2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. HSP
  4. PU-WS13

PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 μM.

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

PU-WS13 Chemical Structure

PU-WS13 Chemical Structure

CAS No. : 1454619-14-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 119 In-stock
Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Solid
5 mg USD 108 In-stock
10 mg USD 156 In-stock
50 mg USD 672 In-stock
100 mg   Get quote  
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Customer Review

Based on 2 publication(s) in Google Scholar

PU-WS13 Related Antibodies

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HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PU-WS13 is a selective Grp94 inhibitor, with an EC50 of 0.22 μM.

IC50 & Target[1]

GRP94

0.22 μM (EC50)

HSP90α

27.3 μM (EC50)

HSP90β

41.8 μM (EC50)

TRAP-1

7.3 μM (EC50)

In Vitro

PU-WS13 is a Grp94 inhibitor, with an EC50 of 0.22 μM. PU-WS13 also slightly suppresses Hsp90α, Hsp90β and Trap-1, with EC50s of 27.3, 41.8 and 7.3 μM, respectively. PU-WS13 (2.5-20 μM) shows no toxicity on two nonmalignant cell lines. PU-WS13 (15 μM) disrupts the circular architecture of HER2 at the plasma membrane of SKBr3 cells mediated through Grp94. PU-WS13 inhibits Grp94, and the inhibition induces apoptosis in and reduce the viability of HER2 overexpressing breast cancer cells[1].

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

PU-WS13 Related Antibodies
Molecular Weight

411.35

Formula

C17H20Cl2N6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(NCCCN1C(SC2=CC(Cl)=CC(Cl)=C2)=NC3=C(N)N=CN=C13)C
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 : ≥ 40 mg/mL (97.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4310 mL 12.1551 mL 24.3102 mL
5 mM 0.4862 mL 2.4310 mL 4.8620 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
=
Concentration
×
Volume
×
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 (6.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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 (6.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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

Purity: 99.94%

COA (253 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

The Hsp90 FP competition assays are carried out in black 96-well micro-plates in a total volume of 100 μL in each well. A stock of 10 μM cy3B-GM and PU-FITC3 is prepared in DMSO and diluted with Felts buffer (20 mM Hepes (K), pH 7.3, 50 mM KCl, 2 mM DTT, 5 mM MgCl2, 20 mM Na2MoO4 and 0.01% NP40 with 0.1 mg/mL BGG). To each well is added the fluorescent dye-labeled Hsp90 ligand (6 nM cy3B-GM for Hsp90α, Hsp90β and Grp94 and 3 nM PU-FITC3 for Trap-1), protein (10 nM Hsp90α, 10 nM Hsp90β, 10 nM Grp94, 30 nM Trap-1) and tested inhibitor (including PU-WS13, initial stock in DMSO) in a final volume of 100 μL Felts buffer. Compounds are added in duplicate or triplicate wells. For each assay, background wells (buffer only), tracer controls (free, fluorescent dye-labeled Hsp90 ligand only) and bound controls (fluorescent dye-labeled Hsp90 ligand in the presence of protein) are included on each assay plate. The assay plate is incubated on a shaker at 4°C for 24 h, and the FP values (in mP) are measured. The fraction of fluorescent dye-labeled Hsp90 ligand bound to Hsp90 is correlated to the mP value and plotted against values of competitor concentrations. The inhibitor concentration at which 50% of bound fluorescent dye-labeled Hsp90 ligand is displaced is obtained by fitting the data. For cy3B-GM, an excitation filter at 530 nm and an emission filter at 580 nm are used with a dichroic mirror of 561 nm. For PU-FITC3, an excitation filter at 485 nm and an emission filter at 530 nm are used with a dichroic mirror of 505 nm. All of the experimental data are analyzed, and binding affinity values are given as relative binding affinity values (EC50, concentration at which 50% of fluorescent ligand is competed off by compound)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Cells are treated for 72 h with inhibitors (including PU-WS13) or transfected with Grp94 siRNA or control siRNA, and their viability is assessed using CellTiter-Glo luminescent Cell Viability Assay. The method determines the number of viable cells in culture based on quantification of the ATP present, which signals the presence of metabolically active cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 2.4310 mL 12.1551 mL 24.3102 mL 60.7755 mL
5 mM 0.4862 mL 2.4310 mL 4.8620 mL 12.1551 mL
10 mM 0.2431 mL 1.2155 mL 2.4310 mL 6.0775 mL
15 mM 0.1621 mL 0.8103 mL 1.6207 mL 4.0517 mL
20 mM 0.1216 mL 0.6078 mL 1.2155 mL 3.0388 mL
25 mM 0.0972 mL 0.4862 mL 0.9724 mL 2.4310 mL
30 mM 0.0810 mL 0.4052 mL 0.8103 mL 2.0258 mL
40 mM 0.0608 mL 0.3039 mL 0.6078 mL 1.5194 mL
50 mM 0.0486 mL 0.2431 mL 0.4862 mL 1.2155 mL
60 mM 0.0405 mL 0.2026 mL 0.4052 mL 1.0129 mL
80 mM 0.0304 mL 0.1519 mL 0.3039 mL 0.7597 mL
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PU-WS13 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:

PU-WS131454619-14-7HSPHeat shock proteinsInhibitorinhibitorinhibit

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