IWR-1-endo

ChemicalBook > CAS DataBase List > 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 USP/EP/BP;Wnt Antagonist I, IWR-1-endo;IWR-1-endo - IWR-1 | endo-IWR-1
CBNumber: CB82518787
Molecular Formula: C25H19N3O3
Formula Weight: 409.44
MOL File: 1127442-82-3.mol

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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.

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Safety

WGK Germany: 3

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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.

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N-Bromosuccinimide Price

Sigma-Aldrich

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

Sigma-Aldrich

Product number: 5.04462
Product name: InSolution Wnt Antagonist I, IWR-1-endo - CAS 1127442-82-3 - Calbiochem
Packaging: 5MG
Price: $118
Updated: 2024/03/01

Sigma-Aldrich

Product number: I0161
Product name: IWR-1
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $103
Updated: 2023/06/20

Sigma-Aldrich

Product number: I0161
Product name: IWR-1
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $393
Updated: 2023/06/20

Cayman Chemical

Product number: 13659
Product name: IWR-1-endo
Purity: ≥98%
Packaging: 5mg
Price: $67
Updated: 2024/03/01

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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) 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

IWR-1-endo Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from IWR-1-endo manufacturers

Career Henan Chemical Co

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

1127442-82-3, IWR-1-endoRelated Search:

TYRPHOSTIN AG 879 Ko 143 Cantharidin Troglitazone KY0211 Y27632 (hydrochloride) xav-939 Wnt-C59 ICG-001 CHIR-99021

[(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

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

ENDO-IWR 1;IWR-1-ENDO;IWR1;IWR 1

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%

4-(1,3,3a,4,7,7a-Hexahydro-1,3-dioxo-4,7-methano-2H-isoindol-2-yl)-N-8-quinolinyl-Benzamide (IWR-1)

CS-1858

IWR-1(IWR-1-endo)

IWR-1-endo - IWR-1 | endo-IWR-1

CS-624

Wnt Antagonist I, IWR-1-endo

IWR-1-endo USP/EP/BP

rel-4-((3aR,4S,7R,7aS)-1,3-Dioxo-1,3,3a,4,7,7a-hexahydro-2H-4,7-methanoisoindol-2-yl)-N-(quinolin-8-yl)benzamide

1127442-82-3

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