iCRT3 | CAS#901751-47-1 | Wnt/wingless signaling pathway inhibitor

MedKoo Cat#: 407847 | Name: iCRT3

Description:

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

iCRT3 is an inhibitor of the Wnt/wingless signaling pathway. iCRT3 efficiently block Wnt/β-catenin-induced target genes and phenotypes in various mammalian and cancer cell lines. Importantly, these Wnt inhibitors are specifically cytotoxic to human colon tumor biopsy cultures as well as colon cancer cell lines that exhibit deregulated Wnt signaling.

Chemical Structure

iCRT3

CAS#901751-47-1

Theoretical Analysis

MedKoo Cat#: 407847

Name: iCRT3

CAS#: 901751-47-1

Chemical Formula: C23H26N2O2S

Exact Mass: 394.1715

Molecular Weight: 394.53

Elemental Analysis: C, 70.02; H, 6.64; N, 7.10; O, 8.11; S, 8.13

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 2,950.00	2 Weeks

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Related CAS #

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Synonym

iCRT3; iCRT-3; iCRT 3;

IUPAC/Chemical Name

2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)acetamide

InChi Key

QTDYVSIBWGVBKU-UHFFFAOYSA-N

InChi Code

InChI=1S/C23H26N2O2S/c1-3-18-9-11-20(12-10-18)23-25-21(17(2)27-23)15-28-16-22(26)24-14-13-19-7-5-4-6-8-19/h4-12H,3,13-16H2,1-2H3,(H,24,26)

SMILES Code

O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2

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

Misregulated β-catenin responsive transcription (CRT) has been implicated in the genesis of various malignancies, including colorectal carcinomas, and it is a key therapeutic target in combating various cancers. Despite significant effort, successful clinical implementation of CRT inhibitory therapeutics remains a challenging goal. T

Product Data

Product Data

Instruction

View handling instruction

Biological target:

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

In vitro activity:

Significantly increased collagen expression was observed in TGF-β–treated WT C1. 1 cells as compared to that in WT untreated (control) cells (Figure 4). Treatment with rhTGF-β1 combined with ICG-001 or iCRT3 significantly reduced collagen expression compared with that in rhTGF-β1-treated C1.1 cells (Figure 4). Reference: Am J Pathol. 2021 Jun;191(6):993-1009. https://pubmed.ncbi.nlm.nih.gov/33753026/

In vivo activity:

Similarly, levels of another common tissue damage marker LDH in these septic mice were 10.9-fold higher and were reduced by 27.7% and 56.9%, respectively after 5 and 10 mg/kg iCRT3 treatment (Fig. 3C). Taken together, these results indicated that administration of iCRT3 resulted in the reduction of systemic levels of pro-inflammatory cytokines and organ injury markers in septic mice. Reference: Sci Rep. 2017 Aug 23;7(1):9235. https://pubmed.ncbi.nlm.nih.gov/28835626/

	Solvent	mg/mL	mM
Solubility
	DMSO	114.0	288.95
	Ethanol	78.0	197.70

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 394.53 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.

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

Formulation protocol:

1. Rao P, Qiao X, Hua W, Hu M, Tahan M, Chen T, Yu H, Ren X, Cao Q, Wang Y, Yang Y, Wang YM, Lee VW, Alexander SI, Harris DC, Zheng G. Promotion of β-Catenin/Forkhead Box Protein O Signaling Mediates Epithelial Repair in Kidney Injury. Am J Pathol. 2021 Jun;191(6):993-1009. doi: 10.1016/j.ajpath.2021.03.005. Epub 2021 Mar 19. PMID: 33753026; PMCID: PMC8351131. 2. Shao S, Fang H, Duan L, Ye X, Rao S, Han J, Li Y, Yuan G, Liu W, Zhang X. Lysyl hydroxylase 3 increases collagen deposition and promotes pulmonary fibrosis by activating TGFβ1/Smad3 and Wnt/β-catenin pathways. Arch Med Sci. 2019 Jan 16;16(2):436-445. doi: 10.5114/aoms.2018.81357. PMID: 32190155; PMCID: PMC7069430. 3. Sharma A, Yang WL, Ochani M, Wang P. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. Sci Rep. 2017 Aug 23;7(1):9235. doi: 10.1038/s41598-017-08711-6. PMID: 28835626; PMCID: PMC5569053.

In vitro protocol:

In vivo protocol:

1. Sharma A, Yang WL, Ochani M, Wang P. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. Sci Rep. 2017 Aug 23;7(1):9235. doi: 10.1038/s41598-017-08711-6. PMID: 28835626; PMCID: PMC5569053.

1: Bo H, Wu Q, Zhu C, Zheng Y, Cheng G, Cui L. PIEZO1 acts as a cancer suppressor by regulating the ROS/Wnt/β-catenin axis. Thorac Cancer. 2024 Apr;15(12):1007-1016. doi: 10.1111/1759-7714.15278. Epub 2024 Mar 18. PMID: 38494915; PMCID: PMC11045336. 2: Sharma A, Yang WL, Ochani M, Wang P. Mitigation of sepsis-induced inflammatory responses and organ injury through targeting Wnt/β-catenin signaling. Sci Rep. 2017 Aug 23;7(1):9235. doi: 10.1038/s41598-017-08711-6. PMID: 28835626; PMCID: PMC5569053. 3: Su M, Liang Z, Shan S, Gao Y, He L, Liu X, Wang A, Wang H, Cai H. Long non- coding RNA NEAT1 promotes aerobic glycolysis and progression of cervical cancer through WNT/β-catenin/PDK1 axis. Cancer Med. 2024 May;13(9):e7221. doi: 10.1002/cam4.7221. PMID: 38733179; PMCID: PMC11087816. 4: Rao P, Qiao X, Hua W, Hu M, Tahan M, Chen T, Yu H, Ren X, Cao Q, Wang Y, Yang Y, Wang YM, Lee VW, Alexander SI, Harris DC, Zheng G. Promotion of β-Catenin/Forkhead Box Protein O Signaling Mediates Epithelial Repair in Kidney Injury. Am J Pathol. 2021 Jun;191(6):993-1009. doi: 10.1016/j.ajpath.2021.03.005. Epub 2021 Mar 19. PMID: 33753026; PMCID: PMC8351131. 5: Shao S, Fang H, Duan L, Ye X, Rao S, Han J, Li Y, Yuan G, Liu W, Zhang X. Lysyl hydroxylase 3 increases collagen deposition and promotes pulmonary fibrosis by activating TGFβ1/Smad3 and Wnt/β-catenin pathways. Arch Med Sci. 2019 Jan 16;16(2):436-445. doi: 10.5114/aoms.2018.81357. PMID: 32190155; PMCID: PMC7069430. 6: Saj A, Chatterjee SS, Zhu B, Cukuroglu E, Gocha T, Zhang X, Göke J, DasGupta R. Disrupting Interactions Between β-Catenin and Activating TCFs Reconstitutes Ground State Pluripotency in Mouse Embryonic Stem Cells. Stem Cells. 2017 Aug;35(8):1924-1933. doi: 10.1002/stem.2647. Epub 2017 Jun 15. PMID: 28577307. 7: You Y, Que K, Zhou Y, Zhang Z, Zhao X, Gong J, Liu Z. MicroRNA-766-3p Inhibits Tumour Progression by Targeting Wnt3a in Hepatocellular Carcinoma. Mol Cells. 2018 Sep 30;41(9):830-841. doi: 10.14348/molcells.2018.0181. Epub 2018 Aug 27. PMID: 30145863; PMCID: PMC6182221. 8: Shin JH, Kim HW, Rhyu IJ, Kee SH. Axin is expressed in mitochondria and suppresses mitochondrial ATP synthesis in HeLa cells. Exp Cell Res. 2016 Jan 1;340(1):12-21. doi: 10.1016/j.yexcr.2015.12.003. Epub 2015 Dec 15. PMID: 26704260. 9: Ito A, Ye K, Onda M, Morimoto N, Osakada F. Efficient and robust induction of retinal pigment epithelium cells by tankyrase inhibition regardless of the differentiation propensity of human induced pluripotent stem cells. Biochem Biophys Res Commun. 2021 May 7;552:66-72. doi: 10.1016/j.bbrc.2021.03.012. Epub 2021 Mar 17. PMID: 33743349. 10: Xiao H, Zeng Y, Wang Q, Wei S, Zhu X. A Novel Positive Feedback Loop Between NTSR1 and Wnt/β-Catenin Contributes to Tumor Growth of Glioblastoma. Cell Physiol Biochem. 2017;43(5):2133-2142. doi: 10.1159/000484232. Epub 2017 Oct 24. PMID: 29065410.

View History

C8-C1

MedKoo CAT#: 565519

CAS#: N/A