IWR-1-endo
- Product Name
- IWR-1-endo
- CAS No.
- 1127442-82-3
- Chemical Name
- IWR-1-endo
- Synonyms
- IWR-1;CS-624;CS-1858;endo-IWR 1;IWR-1-endo;IWR-1-endo, >=98%;IWR-1(IWR-1-endo);IWR-1-endo ，S7086;IWR-1-endo USP/EP/BP;IWR-1, 10 mM in DMSO
- CBNumber
- CB82518787
- Molecular Formula
- C25H19N3O3
- Formula Weight
- 409.44
- MOL File
- 1127442-82-3.mol
IWR-1-endo Property
- alpha
- -3.0～+3.0°(20℃/D)(c=0.1,CH3CN)
- Boiling point:
- 643.9±55.0 °C(Predicted)
- Density
- 1.425±0.06 g/cm3(Predicted)
- storage temp.
- room temp
- solubility
- DMSO: soluble5mg/mL, clear
- form
- Liquid
- pka
- 11.88±0.43(Predicted)
- color
- white to beige
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Safety
- WGK Germany
- 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
- Precautionary statements
-
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- I0161
- Product name
- IWR-1
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $109
- Updated
- 2025/07/31
- Product number
- I0161
- Product name
- IWR-1
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $393.3
- Updated
- 2025/07/31
- Product number
- 5.04462
- Product name
- InSolution Wnt Antagonist I, IWR-1-endo - CAS 1127442-82-3 - Calbiochem
- Packaging
- 5MG
- Price
- $103
- Updated
- 2025/07/31
- Product number
- 681669
- Product name
- Wnt Antagonist I, IWR-1-<i>endo</i>
- Purity
- Wnt Antagonist I, IWR-1-endo, is a cell-permeable inhibitor of TNKS1/PARP5a (IC₅₀ = 131
- Packaging
- 10 mg
- Price
- $207
- Updated
- 2025/07/31
- Product number
- 681669
- Product name
- Wnt Antagonist I, IWR-1-endo
- Purity
- Wnt Antagonist I, IWR-1-endo, is a cell-permeable inhibitor of TNKS1/PARP5a (IC?? = 131 nM) & TNKS2/PARP5b (IC??= 56 nM). Suppress Wnt-stimulated transcription activity (IC?? = 180 nM).
- Packaging
- 10MG
- Price
- $201
- Updated
- 2024/03/01
IWR-1-endo Chemical Properties,Usage,Production
Description
IWR-1 endo (1127442-82-3) is a potent inhibitor of Wnt signaling (IC50=180 nM).1?Inhibits zebrafish tailfin regeneration (0.5 mM).2?Acts via inhibition of tankyrase and attenuates Wnt/β-catenin signaling in cancer stem-like cells.3?Promotes self-renewal and maintains pluripotency of human embryonic stem cells.4?Promotes differentiation of pluripotent stem cells into cardiomyocytes.5
Uses
IWR-3 act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b).Such compounds may be used in the treatment of Wnt protein signaling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.
Uses
IWR-1-endo act as inhibitors of Wnt response. It appear that IWR compounds induce stabilization of Axin proteins via a direct interaction, which is a part of the b-catenin destruction complex (consists of Apc, Axin, Ck1 and Gsk3b). Such compounds may be used in the treatment of Wnt protein signaling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosi s.
Definition
ChEBI: IWR-1-endo is a dicarboximide having an endo bridged phthalimide structure, substituted at nitrogen by a 4-(quinolin-8-ylcarbamoyl)benzoyl group. It has a role as an axin stabilizer and a Wnt signalling inhibitor. It is a dicarboximide, a bridged compound, a member of quinolines and a member of benzamides.
General Description
A cell-permeable p-imidobenzamidoquinoline, endo-diastereomer that is shown to inhibit the activity of TNKS1/PARP5a and TNKS2/PARP5b in in vitro auto-PARsylation assays (IC50 = 131 and 56 nM, respectively) and effectively suppress Wnt-stimulated transcription activity in L-Wnt-STF-based reporter assays (IC50 = 180 nM), while exhibiting little activity against PARP1 or PARP2 (IC50 >18.75 μM). Although both IWR-1-endo and XAV939 (Tankyrase1/2 Inhibitor; >Cat. No. 575545) act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effects both in vitro and in vivo, IWR-1-endo exerts its effect via interaction with Axin, while XAV939 binds TNKS directly.
Biochem/physiol Actions
Cell permeable: yes
storage
Store at RT
References
[1] BAOZHI CHEN. Small molecule–mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer[J]. Nature chemical biology, 2009, 5 2: 100-107. DOI:10.1038/nchembio.137
[2] JIANMING LU . Structure–activity relationship studies of small-molecule inhibitors of Wnt response[J]. Bioorganic & Medicinal Chemistry Letters, 2009, 19 14: Pages 3825-3827. DOI:10.1016/j.bmcl.2009.04.040
[3] SARA R. MARTINS-NEVES . IWR-1, a tankyrase inhibitor, attenuates Wnt/β-catenin signaling in cancer stem-like cells and inhibits in vivo the growth of a subcutaneous human osteosarcoma xenograft[J]. Cancer letters, 2018, 414: Pages 1-15. DOI:10.1016/j.canlet.2017.11.004
[4] HOON KIM. Modulation of β-catenin function maintains mouse epiblast stem cell and human embryonic stem cell self-renewal.[J]. Nature Communications, 2013: 2403. DOI:10.1038/ncomms3403
[5] YONGMING REN . Small molecule Wnt inhibitors enhance the efficiency of BMP-4-directed cardiac differentiation of human pluripotent stem cells[J]. Journal of molecular and cellular cardiology, 2011, 51 3: Pages 280-287. DOI:10.1016/j.yjmcc.2011.04.012
IWR-1-endo Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from IWR-1-endo manufacturers
- Product
- IWR-1-endo 1127442-82-3
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100kgs
- Release date
- 2019-12-17