2. Apoptosis Cell Cycle/DNA Damage
  3. MDM-2/p53 DNA Alkylator/Crosslinker
  4. PK11000

PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities.

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

PK11000 Chemical Structure

PK11000 Chemical Structure

CAS No. : 38275-34-2

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 48 In-stock
Solution
10 mM * 1 mL in DMSO USD 48 In-stock
Solid
5 mg USD 43 In-stock
10 mg USD 70 In-stock
25 mg USD 140 In-stock
50 mg USD 224 In-stock
100 mg USD 360 In-stock
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PK11000 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities[1].

IC50 & Target

p53[1]
In Vitro

PK11000 (0-120 μM, 24 h) mildly inhibits mutant p53 cancer cells[1].
PK11000 (0-50 μM, 5 d) shows anti-proliferation effects of breast cell lines[2].

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

PK11000 Related Antibodies

Cell Viability Assay[1]

Cell Line: WI-38, HUH-6, NUGC-4, SJSA-1, HUH-7, NUGC-3, SW480 and MKN1 cells
Concentration: 0-120 μM
Incubation Time: 24 hours
Result: Inhibited NUGC-3 cells mildly.

Cell Proliferation Assay[2]

Cell Line: UACC812, BT474, ZR-75-1, SUM 159, MDA-MD-468, MDA-MD-453, T47D, Hs578T(i8), MCF7, HCC1937, JimT1, BT20, HCC1143, BT549, SKBR3, MCF12A, MCF10A cells
Concentration: 0-50 μM
Incubation Time: 5 days
Result: Inhibited breast cell lines with IC50 values ranging from 2.5 to >50 µM.
Molecular Weight

236.63

Formula

C6H5ClN2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NC(S(=O)(C)=O)=NC=C1Cl)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (422.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 25 mg/mL (105.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2260 mL 21.1300 mL 42.2601 mL
5 mM 0.8452 mL 4.2260 mL 8.4520 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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

×
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 (10.57 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 (10.57 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 20 mg/mL (84.52 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.2260 mL 21.1300 mL 42.2601 mL 105.6502 mL
5 mM 0.8452 mL 4.2260 mL 8.4520 mL 21.1300 mL
10 mM 0.4226 mL 2.1130 mL 4.2260 mL 10.5650 mL
15 mM 0.2817 mL 1.4087 mL 2.8173 mL 7.0433 mL
20 mM 0.2113 mL 1.0565 mL 2.1130 mL 5.2825 mL
25 mM 0.1690 mL 0.8452 mL 1.6904 mL 4.2260 mL
30 mM 0.1409 mL 0.7043 mL 1.4087 mL 3.5217 mL
40 mM 0.1057 mL 0.5283 mL 1.0565 mL 2.6413 mL
50 mM 0.0845 mL 0.4226 mL 0.8452 mL 2.1130 mL
60 mM 0.0704 mL 0.3522 mL 0.7043 mL 1.7608 mL
80 mM 0.0528 mL 0.2641 mL 0.5283 mL 1.3206 mL
100 mM 0.0423 mL 0.2113 mL 0.4226 mL 1.0565 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PK11000 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:

PK1100038275-34-2PK 11000PK-11000MDM-2/p53DNA Alkylator/Crosslinkermutant p53 cancer cellsanti-proliferation activity,WI-38HUH-6NUGC-4SJSA-1HUH-7NUGC-3SW480MKN1UACC812BT474ZR-75-1SUM 159MDA-MD-468MDA-MD-453T47DHs578T(i8)MCF7HCC1937JimT1BT20HCC1143BT549SKBR3MCF12AMCF10AInhibitorinhibitorinhibit

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