1427782-89-5 Usage
Uses
Used in Pharmaceutical Industry:
IWP L6 is used as an inhibitor for Porcupine, which is essential for the regulation of the Wnt signaling pathway. By inhibiting Porcupine, IWP L6 can potentially be employed in the development of therapeutic strategies for various diseases, including cancer, where the Wnt signaling pathway is often dysregulated.
Used in Cancer Research:
IWP L6 is used as a research tool to study the role of Porcupine and the Wnt signaling pathway in cancer development and progression. By understanding the molecular mechanisms underlying these processes, researchers can identify potential targets for the development of novel cancer therapies.
Used in Drug Development:
IWP L6 can be used in the development of new drugs that target the Wnt signaling pathway, which is implicated in various diseases, including cancer, neurological disorders, and cardiovascular diseases. By inhibiting Porcupine, these drugs may help to modulate the Wnt signaling pathway and potentially provide therapeutic benefits for patients with these conditions.
Used in Drug Delivery Systems:
Similar to gallotannin, IWP L6 can also be incorporated into novel drug delivery systems to enhance its delivery, bioavailability, and therapeutic outcomes. Various organic and metallic nanoparticles can be employed as carriers for IWP L6 delivery, aiming to improve its efficacy against diseases where the Wnt signaling pathway is involved.
Biological Activity
iwp-l6 is an inhibitor of porcupine with ic50 value of 0.5nm [1].iwp-l6 is developed as a sub-nanomolar inhibitor.of porcupine. it targets the wnt signaling since porcupine is the enzyme to catalyze the palmitoylation of wnt proteins. in hek293 cells, iwp-l6 is found to inhibi the phosphorylation of dishevelled 2 (dvl2) significantly. iwp-l6 has good stability in human plasma but weaker stability in rat and mouse plasma. in vivo assay shows that iwp-l6 is quite active in zebrafish. it blocks the regeneration of the tailfin effectively. it also shows inhibition of posterior axis formation at low micromolar concentrations. additionally, in cultured mouse embryonic kidneys, 10nm iwp-l6 can significantly reduce branching morphogenesis while 50nm iwp-l6 completely blocks wnt signaling [1].
references
[1] wang x, moon j, dodge me, pan x, zhang l, hanson jm, tuladhar r, ma z, shi h, williams ns, amatruda jf, carroll tj, lum l, chen c. the development of highly potent inhibitors for porcupine. j med chem. 2013 mar 28;56(6):2700-4.
Check Digit Verification of cas no
The CAS Registry Mumber 1427782-89-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,2,7,7,8 and 2 respectively; the second part has 2 digits, 8 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1427782-89:
(9*1)+(8*4)+(7*2)+(6*7)+(5*7)+(4*8)+(3*2)+(2*8)+(1*9)=195
195 % 10 = 5
So 1427782-89-5 is a valid CAS Registry Number.
1427782-89-5Relevant articles and documents
HIGHLY POTENT INHIBITORS OF PORCUPINE
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Page/Page column 47, (2014/12/12)
The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.
The development of highly potent inhibitors for porcupine
Wang, Xiaolei,Moon, Jesung,Dodge, Michael E.,Pan, Xinchao,Zhang, Lishu,Hanson, Jordan M.,Tuladhar, Rubina,Ma, Zhiqiang,Shi, Heping,Williams, Noelle S.,Amatruda, James F.,Carroll, Thomas J.,Lum, Lawrence,Chen, Chuo
, p. 2700 - 2704 (2013/05/08)
Porcupine is a member of the membrane-bound O-acyltransferase family of proteins. It catalyzes the palmitoylation of Wnt proteins, a process required for their secretion and activity. We recently disclosed a class of small molecules (IWPs) as the first reported Porcn inhibitors. We now describe the structure-activity relationship studies and the identification of subnanomolar inhibitors. We also report herein the effects of IWPs on Wnt-dependent developmental processes, including zebrafish posterior axis formation and kidney tubule formation.
