687561-60-0 Usage
Description
IWP-3 is a small molecule inhibitor that targets porcupine, an enzyme responsible for the palmitoylation of Wnt proteins. This process is essential for the regulation of Wnt signaling, which plays a critical role in various biological processes, including embryonic development, tissue homeostasis, and tumorigenesis. By inhibiting porcupine, IWP-3 can potentially disrupt the Wnt signaling pathway and exhibit therapeutic effects against cancer.
Uses
Used in Anticancer Applications:
IWP-3 is used as an anticancer agent for its ability to inhibit the palmitoylation of Wnt proteins, which are crucial in tumorigenesis. By targeting porcupine, IWP-3 can potentially disrupt the Wnt signaling pathway, leading to the suppression of tumor growth and progression.
Used in Drug Delivery Systems:
In the pharmaceutical industry, IWP-3 is used as a key component in the development of drug delivery systems designed to improve the efficacy and bioavailability of anticancer treatments. These systems may include various organic and metallic nanoparticles as carriers for IWP-3, aiming to enhance its delivery to cancer cells and improve therapeutic outcomes.
Biological Activity
iwp-3 is an inhibitor of wnt production.wnt signaling proteins, a group of small secreted proteins, are active in tissue homeostasis, embryonic development, as well as tumorigenesis. wnt proteins can bind to the cell surface receptors, initiating a signaling cascade that results in the β-catenin activation of gene transcription.
Biochem/physiol Actions
IWP-3 is a Wnt inhibitor that prevents palmitylation of Wnt proteins by Porcupine (Porcn). IWP-3 is an inactivator of Porcn function that acts as inhibitors of Wnt production. Studies revealed that IWP-3 induces differentiation of human mesoderm cells to form cardiomyocytes.
in vitro
in previous study, iwp-3 was identified as an inhibitor of wnt production that could regulate in vitro wnt pathway activity with an ic50 value of 40 nm. in addition, iwp-3 was found to be able to inactivate porcupine, a o-acyltransferase for palmitoylating wnt proteins that was critical for the signaling ability and secretion. moreover, iwp-3 at 5 μm was found to block wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 and the scaffold protein dishevelled, resulting in preventing the accumulation of β-catenin [1]. in another study, iwp-3 was applied to promote cardiomyocyte generation from human embryonic stem cells by inhibiting wnt signaling [2].
IC 50
40 nm
references
[1] b. chen, m. e. dodge, w. tang, et al. small molecule-mediated disruption of wnt-dependent signaling in tissue regeneration and cancer. nature chemical biology 5(2), 100-107 (2009).[2] e. willems, s. spiering, h. davidovics, et al. small molecule inhibitors of the wnt pathway potently promote cardiomyocytes from human embryonic stem cell derived mesoderm. circulation research 109(4), 360-364 (2011).
Check Digit Verification of cas no
The CAS Registry Mumber 687561-60-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,8,7,5,6 and 1 respectively; the second part has 2 digits, 6 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 687561-60:
(8*6)+(7*8)+(6*7)+(5*5)+(4*6)+(3*1)+(2*6)+(1*0)=210
210 % 10 = 0
So 687561-60-0 is a valid CAS Registry Number.