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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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IWR-1-endo Suppliers

Canada 1 China 116 India 2 United Kingdom 2 United States 18 Global 139
AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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info@adooq.com
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United States
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Target molecule Corp.
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857-239-0968
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TargetMol Chemicals Inc.
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+1-781-999-5354 +1-00000000000
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marketing@targetmol.com
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InvivoChem
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Cckinase, Inc.
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BOC Sciences
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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
  • 4-((3aR,4R,7S,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
  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Inhibitors