2. Protein Tyrosine Kinase/RTK JAK/STAT Signaling Metabolic Enzyme/Protease NF-κB Stem Cell/Wnt
  3. FAK EGFR MMP NF-κB SDCBP
  4. PDZ1i

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.

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

PDZ1i

PDZ1i Chemical Structure

CAS No. : 2083618-79-3

Size Price Stock Quantity
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

PDZ1i Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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[1][2][3].

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.

PDZ1i Related Antibodies

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).
Molecular Weight

538.56

Formula

C28H26N8O4
CAS No.
Appearance

Solid

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
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 (185.68 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 1.8568 mL 9.2840 mL 18.5680 mL
5 mM 0.3714 mL 1.8568 mL 3.7136 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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
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 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
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PDZ1i Related Classifications

Help & FAQs
  • 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:

PDZ1i2083618-79-3113B7FAKEGFRMMPNF-κBSDCBPPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseEpidermal growth factor receptorErbB-1HER1Matrix metalloproteinasesNuclear factor-κBNuclear factor-kappaBSyntenin Syndecan Binding Protein (SDCBP)/MDA-9T98G cellsU87 cellsU1242 cellsGBM cellsbrain tumorglioblastoma multiforme (GBM)syndecan-binding protein (SDCBP)Melanoma differentiation-associated gene (MDA)Inhibitorinhibitorinhibit

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