LGK974 | Porcupine inhibitor

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LGK974 (1243244-14-5) is a potent and selective inhibitor of Porcupine (IC50 = 1 nM). Inhibits Wnt signaling (IC50 = 0.4 nM) in vitro and in vivo.1 It displays efficacy in several cancer models including glioblastoma2,6, squamous cell3, renal cell carcinoma4, and non-small cell lung5. LGK974 reprogrammed the immune suppressive tumor microenvironment in a mouse model of glioblastoma to increase antitumor immune responses.6 It also potentiated anti-PD1 therapy by increasing DC3-like dendritic cells and decreasing myeloid suppressor cells. LGK974 attenuated myocardial ischemia-reperfusion injury by reducing inflammatory responses.7

References/Citations:

  1. Liu et al. (2013), Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974; Proc. Natl. Acad. Sci. USA 110 20224
  2. Suwala et al. (2018), Inhibition of Wnt/beta-catenin signaling downregulates expression of aldehyde dehydrogenase isoform 3A1 (ALDH3A1) to reduce resistance against temozolomide in glioblastoma in vitro; Oncotarget 9 22703
  3. Zimmerli et al. (2018), WNT ligands control initiation and progression of human papillomavirus-driven squamous cell carcinoma; Oncogene 37 3753
  4. Li et al. (2020), Porcupine Inhibitor LGK974 Downregulates the Wnt Signaling Pathway and Inhibits Clear Cell Renal Cell Carcinoma; Biomed. Res. Int. 2020 2527643
  5. Tang et al. (2021), Porcupine inhibitor LGK-974 inhibits Wnt/ß-catenin signaling and modifies tumor-associated macrophages resulting in inhibition of the malignant behaviors of non-small cell lung cancer cells; Mol. Med. Rep. 24 550
  6. Krishnan et al. (2025), Wnt inhibition alleviates resistance to anti-PD1 therapy and improves antitumor immunity in glioblastoma; Proc. Natl. Acad. Sci. USA 122 e2414941122
  7. Meyer et al. (2022), Blockade of Wnt Secretion Attenuates Myocardial Ischemia-Reperfusion Injury by Modulating the Inflammatory Response; Int. J. Mol. Sci. 23 12252
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Alternate Name:
WNT974

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

LGK974 (1243244-14-5) is a potent and selective inhibitor of Porcupine (IC50 = 1 nM). Inhibits Wnt signaling (IC50 = 0.4 nM) in vitro and in vivo.1 It displays efficacy in several cancer models including glioblastoma2,6, squamous cell3, renal cell carcinoma4, and non-small cell lung5. LGK974 reprogrammed the immune suppressive tumor microenvironment in a mouse model of glioblastoma to increase antitumor immune responses.6 It also potentiated anti-PD1 therapy by increasing DC3-like dendritic cells and decreasing myeloid suppressor cells. LGK974 attenuated myocardial ischemia-reperfusion injury by reducing inflammatory responses.7

References/Citations:

  1. Liu et al. (2013), Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974; Proc. Natl. Acad. Sci. USA 110 20224
  2. Suwala et al. (2018), Inhibition of Wnt/beta-catenin signaling downregulates expression of aldehyde dehydrogenase isoform 3A1 (ALDH3A1) to reduce resistance against temozolomide in glioblastoma in vitro; Oncotarget 9 22703
  3. Zimmerli et al. (2018), WNT ligands control initiation and progression of human papillomavirus-driven squamous cell carcinoma; Oncogene 37 3753
  4. Li et al. (2020), Porcupine Inhibitor LGK974 Downregulates the Wnt Signaling Pathway and Inhibits Clear Cell Renal Cell Carcinoma; Biomed. Res. Int. 2020 2527643
  5. Tang et al. (2021), Porcupine inhibitor LGK-974 inhibits Wnt/ß-catenin signaling and modifies tumor-associated macrophages resulting in inhibition of the malignant behaviors of non-small cell lung cancer cells; Mol. Med. Rep. 24 550
  6. Krishnan et al. (2025), Wnt inhibition alleviates resistance to anti-PD1 therapy and improves antitumor immunity in glioblastoma; Proc. Natl. Acad. Sci. USA 122 e2414941122
  7. Meyer et al. (2022), Blockade of Wnt Secretion Attenuates Myocardial Ischemia-Reperfusion Injury by Modulating the Inflammatory Response; Int. J. Mol. Sci. 23 12252