ZW4864 | MedChemExpress (MCE)
品牌 | 厂商性质 | 产地 | 货期 | 价格 |
---|---|---|---|---|
MedChemExpress (MCE) | 生产商 | 美国 | 现货 | 8500 |
性能特点
ZW4864 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 抑制
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
5 mg | 2632259-93-7 | ¥5,000.00 | 询底价 |
10 mg | 2632259-93-7 | ¥8,500.00 | 询底价 |
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CAS No. : 2632259-93-7
MCE 国际站:ZW4864
产品活性:ZW4864 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 抑制 β catenin/BCL9 PPI 的 Ki 值为0.76 μM,IC50 值为 0.87 μM。
研究领域:Stem Cell/Wnt
作用靶点:β-catenin
In Vitro: ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) decreases the expression levels of Axin2 and cyclin D1 proteins.
ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A and MDA-MB-468 cells) selectively triggeres rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.
ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) suppresses the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells.
ZW4864 binds with β-catenin and selectively disrupts the protein−protein interaction (PPI) between B-cell lymphoma 9 (BCL9) and β-catenin while sparing the β-catenin/E-cadherin PPI. ZW4864 dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC50 of 11 μM. ZW4864 also dose-dependently suppresses the TOPFlash luciferase activities in SW480 and Wnt 3a-activated MDA-MB-468 cells with the IC50s of 7.0 and 6.3 μM, respectively. ZW4864 selectively suppresses transactivation of β-catenin signaling.
In Vivo: ZW4864 (20 mg/kg; p.o.) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %.
ZW4864 (90 mg/kg; p.o.) shows a variation in tumor growth in mice.
ZW4864 shows good pharmacokinetic properties and effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse model.
相关产品:Bioactive Compound Library Plus | Stem Cell Signaling Compound Library | Wnt/Hedgehog/Notch Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Neuroprotective Compound Library | Anti-Breast Cancer Compound Library | Anti-Blood Cancer Compound Library | Transcription Factor-Targeted Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Antihypertensive Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | CDK8-IN-11 | FzM1 | Wnt/β-catenin agonist 3 hydrochloride | Pamidronic acid | NRX-252114 | (E)-Ferulic acid | UU-T01 | L-Quebrachitol | HLY78 | Wnt/β-catenin agonist 2 | Cardiogenol C hydrochloride | Laduviglusib (GMP) | FzM1.8 | iCRT-5 | NRX-252262 | NLS-StAx-h TFA | UU-T02 | Dinactin | Triptonide | Astragaloside I | CWP232228 | β-catenin-IN-2 | SKL2001 | Chrysomycin A | Nefopam-d3 | Cardamonin | DK419 | MSAB
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货号: HY-132300
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途