1. Stem Cell/Wnt
  2. β-catenin
  3. ZW4864

ZW4864 

Cat. No.: HY-132300
Handling Instructions

ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.

For research use only. We do not sell to patients.

ZW4864 Chemical Structure

ZW4864 Chemical Structure

CAS No. : 2632259-93-7

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Description

ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM[1].

IC50 & Target

IC50: 0.87 μM (β catenin/BCL9 PPI)[1].
Ki: 0.76 μM(β catenin/BCL9 PPI)[1]

In Vitro

ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) decreases the expression levels of Axin2 and cyclin D1 proteins[1].
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[1].
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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: SW480 and MBA-MD-231 cells
Concentration: 10~40 μM
Incubation Time: 24 hours
Result: Decreased the expression levels of Axin2 and cyclin D1 proteins.

Apoptosis Analysis[1]

Cell Line: MDA-MB231, MCF10A and MDA-MB-468 cells
Concentration: 10~40 μM
Incubation Time: 72 hours
Result: Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.

RT-PCR[1]

Cell Line: SW480 and MBA-MD-231 cells
Concentration: 10~40 μM
Incubation Time: 24 hours
Result: Suppressed 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.
In Vivo

ZW4864 (20 mg/kg; p.o.) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %[1].
ZW4864 (90 mg/kg; p.o.) shows a variation in tumor growth in mice[1].
ZW4864 shows good pharmacokinetic properties and effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.
Animal Model: Mice[1]
Dosage: 90 mg/kg
Administration: P.o.
Result: Showed a variation in tumor growth in mice.
Molecular Weight

607.19

Formula

C₃₃H₄₃ClN₆O₃

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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