MedKoo Cat#: 406994 | Name: IWR-1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

IWR-1, also known as IWR-1-endo, is a an inhibitor of the Wnt signaling cascade through inhibiting TNKSs, binding only to the adenosine-binding site. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. IWR-1 inhibits cell proliferation and EMT even in the presence of TNF-α-induced cancer cell stimulation. IWR-1 also significantly suppressed cell migration, invasion, and matrix metalloproteinase activities of CRC cell lines. IWR-1 provides EMT reversal effects by directly suppressing survivin expression.

Chemical Structure

IWR-1
IWR-1
CAS#1127442-82-3

Theoretical Analysis

MedKoo Cat#: 406994

Name: IWR-1

CAS#: 1127442-82-3

Chemical Formula: C25H19N3O3

Exact Mass: 409.1426

Molecular Weight: 409.44

Elemental Analysis: C, 73.34; H, 4.68; N, 10.26; O, 11.72

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,650.00 2 Weeks
1g USD 2,850.00 2 Weeks
2g USD 4,650.00 2 Weeks
5g USD 6,450.00 2 Weeks
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Synonym
IWR-1; IWR 1; IWR1; IWR-1-endo.
IUPAC/Chemical Name
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-benzamide
InChi Key
ZGSXEXBYLJIOGF-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)
SMILES Code
O=C(NC1=C2N=CC=CC2=CC=C1)C3=CC=C(N(C(C4C(C5)C=CC5C64)=O)C6=O)C=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 409.44 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wang W, Lai S, Xiao Z, Yan H, Li Y, Zhang Y, Wu Y, Wang L. IWR-1 Inhibits Collagen-Induced Platelet Activation and Protects against Thrombogenesis. Hamostaseologie. 2019 Nov;39(4):392-397. doi: 10.1055/s-0038-1676822. Epub 2019 Mar 8. PMID: 30849780. 2: Gustafson CT, Mamo T, Maran A, Yaszemski MJ. Efflux inhibition by IWR-1-endo confers sensitivity to doxorubicin effects in osteosarcoma cells. Biochem Pharmacol. 2018 Apr;150:141-149. doi: 10.1016/j.bcp.2018.01.037. Epub 2018 Feb 8. PMID: 29412166; PMCID: PMC6121219. 3: Wang WM, Gao YM, Zheng XF, Jin HZ. IWR-1 attenuates the promotional effect of IL-36γ in a mouse model of psoriasis. BMC Immunol. 2024 Nov 23;25(1):78. doi: 10.1186/s12865-024-00669-1. PMID: 39578777; PMCID: PMC11585084. 4: Zhou MW, Yin WT, Jiang RH, Lee JH, Kim CD, Lee JH, Zhu MJ, Yoon TJ. Inhibition of collagen synthesis by IWR-1 in normal and keloid-derived skin fibroblasts. Life Sci. 2017 Mar 15;173:86-93. doi: 10.1016/j.lfs.2016.12.003. Epub 2016 Dec 7. PMID: 27939785. 5: Lee SC, Kim OH, Lee SK, Kim SJ. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. Oncotarget. 2015 Sep 29;6(29):27146-59. doi: 10.18632/oncotarget.4354. PMID: 26450645; PMCID: PMC4694979. 6: Martins-Neves SR, Paiva-Oliveira DI, Fontes-Ribeiro C, Bovée JVMG, Cleton- Jansen AM, Gomes CMF. 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. Cancer Lett. 2018 Feb 1;414:1-15. doi: 10.1016/j.canlet.2017.11.004. Epub 2017 Nov 8. PMID: 29126913. 7: Nair S, Davis A, Campagne O, Schuetz JD, Stewart CF. Development and Validation of a Sensitive and Specific LC-MS/MS Method for IWR-1-Endo, a Wnt Signaling Inhibitor: Application to a Cerebral Microdialysis Study. Molecules. 2022 Aug 25;27(17):5448. doi: 10.3390/molecules27175448. PMID: 36080214; PMCID: PMC9457781. 8: Xiao Y, Wang Y, Zhang M, Zhang Y, Ju Z, Wang J, Zhang Y, Yang C, Wang X, Jiang Q, Gao Y, Wei X, Liu W, Gao Y, Hu P, Huang J. Tankyrase inhibitor IWR-1 modulates HIPPO and Transforming Growth Factor β signaling in primed bovine embryonic stem cells cultured on mouse embryonic fibroblasts. Theriogenology. 2025 Feb;233:100-111. doi: 10.1016/j.theriogenology.2024.11.010. Epub 2024 Nov 19. PMID: 39613494.