Art. -Nr.: HY-124813

PDZ1i

(Synonyms: 113B7)

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PDZ1i (113B7) is a inhibitor of MDA-9/Syntenin, with selective binding to the PDZ1 domain. PDZ1i inhibits radiation-induced invasion of glioblastoma (GBM) cells, radiosensitizes GBM cells, and impairs GBM-related signaling pathways (including Src/EphA2, EGFRvIII/FAK, and NF-κB). PDZ1i reduces radiation-induced secretion of invasion-related proteases (MMP-2, MMP-9, ADAM9). PDZ1i shows anti-tumor effects in nude mice bearing intracranial U1242-luc xenografts or GBM xenografts. PDZ1i can be used for the study of glioblastoma (GBM), breast cancer and prostate cancer.

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Reinheit: 99.29%
CAS. Nr.: 2083618-79-3
Formel: C₂₈H₂₆N₈O₄
Molecular Weight:538.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PDZ1i Chemical Structure

CAS. Nr.: 2083618-79-3

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle EGFR Isoform-spezifische Produkte anzeigen :

Alle MMP Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

PDZ1i (50 μM, 2 h) does not further radiosensitize immortalized primary human fetal astrocytes (Im-PHFAs) but markedly enhances radiosensitivity of U87 GBM cells, and significantly decreases proliferation of U87 cells when combined with radiation^[1].
PDZ1i (50 μM, 2 h) abolishes radiation-induced invasion gains in U87 GBM cells^[1].
PDZ1i (2 h) significantly reduces phospho-EGFR (Y845) levels in both non-radiated and radiated U87-EGFRvIII GBM cells, nullifies radiation-enhanced FAK activation (phospho-FAK Y576/577), and decreases radiation-induced NF-κB activation (phospho-p65) in U87-EGFRvIII cells^[1].
PDZ1i disrupts the interaction between MDA-9/Syntenin and EGFR in both non-radiated and radiated GBM cells^[1].
PDZ1i (50 μM, 2 h) reduces radiation-induced increases in the secretion of MMP-2, MMP-9, cathepsin family members, and ADAM9 in U1242 GBM cells^[1].
PDZ1i (50 μM, 24 h) effectively crosses the human brain microvascular endothelial cell (HBMEC) barrier and inhibits the invasion of GBM6 cells, with comparable efficacy to direct pretreatment of GBM6 cells^[1].
PDZ1i (5 μM) reduces the expression levels of CD44v3 and heparan sulfate (HS) on the surface of radiation-induced extracellular vesicles (IR-tEVs) derived from breast cancer MDA-MB-231 cells, and decreases the total production of IR-tEVs^[3].

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

Cell Viability Assay^[1]

Cell Line:

U87 GBM cells
Concentration:

50 μM
Incubation Time:

2 h
Result:

Abolished radiation-induced invasion gains in U87 GBM cells.

In Vivo

PDZ1i (30 mg/kg, i.p., three times per week, 2 weeks) demonstrates efficacy in reducing tumor size in nude mice bearing intracranial GBM6 xenografts^[1].
PDZ1i (30 mg/kg, i.p., 2 h before radiation, 4 consecutive days) shows enhanced anti-tumor effects when combined with radiation (2.5 Gy/day, 4 days) in nude mice bearing intracranial U1242-luc xenografts^[1].

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

Animal Model:

GBM6 cells were intracranially implanted into nude mice^[1]
Dosage:

30 mg/kg
Administration:

i.p., three times per week, 2 weeks
Result:

Demonstrated efficacy in reducing tumor size, increasing tumor demarcation, and extending survival.

Animal Model:

U1242-luc cells were intracranially implanted into nude mice under anesthesia^[1]
Dosage:

30 mg/kg
Administration:

i.p., 2 h before radiation, 4 consecutive days
Result:

Showed enhanced anti-tumor effects when combined with radiation (2.5 Gy/day, 4 days).

Chemical Information

CAS. Nr. 2083618-79-3
Appearance Solid
Molecular Weight 538.56
Formel C₂₈H₂₆N₈O₄
Color White to off-white
SMILES

O=C1N2C(NC3=C1CCC3)=NC(C(NC(C=C4C)=C(C=C4NC(CCC5=NN=C(C6=CC=CC=C6)O5)=O)C)=O)=N2
Synonyms

113B7
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (185.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8568 mL

9.2840 mL

18.5680 mL

5 mM

0.3714 mL

1.8568 mL

3.7136 mL

10 mM

0.1857 mL

0.9284 mL

1.8568 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (4.64 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.64 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: 2.5 mg/mL (4.64 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[1]. Kegelman TP, et al. Inhibition of radiation-induced glioblastoma invasion by genetic and pharmacological targeting of MDA-9/Syntenin. Proc Natl Acad Sci U S A. 2017 Jan 10;114(2):370-375. [Content Brief]

[2]. Das D, et al. Suppression of Prostate Cancer Pathogenesis Using an MDA-9/Syntenin (SDCBP) PDZ1 Small-Molecule Inhibitor. Mol Cancer Ther. 2019 Nov;18(11):1997-2007. [Content Brief]

[3]. Clark GC, et al. Radiation induces ESCRT pathway dependent CD44v3+ extracellular vesicle production stimulating pro-tumor fibroblast activity in breast cancer. Front Oncol. 2022 Aug 29;12:913656. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	1.8568 mL	9.2840 mL	18.5680 mL	46.4201 mL
	5 mM	0.3714 mL	1.8568 mL	3.7136 mL	9.2840 mL
	10 mM	0.1857 mL	0.9284 mL	1.8568 mL	4.6420 mL
	15 mM	0.1238 mL	0.6189 mL	1.2379 mL	3.0947 mL
	20 mM	0.0928 mL	0.4642 mL	0.9284 mL	2.3210 mL
	25 mM	0.0743 mL	0.3714 mL	0.7427 mL	1.8568 mL
	30 mM	0.0619 mL	0.3095 mL	0.6189 mL	1.5473 mL
	40 mM	0.0464 mL	0.2321 mL	0.4642 mL	1.1605 mL
	50 mM	0.0371 mL	0.1857 mL	0.3714 mL	0.9284 mL
	60 mM	0.0309 mL	0.1547 mL	0.3095 mL	0.7737 mL
	80 mM	0.0232 mL	0.1161 mL	0.2321 mL	0.5803 mL
	100 mM	0.0186 mL	0.0928 mL	0.1857 mL	0.4642 mL

Keywords

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PDZ1i

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle EGFR Isoform-spezifische Produkte anzeigen

Alle MMP Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PDZ1i Related Classifications

HY-124813 Related Classifications