Beta-catenin
β-Catenin is a multifunctional protein with a central role in physiological homeostasis. Its aberrant high expression leads to various diseases including cancer. β-Catenin is the mammalian homologue of the drosophila armadillo gene. It acts both as a transcriptional co-regulator and an adaptor protein for intracellular adhesion. Wnt is the chief regulator of β-catenin, which is a family of 19 glycoproteins to regulate both the β-catenin-dependent (canonical Wnt) and -independent (non-canonical Wnt) signaling pathways. In canonical Wnt pathway, Dsh, β-catenin, Glycogen Synthase Kinase 3 beta (GSK3β), adenomatous polyposis coli (APC), AXIN, and T-cell factor (TCF)/lymphoid enhancement factor (LEF) have been identified as signal transducers of the canonical Wnt pathway, in which β-catenin is a core molecule. In the absence of Wnt ligands, β-catenin is kept at a low level through the ubiquitin proteasome system (UPS).
β-Catenin is recruited into a destruction complex that contains APC and AXIN, which facilitates the phosphorylation of β-catenin by casein kinase 1 (CK1) and then GSK3β. This leads to the ubiquitylation and proteasomal degradation of β-catenin. Upon Wnt activation or genetic mutations of Wnt components, β-catenin accumulates in the cytoplasm and then translocates into the nucleus. Consequently, it binds to LEF-1/TCF4 and some other co-regulators to promote the transcription of target genes such as Jun, c-Myc and CyclinD-1 in a tissue specific manner, most of which encode oncoproteins. In more than half of all cancer cases, such as colorectal carcinoma, breast cancer, liver carcinoma, melanoma and leukemia, β-catenin accumulates within the nucleus or cytoplasm.
References
1.Shuang Shang,et al. Oncotarget. 2017 May 16; 8(20): 33972–33989.
β-Catenin is recruited into a destruction complex that contains APC and AXIN, which facilitates the phosphorylation of β-catenin by casein kinase 1 (CK1) and then GSK3β. This leads to the ubiquitylation and proteasomal degradation of β-catenin. Upon Wnt activation or genetic mutations of Wnt components, β-catenin accumulates in the cytoplasm and then translocates into the nucleus. Consequently, it binds to LEF-1/TCF4 and some other co-regulators to promote the transcription of target genes such as Jun, c-Myc and CyclinD-1 in a tissue specific manner, most of which encode oncoproteins. In more than half of all cancer cases, such as colorectal carcinoma, breast cancer, liver carcinoma, melanoma and leukemia, β-catenin accumulates within the nucleus or cytoplasm.
References
1.Shuang Shang,et al. Oncotarget. 2017 May 16; 8(20): 33972–33989.
Wnt/Notch/Hedgehog
Beta-catenin
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CWP-232228
产品货号 : M16979
cas no: ——
CWP-232228 是一种高效小分子 Wnt/β-catenin 信号传导抑制剂,针对细胞核中的 β-catenin/Tcf4 相互作用。 -
T-155535
产品货号 : M16627
cas no: 925001-05-4
T-155535 是一种小分子抑制剂,可有效抑制 β-catenin/Tcf4 相互作用,AlphaScreen 测定中 Ki 为 21 uM。 -
SKL2001
产品货号 : M16533
cas no: 909089-13-0
SKL2001 是 Wnt/β-catenin 通路的特异性小分子激活剂(激动剂)。 -
R-999636
产品货号 : M16529
cas no: 90833-53-7
R-999636 是一种小分子抑制剂,可有效抑制 β-catenin/Tcf4 相互作用,在 FP 测定中 Ki 为 8.8 uM。 -
iCRT-3
产品货号 : M16485
cas no: 901751-47-1
iCRT-3 是一种选择性、细胞渗透性 β-连环蛋白响应性转录 (CRT) 抑制剂,IC50 为 8.2 nM。