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

PU-WS13 

Cat. No.: HY-18680 Purity: 95.69%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
50 mg USD 672 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

Molecular Weight

411.35

Formula

C₁₇H₂₀Cl₂N₆S

CAS No.

1454619-14-7

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)

*"≥" 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
10 mM 0.2431 mL 1.2155 mL 2.4310 mL
*Please refer to the solubility information to select the appropriate solvent.
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
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Keywords:

PU-WS13HSPHeat shock proteinsInhibitorinhibitorinhibit

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