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Cat. No.: HY-191349

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ZD37-28R

ZD37-28R is a β-catenin/BCL9 interaction inhibitor with an IC₅₀of 1.169 μM for β-catenin. ZD37-28R inhibits SREBP1 and c-MYC expression and induces Apoptosis. ZD37-28R downregulates ACC1, FASN, ACLY, and SCD1. ZD37-28R reduces lipid accumulation. ZD37-28R shows antitumor effects in subcutaneous and orthotopic glioma models and enhances the effect of Temozolomide (HY-17364).

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

Formula: C₃₃H₄₂N₆O₄
Molecular Weight:586.72

Storage:

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

Data Sheet (279 KB)

ZD37-28R Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
U-251	IC50	2.055 μM	Inhibition of β-catenin-dependent TCF/LEF transcriptional activity in human U251 glioma cells by TCF/LEF luciferase reporter assay. Inhibition of β-catenin-dependent TCF/LEF transcriptional activity in human U251 glioma cells by TCF/LEF luciferase reporter assay.	5453196
U-251	IC50	4.892 μM	Inhibition of AXIN2 mRNA expression in human U251 glioma cells after 24 hrs incubation measured by quantitative real-time PCR. Inhibition of AXIN2 mRNA expression in human U251 glioma cells after 24 hrs incubation measured by quantitative real-time PCR.	5453196
U-87MG ATCC	IC50	6.667 μM	Inhibition of AXIN2 mRNA expression in human U87-MG glioma cells after 24 hrs incubation measured by quantitative real-time PCR. Inhibition of AXIN2 mRNA expression in human U87-MG glioma cells after 24 hrs incubation measured by quantitative real-time PCR.	5453196
U-87MG ATCC	IC50	2.165 μM	Antiproliferative activity against human U87-MG glioma cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay. Antiproliferative activity against human U87-MG glioma cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.	5453196
U-251	IC50	15.82 μM	Antiproliferative activity against human U251 glioma cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay. Antiproliferative activity against human U251 glioma cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.	5453196
GL261	IC50	5.701 μM	Antiproliferative activity against murine GL261 glioma cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay. Antiproliferative activity against murine GL261 glioma cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.	5453196
U-87MG ATCC	IC50	3.154 μM	Inhibition of wild-type human U87-MG glioma cell viability in a BCL9-dependent viability assay. Inhibition of wild-type human U87-MG glioma cell viability in a BCL9-dependent viability assay.	5453196

In Vitro

Anti-cancerApoptosisLipid MetabolismOthers

Anti-cancer

ZD37-28R (2.5 μM) disrupts the formation of the BCL9/β-catenin complex in U87-MG cells at concentrations as low as 2.5 μM^[1].
ZD37-28R inhibits β-catenin-dependent TCF/LEF transcriptional activity in U251 cells with an IC₅₀ of 2.055 μM^[1].
ZD37-28R (24 h) reduces AXIN2 mRNA expression in U251 and U87-MG cells, with IC₅₀ values of 4.892 and 6.667 μM, respectively^[1].
ZD37-28R (48 h) inhibits glioma cell proliferation, showing the strongest CCK-8 potency in U87-MG cells with an IC₅₀ of 2.165 μM^[1].
ZD37-28R (5 μM) almost completely inhibits the growth of U87-MG and GL261 cells^[1].
ZD37-28R (0-10 μM; 2 weeks) reduces clonogenic survival of U87-MG and U251 cells in a dose-dependent manner^[1].
ZD37-28R reduces the Ki67-positive proliferating cell population in U87-MG and U251 cells^[1].
ZD37-28R inhibits U87-MG viability in a BCL9-dependent manner, with an IC₅₀ of 3.154 μM against the wild type, and the growth inhibitory effect disappears after BCL9 knockdown^[1].
ZD37-28R (0-5 μM; 12-24 h) inhibits scratch-wound migration of U87-MG and U251 cells^[1].
ZD37-28R (0-5 μM; 24 h) inhibits Transwell migration of U87-MG and U251 cells in a concentration-dependent manner^[1].
ZD37-28R reverses EMT-like marker expression and reduces PRRX1, PITX2, and SNAI2 in U87-MG and U251 cells^[1].

Anti-cancer

Apoptosis

ZD37-28R (2.5-10 μM; 24 h) induces apoptosis in U87-MG and U251 cells in a dose-dependent manner^[1].

Anti-cancer

Lipid Metabolism

ZD37-28R (5 μM; 24 h) reduces lipid accumulation in U87-MG and U251 cells^[1].

Others

ZD37-28R binds β-catenin with potent affinity, with an FP IC₅₀ of 1.169 μM^[1].

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

Cell Migration Assay ^[1]

Cell Line:

U87-MG and U251 glioma cells
Concentration:

0, 2.5, 5 μM
Incubation Time:

12 and 24 h
Result:

Lower migration rates at 12 and 24 h were observed in U87-MG and U251 cells.
U251 24 h migration was also reduced.

Cell Migration Assay ^[1]

Cell Line:

U87-MG and U251 glioma cells
Concentration:

0, 2.5, 5, and 10 μM
Incubation Time:

24 h
Result:

Glioma cell migration across the porous membrane was inhibited in a concentration-dependent manner.

In Vivo

Anti-cancer

ZD37-28R (15-25 mg/kg) dose-dependently inhibits subcutaneous U87-MG glioma growth in nude mice, with 25 mg/kg showing greater antitumor activity than TMZ^[1].
ZD37-28R (25 mg/kg; every other day; 21 days) alone reduces orthotopic U251 glioma tumor burden and enhances TMZ efficacy in nude mice^[1].

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

Animal Model:

nude mice (nu/nu; female; 3-4 weeks old; 15-18 g)^[1]
Dosage:

25 mg/kg (single-agent); 25 mg/kg combined with TMZ 25 mg/kg
Administration:

every other day; for 21 days
Result:

After 21 days of dosing, tumors in the 25 mg/kg single-agent group were smaller than those in the control group.
TMZ single-agent showed a stronger effect than the 25 mg/kg single-agent alone.
The combination produced the greatest antitumor effect among the dosing groups; the combination produced stronger tumor suppression than either single agent.

Related Protocols :

Chemical Information

Molecular Weight 586.72
Formula C₃₃H₄₂N₆O₄
SMILES

CC(OC1=CC(N2CCC[C@@H](C2)NC(N(C3CC3)CC4=CC=C(C=C4)C5=CNN=C5)=O)=CC=C1)(C(N6CC[C@H](C6)O)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li H, et al. Pharmacological Study of Novel Small-Molecule Inhibitors Targeting B-Cell Lymphoma 9/β-Catenin in the Treatment of Glioma[J]. ACS Pharmacology & Translational Science.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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ZD37-28R