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Merck
모든 사진(1)

문서

219332

Sigma-Aldrich

β-Catenin/Tcf Inhibitor III, iCRT3

The β-Catenin/Tcf Inhibitor III, iCRT3 controls the biological activity of β-Catenin/Tcf. This small molecule/inhibitor is primarily used for Biochemicals applications.

동의어(들):

β-Catenin/Tcf Inhibitor III, iCRT3, 2-(((2-(4-Ethylphenyl)-5-methyl-1,3-oxazol-4-yl)methyl)sulfanyl)-N-(2-phenylethyl)acetamide, Inhibitor of β-Catenin Responsive Transcription, C3, Wnt Pathway Inhibitor VIII, C3, 2-(((2-(4-Ethylphenyl)-5-methyl-1,3-oxazol-4-yl)methyl)sulfanyl)-N-(2-phenylethyl)acetamide, Inhibitor of β-Catenin Responsive Transcription, Wnt Pathway Inhibitor VIII

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About This Item

실험식(Hill 표기법):
C23H26N2O2S
Molecular Weight:
394.53
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥95% (HPLC)

형태

powder

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

tan

solubility

DMSO: 50 mg/mL

배송 상태

ambient

저장 온도

−20°C

일반 설명

A cell-permeable oxazole compound that acts as a selective CRT (β-catenin responsive transcription) inhibitor (IC50 = 8.2 nM against Wnt3a-dependent SuperTopFlash STF16-luc reporter activity in HEK293 cultures) by interfering with β-cat-TCF4 interaction via direct β-catenin (β-cat) binding, while exhibiting much reduced activity against Hedgehog, Jak/Stat, or Notch signaling pathway-dependent transcription activation. Effectively inhibits cellular expression of CRT target genes, including WISP1, AXN2, and CYCD1, in a dose-dependent manner (25 to 75 µM), and selectively inhibits the proliferation of HCT116 (75 µM), HT29 (75 µM), and several primary human colon cancer cultures (6.25 to 100 µg/ml; average IC50 ~36 µg/ml) that require sustained Wnt/CRT activity for survival.

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Lee, E., et al. 2013. Proc. Natl. Acad. Sci. USA110, 15710.

Gonsalves, F.C., et al. 2011. Proc. Natl. Acad. Sci. USA108, 5954.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


시험 성적서(COA)

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문서 라이브러리 방문

Eugine Lee et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(39), 15710-15715 (2013-09-11)
Androgen receptor (AR) is the major therapeutic target in aggressive prostate cancer. However, targeting AR alone can result in drug resistance and disease recurrence. Therefore, simultaneous targeting of multiple pathways could in principle be an effective approach to treating prostate
Foster C Gonsalves et al.
Proceedings of the National Academy of Sciences of the United States of America, 108(15), 5954-5963 (2011-03-12)
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
Camille Cohen et al.
Nature communications, 15(1), 743-743 (2024-01-26)
Chronic kidney disease (CKD) is a public health problem driven by myofibroblast accumulation, leading to interstitial fibrosis. Heterogeneity is a recently recognized characteristic in kidney fibroblasts in CKD, but the role of different populations is still unclear. Here, we characterize

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