R-Spondin4 by promoting the breakdown of β-catenin. | ||||||
JW 55 | 664993-53-7 | sc-364517 sc-364517A | 10 mg 50 mg | $172.00 $726.00 | ||
JW55 antagonizes the Wnt/β-catenin pathway by inhibiting the interaction between β-catenin and TCF. Since R-Spondin4 enhances the Wnt/β-catenin signaling, JW55 inhibition of this interaction diminishes the functional enhancement of the pathway by R-Spondin4. | ||||||
Cercosporin | 35082-49-6 | sc-255013 | 5 mg | $450.00 | 1 | |
Cercosporin acts as an inhibitor of Wnt/β-catenin signaling by selectively binding to and inhibiting TCF. The inhibition of TCF by Cercosporin results in a functional inhibition of R-Spondin4, as it cannot effectively enhance Wnt signaling without TCF's activity. | ||||||
β-Catenin/Tcf Inhibitor, FH535 | 108409-83-2 | sc-221398 sc-221398A | 10 mg 50 mg | $178.00 $367.00 | 7 | |
FH535 is known to inhibit both Wnt/β-catenin and PPAR signaling. By inhibiting these pathways, FH535 impedes the ability of R-Spondin4 to potentiate the Wnt/β-catenin pathway, leading to a functional inhibition of R-Spondin4's activity. | ||||||
PKF118-310 | 84-82-2 | sc-364590 sc-364590A | 5 mg 25 mg | $176.00 $638.00 | ||
PKF118-310 is a β-catenin/TCF interaction inhibitor. By preventing the formation of the β-catenin/TCF complex, it functionally inhibits the enhancement of Wnt/β-catenin signaling by R-Spondin4. | ||||||
LF3 | 664969-54-4 | sc-507526 | 10 mg | $160.00 | ||
LF3 inhibits the Wnt/β-catenin pathway by blocking the interaction between β-catenin and TCF. This inhibition directly reduces the ability of R-Spondin4 to potentiate its signaling effects within this pathway. | ||||||