- IWR-1
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- $50.00
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2026-05-29
- CAS:1127442-82-3
- Purity: 99.61%
- Supply Ability: 10g
- IWR-1-endo
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- $1.00
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2019-12-20
- CAS:1127442-82-3
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: 100kgs
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| | IWR-1-endo Basic information |
| Product Name: | IWR-1-endo | | Synonyms: | [(3aR*,4S*,7R*,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide;Benzamide, 4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinyl-, rel-;endo-IWR 1;IWR-1-endo;rel-4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-Methano-2H-isoindol-2-yl]-N-8-quinolinylbenzaMide;rel-4-[(3aR,4S,7R,7aS)-1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl]-N-8-quinolinylbenzamide IWR-1-endo;IWR-1-endo, >=98%;ENDO-IWR 1;IWR-1-ENDO;IWR1;IWR 1 | | CAS: | 1127442-82-3 | | MF: | C25H19N3O3 | | MW: | 409.44 | | EINECS: | | | Product Categories: | Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors | | Mol File: | 1127442-82-3.mol |  |
| | IWR-1-endo Chemical Properties |
| 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. | | InChIKey | ZGSXEXBYLJIOGF-ALFLXDJESA-N | | SMILES | N4(C(=O)[C@@H]5[C@@H]([C@H]6C[C@@H]5C=C6)C4=O)c1ccc(cc1)C(=O)Nc2c3ncccc3ccc2 |
| WGK Germany | 3 | | Storage Class | 10 - Combustible liquids |
| | IWR-1-endo Usage And Synthesis |
| Description | IWR-1 endo (1127442-82-3) is a potent inhibitor of Wnt signaling (IC50=180 nM).1Inhibits zebrafish tailfin regeneration (0.5 mM).2Acts via inhibition of tankyrase and attenuates Wnt/β-catenin signaling in cancer stem-like cells.3Promotes self-renewal and maintains pluripotency of human embryonic stem cells.4Promotes differentiation of pluripotent stem cells into cardiomyocytes.5 | | 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. | | 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. | | 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 |
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