LGK974,1243244-14-5

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

LGK974

CAS No. : 1243244-14-5

MCE 国际站：LGK974

产品活性：LGK974 (WNT974) 是一种有效的，具有口服活性的特异性 Porcupine (PORCN) 抑制剂，IC₅₀ 为 0.1 nM。

研究领域：Stem Cell/Wnt

作用靶点：Porcupine

In Vitro: LGK974 effectively displaces [³H]-GNF-1331 with an IC₅₀ of 1 nM in the PORCN radioligand binding assay. LGK974 potently reduces Wnt-dependent AXIN2 mRNA levels in HN30 cells with an IC₅₀ of 0.3 nM.

In Vivo: LGK974, a drug that targets Porcupine, a Wnt-specific acyltransferase. LGK974 potently inhibits Wnt signaling, has strong efficacy in rodent tumor models, and is well-tolerated. Toxicology studies are performed on nontumor bearing rats at 3 and 20 mg/kg. At the efficacious dose of 3 mg/kg per day for 14 d, LGK974 is well-tolerated without abnormal histopathological findings in Wnt-dependent tissues, including the intestine, stomach, and skin. When rats are administrated a very high dose of 20 mg/kg per day for 14 d, loss of intestinal epithelium is observed, consistent with the concept that Wnt is required for intestinal tissue homeostasis.

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Heterocyclic Compound Library  |  Highly Selective Inhibitors Library  |  IWP-2  |  Wnt-C59  |  ETC-159  |  IWP L6  |  IWP-O1  |  GNF-6231  |  Porcn-IN-1  |  Zamaporvint

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds