1127442-82-3 Usage
Description
[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide, also known as IWR-1 endo, is a cell-permeable p-imidobenzamidoquinoline endo-diastereomer that has been shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b in in vitro auto-PARsylation assays. It effectively suppresses Wnt-stimulated transcription activity while exhibiting little activity against PARP1 or PARP2. IWR-1 endo acts as a potent inhibitor of Wnt signaling and has various applications in the treatment of Wnt protein signaling-related diseases and conditions.
Uses
1. Used in Anticancer Applications:
IWR-1 endo is used as an inhibitor of Wnt response for the treatment of cancer. It induces stabilization of Axin proteins via a direct interaction, which is a part of the β-catenin destruction complex. [(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide may be used in the treatment of Wnt protein signaling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes, and osteopetrosis.
2. Used in Regeneration and Stem Cell Applications:
IWR-1 endo is used as a promoter of self-renewal and maintenance of pluripotency in human embryonic stem cells. It also promotes differentiation of pluripotent stem cells into cardiomyocytes.
3. Used in Degenerative Disease Treatment:
IWR-1 endo is used as an inhibitor of Wnt response for the treatment of degenerative diseases, as it modulates Wnt protein signaling.
4. Used in Type II Diabetes Treatment:
IWR-1 endo is used as an inhibitor of Wnt response for the treatment of type II diabetes, as it modulates Wnt protein signaling.
5. Used in Osteopetrosis Treatment:
IWR-1 endo is used as an inhibitor of Wnt response for the treatment of osteopetrosis, as it modulates Wnt protein signaling.
Biochem/physiol Actions
Cell permeable: yes
References
1) Chen?et al. (2009),?Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer; Nature Chem. Biol.,?5?100
2) Lu?et al.?(2009),?Structure-activity Relationship Studies of Small-Molecule Inhibitors of Wnt Response; Bioorg. Med. Chem. Lett.,?19?3825
3) Martins-Neves?et al.?(2018),?IWR-1, a tankyrase inhibitor, attenuates Wnt/?-catenin signaling in cancer stem-like cells and inhibits in vivo the growth of subcutaneous human osteosarcoma xenograft; Cancer Lett.,?414?1
4) Kim?et al.?(2013),?Modulations of ?-catenin function maintains mouse epiblast stem cell and human embryonic stem cell self-renewal; Nat. Commun., 4?4403
5) Ren?et al.?(2011),?Small Molecule Wnt Inhibitors Enhance the Efficiency of BMP-4-directed Cardiac Differentiation of Human Pluripotent Stem Cells; J. Mol. Cell. Cardiol.,?51?280
Check Digit Verification of cas no
The CAS Registry Mumber 1127442-82-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,2,7,4,4 and 2 respectively; the second part has 2 digits, 8 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1127442-82:
(9*1)+(8*1)+(7*2)+(6*7)+(5*4)+(4*4)+(3*2)+(2*8)+(1*2)=133
133 % 10 = 3
So 1127442-82-3 is a valid CAS Registry Number.
