MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

ZW4864

CAS No. : 2632259-93-7

MCE 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 K_i 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：CHIR-99021  |  XAV-939  |  ICG-001  |  Salinomycin  |  SKL2001  |  Toxoflavin  |  LF3  |  FH535  |  MSAB  |  Tegatrabetan  |  WAY-262611  |  PNU-74654  |  Triptonide  |  KYA1797K  |  L-Quebrachitol  |  NRX-252262  |  β-catenin-IN-2  |  Pamidronic acid  |  (E)-Ferulic acid  |  Nefopam hydrochloride  |  FzM1.8  |  Astragaloside I  |  KY19382  |  CWP232228  |  KY1220  |  Cardiogenol C hydrochloride  |  WIKI4

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。