Wnt/beta/catenin
The Wnt/β-catenin pathway is activated when a Wnt ligand binds to a seven-pass transmembrane Frizzled (Fz) receptor and its co-receptor, low-density lipoprotein receptor related protein 6 (LRP6) or its close relative LRP5. The formation of a likely Wnt-Fz-LRP6 complex together with the recruitment of the scaffolding protein Dishevelled (Dvl) results in LRP6 phosphorylation and activation and the recruitment of the Axin complex to the receptors. These events lead to inhibition of Axin-mediated β-catenin phosphorylation and thereby to the stabilization of β-catenin, which accumulates and travels to the nucleus to form complexes with TCF/LEF and activates Wnt target gene expression.Two distinct classes of Wnt inhibitors are the Dickkopf (Dkk) family and the Wise/SOST family. Dkk proteins, exemplified by Dkk1, are LRP5/6 ligands/antagonists and are considered specific inhibitors for Wnt/β-catenin signaling.
References
Bryan T. MacDonald et al.Dev Cell. 2009 Jul; 17(1): 9–26.
References
Bryan T. MacDonald et al.Dev Cell. 2009 Jul; 17(1): 9–26.
Wnt/Notch/Hedgehog
Wnt/beta/catenin
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ZW4864 free base
产品货号 : M37644
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ZW4864 (free base) 是一种具有口服活性和选择性的 β catenin/ B-Cell lymphoma 9 蛋白-蛋白相互作用 (β catenin/BCL9 PPI) 抑制剂。ZW4864 (free base) 抑制 β catenin/BCL9 PPI 的 Ki 值为 0.76 μM,IC50 值为 0.87 μM。 -
TNIK-IN-3
产品货号 : M37634
cas no: 2754265-25-1
TNIK-IN-3 (化合物 21k) 是一种有效,选择性和具有口服活性的 TNIK 抑制剂,IC50 值为 0.026 μM。TNIK-IN-3 还可以抑制 Flt4 (IC50=0.030 μM),Flt1 (IC50=0.191 μM) 和 DRAK1 (IC50=0.411 μM)。TNIK-IN-3 可用于结直肠癌的研究。 -
TNKS-2-IN-2
产品货号 : M37091
cas no: 2719726-91-5
TNKS-2-IN-2 是一种有效的 TNKS2 选择性抑制剂,其 IC50 为 22 nM。 -
TNIK-IN-7
产品货号 : M37080
cas no: 1417795-24-4
TNIK-IN-7 (Compound 8) 是一种 Traf2 和 Nck 相互作用激酶 (TNIK) 抑制剂,IC50 为 11 nM,具有抗肿瘤活性。 -
TNKS-2-IN-1
产品货号 : M37041
cas no: 4765-59-7
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