2. Metabolic Enzyme/Protease Apoptosis Stem Cell/Wnt MAPK/ERK Pathway
  3. Pyruvate Carboxylase (PC) Apoptosis β-catenin ERK
  4. ZY-444

ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer.

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

ZY-444

ZY-444 Chemical Structure

CAS No. : 1802650-31-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

ZY-444 Related Antibodies

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ERK ERK1 ERK2 ERK5 ERK8

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Description

ZY-444 is an anti-cancer agent, targeting pyruvate carboxylase (PC). ZY-444 suppresses the Wnt/β-catenin/Snail signaling pathway by blocking nuclear translocation of β-catenin. ZY-444 selectively inhibits proliferation, migration, and invasion and induces apoptosis in cancer cells. ZY-444 exhibits potent anti-tumor in cancer mouse models. ZY-444 can be used for the study of breast cancer, lung cancer (NSCLC), prostate cancer and iodine-refractory thyroid cancer[1][2][3].

In Vitro

ZY-444 (0-10 μM, 48 h) inhibits BCA cell lines (MDA-MB-231 and 4T1) and (PCa cells DU145 and PC3) proliferation, migration, and invasion[1][2].
ZY-444 (0-20 μM, 24 h) significantly induces apoptosis in BCA cells (MDA-MB-231, MCF7, 4T1)[1].
ZY-444 (2-18 μM, 5 h) dose-dependently decreases basal respiration, spare respiratory capacity, and ATP production in BCA cells (MDA-MB-231)[1].
ZY-444 (0-10 μM, 24 h) downregulates total expression of key Wnt/β-catenin/Snail pathway proteins in MDA-MB-231 cells, prevents nuclear translocation of β-catenin, and similar effects are observed in PC-silenced MDA-MB-231 cells[1].
ZY-444 (24-72 h) halves the proliferation ability of TPC-1 and KTC-1 cells, with IC50 values of 3.82 μM (48 h) and 3.34 μM (72 h) for TPC-1 cells, and 3.79 μM (48 h) and 3.69 μM (72 h) for KTC-1 cells[3].
ZY-444 significantly inhibits the activation of the MAPK/ERK signaling pathway in TPC-1 and KTC-1 cells, reducing the expression levels of ERK1/2 and p-ERK1/2[3].

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

ZY-444 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, MCF7, and 4T1cells
Concentration: 0, 5, 6, 8, 10, 15, 20 μM
Incubation Time: 24 h
Result: Induced apoptosis in BCA cells (MDA-MB-231, MCF7).
Increased apoptotic cells.
Upregulated expression of apoptotic biomarkers (cleaved caspase-3, cleaved PARP).
Downregulated anti-apoptotic biomarker (Bcl-2).

Cell Invasion Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 0, 6, 8, 10 μM
Incubation Time: 24 h
Result: Downregulated expression of mesenchymal markers (Snail1, Snail2, Vimentin, N-cadherin) associated with epithelial-mesenchymal transition (EMT).

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MCF7, and 4T1cells
Concentration: MDA-MB-231 cells
Incubation Time: 24 h
Result: Downregulated total expression of β-catenin, c-Myc, and Cyclin D1 in MDA-MB-231 cells.
Prevented nuclear translocation of β-catenin (increased cytosolic β-catenin).
In Vivo

ZY-444 (2.5-5 mg/kg, i.p., daily or every 2 days, 26 days) exhibits potent anti-tumor and anti-metastatic efficacy in orthotopic 4T1 and MDA-MB-231 breast cancer mouse model[1].
ZY-444 (2.5-5 mg/kg, i.p., daily, 24 days) demonstrates excellent anti-prostate cancer efficacy in DU145 xenograft model[2].
ZY-444 (daily, 12 days) exhibits inhibitory effect on the growth of xenograft tumors derived from TPC-1 and KTC-1 PTC cells in 4-week-old female BALB/c nude mice[3].

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

Animal Model: 4T1 or MDA-MB-231 breast cancer cells were orthotopically implanted into female mice[1]
Dosage: 2.5, 5 mg/kg
Administration: i.p., daily or every 2 days, 26 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Upregulated apoptotic biomarkers and downregulated mesenchymal biomarkers in primary tumors.
Animal Model: DU145 cells (5 × 107) were subcutaneously implanted into the right flanks of 6-8-week-old male NOD-scid mice[2]
Dosage: 2.5, 5 mg/kg
Administration: i.p., daily, 24 days
Result: Achieved tumor growth inhibition.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Upregulated the expression of TNFAIP3 and IKBα, while downregulated the expression of RIPK1, IKKα, p-IKBα, NF-κB, and p-p65.
Molecular Weight

444.59

Formula

C26H28N4OS
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)CNC1=NC=CC(NCC2=CC=C(C3=CC=C(OCC4=CC=CC=C4)C=C3)S2)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (224.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2493 mL 11.2463 mL 22.4926 mL
5 mM 0.4499 mL 2.2493 mL 4.4985 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.51%

SDS (251 KB)

COA (244 KB) HNMR (124 KB) LCMS (90 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2493 mL 11.2463 mL 22.4926 mL 56.2316 mL
5 mM 0.4499 mL 2.2493 mL 4.4985 mL 11.2463 mL
10 mM 0.2249 mL 1.1246 mL 2.2493 mL 5.6232 mL
15 mM 0.1500 mL 0.7498 mL 1.4995 mL 3.7488 mL
20 mM 0.1125 mL 0.5623 mL 1.1246 mL 2.8116 mL
25 mM 0.0900 mL 0.4499 mL 0.8997 mL 2.2493 mL
30 mM 0.0750 mL 0.3749 mL 0.7498 mL 1.8744 mL
40 mM 0.0562 mL 0.2812 mL 0.5623 mL 1.4058 mL
50 mM 0.0450 mL 0.2249 mL 0.4499 mL 1.1246 mL
60 mM 0.0375 mL 0.1874 mL 0.3749 mL 0.9372 mL
80 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7029 mL
100 mM 0.0225 mL 0.1125 mL 0.2249 mL 0.5623 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZY-4441802650-31-2ZY444ZY 444Pyruvate Carboxylase (PC)Apoptosisβ-cateninERKPyruvate Carboxylase Beta cateninExtracellular signal regulated kinasesbreast cancerlung cancer (NSCLC)prostate canceriodine-refractory thyroid cancer,4T1MDA-MB-231,β-cateninInhibitorinhibitorinhibit

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