Porcupine
Porcupine (Porcn), a member of the membrane bound O-acyltransferase (MBOAT) family, and is required for Wnt secretion and signaling. MBOATs are further categorized into three subgroups based on their biochemical reactions: lipid biosynthesis, sterol acylation and acylation of secreted proteins/peptides, including the appetite stimulating peptide hormone ghrelin and the hedgehog (Hh) and Wnt morphogen families.MBOATs are predicted to have 8–12 transmembrane domains (TMDs) and localize in the protein secretory pathway. The endoplasmic recticulum resident enzyme, porcupine (PORCN) is essential for the palmitoleation of the Wnt ligands at the highly conserved serine residue 209 before their secretion. Secreted Wnt proteins play key roles in embryonic development, tissue homoeostasis and stem cell self-renewal; among the 19 Wnt proteins encoded in humans, Wnt3a is the most extensively studied isoform. An early report that PORCN palmitoylated Wnts at a cysteine residue in the N-terminal region (Cys77 in Wnt3a) has been shown to be erroneous. The membrane bound O-acyl transferase (MBOAT) PORCN has emerged as a molecular target of interest in the search for more clinical options to treat Wnt-driven cancers.
References
1.Ho SY,et al. Bioorg Med Chem Lett. 2015;25(23):5472–5476. 2.Masumoto N, et al. Biochem Soc Trans. 2015;43(2):246–252.
References
1.Ho SY,et al. Bioorg Med Chem Lett. 2015;25(23):5472–5476. 2.Masumoto N, et al. Biochem Soc Trans. 2015;43(2):246–252.
Wnt/Notch/Hedgehog
Porcupine
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GNF-6231
产品货号 : M32943
cas no: 1243245-18-2
GNF-6231 是一种具有口服活性 Porcupine (IC50= 0.8 nM) 、Pron 和内质网蛋白抑制剂。GNF-6231 具有抗癌活性。GNF-6231 可以通过阻断所有 Wnt 配体的分泌来抑制 Wnt 通路的激活。GNF-6231 可以用于心肌梗死的研究。 -
IWP-O1
产品货号 : M20089
cas no: 2074607-48-8
IWP-O1 是一种高效的豪猪 (Porcn) 抑制剂 (EC50: 80 pM),可有效抑制 HeLa 细胞中 Dvl2/3 和 LRP6 的磷酸化。 -
Clindamycin HCl
产品货号 : M18238
cas no: 21462-39-5
Clindamycin HydroHClide 通过作用于 50S 核糖体来抑制蛋白质合成。 -
VEGFR2 KiN/Ase Inhibitor I
产品货号 : M17339
cas no: 15966-93-5
VEGFR2 激酶抑制剂 I 是一种有效的、细胞渗透性的 VEGFR2 激酶抑制剂。 -
WNT-974
产品货号 : M10986
cas no: 1243244-14-5
一种有效且特异性的小分子豪猪 (PORCN) 抑制剂,在 PORCN 放射性配体结合测定中 IC50 为 1 nM。