Art. -Nr.: HY-179560

PMV6-PEG4-BI2536

Name: PMV6-PEG4-BI2536
Brand: MedChemExpress
SKU: HY-179560
Price: 480.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53^Y220C-PLK1 ternary complex (EC₅₀ = 1.4 μM). PMV6-PEG4-BI2536 causes PLK1 mislocalization and inhibits PLK1 activity, inducing G2/M phase arrest and apoptosis in p53^Y220C-mutant cells, while sparing cells with wild-type TP53. PMV6-PEG4-BI2536 can be used in research on uterine, gastric, pancreatic, prostate, and breast cancers harboring the p53^Y220C mutation. PMV6-PEG4-BI2536 is composed of PMV6 (a p53^Y220C mutant-binding ligand), PEG4 (a linker), and BI2536 (HY-159493) (a PLK inhibitor).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.47%
Formel: C₅₉H₇₅F₃N₁₀O₁₁S
Molecular Weight:1189.35

Speicherung:

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

PMV6-PEG4-BI2536 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

HY-169369
TRAP-1

p53 Transcriptional Activator

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

PLK1

Caspase 3

Caspase-7

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NUGC-3	IC50	1713.0956 nM	Significantly inhibits cell proliferation. Significantly inhibits cell proliferation.	41184486
MFE-296	IC50	4320.9284 nM	Significantly inhibits cell proliferation. Significantly inhibits cell proliferation.	41184486
BXPC-3	IC50	8251.9582 nM	Significantly inhibits cell proliferation. Significantly inhibits cell proliferation.	41184486
MCF7	IC50	1268.3102 nM	Significantly inhibits cell proliferation. Significantly inhibits cell proliferation.	41184486
Huh-7	IC50	200000 nM	Does not significantly inhibit cell proliferation. Does not significantly inhibit cell proliferation.	41184486
LNCaP	IC50	14113.1353 nM	Does not significantly inhibit cell proliferation. Does not significantly inhibit cell proliferation.	41184486
DU-145	IC50	20000 nM	Does not significantly inhibit cell proliferation. Does not significantly inhibit cell proliferation.	41184486
HepG2	IC50	20000 nM	Does not significantly inhibit cell proliferation. Does not significantly inhibit cell proliferation.	41184486

In Vitro

PMV6-PEG4-BI2536 (compound p53-01) (1 nM-10 μM; 24 h) induces an increase in luminescence signals in 293T cells co-transfected with NLS-LgBiT-p53-Y220C and mEGFP-PLK1-SmBiT, indicating the promotion of ternary complex formation between p53-Y220C and PLK1 (EC₅₀ = 1.4 μM)^[1].
PMV6-PEG4-BI2536 (62.5 nM-2 μM; 8 days) selectively inhibits the proliferation of mutant cells in a co-culture system of TP53^Y220C-mutant 293T cells and wild-type 293T cells (EC₅₀ = 443 nM)^[1].
PMV6-PEG4-BI2536 (1 nM-1 μM; 8 days) dose not affect the proliferative capacity of P53-R273H (FL)-mutant 293T cells^[1].
PMV6-PEG4-BI2536 (7.5 μM-1.5 μM; 5 days) significantly inhibits the proliferation of TP53^Y220C-mutant 293T cells ^[1].
PMV6-PEG4-BI2536 (62.5 nM-1 μM; 7 days) dose not affect the proliferative capacity of P53-R273H (FL)-mutant CALU-1 cells or wild-type CALU-1 cells ^[1].
PMV6-PEG4-BI2536 (1.5 μM; 1 day) upregulates Caspase 3/7 activity and induces apoptosis in TP53^Y220C-mutant 293T cells^[1].
PMV6-PEG4-BI2536 (0.75-1.5 μM; 1 day) increases the proportion of early and late apoptotic cells in TP53^Y220C-mutant 293T cells^[1].
PMV6-PEG4-BI2536 (0.375-1.5 μM; 1 day) induces G2/M phase arrest in TP53^Y220C-mutant 293T cells synchronized with Palbociclib (HY-50767)^[1].
PMV6-PEG4-BI2536 (1.5 μM; 8.5 h) inhibits PLK1 activity in TP53^Y220C-mutant 293T cells synchronized via double-thymidine block^[1].
PMV6-PEG4-BI2536 (4 days) significantly inhibits the proliferation of most Y220C⁺ cell lines (MFE319 (IC₅₀ = 1268.3102 nM), NUGC3 (IC₅₀ = 1713.0956 nM), MFE296 (IC₅₀ = 4320.9284 nM), BxPC-3 (IC₅₀ = 8251.9582 nM)) and the Y220C^- cell line MCF7 (IC₅₀ = 1268.3102 nM). PMV6-PEG4-BI2536 has no significant effect on the proliferation of the Y220C⁺ cell line Huh7 (IC₅₀ = 20000 nM) or most Y220C^- cell lines (LNCaP (IC₅₀ = 14113.1353 nM), DU145 (IC₅₀ = 20000 nM), HepG2 (IC₅₀ = 20000 nM)).^[1].
PMV6-PEG4-BI2536 (0.16-1.25 μM; 9 days) shows no significant cytotoxic effect on TP53-knockout MFE319 cells in a co-culture system with wild-type MFE319 cells^[1].
PMV6-PEG4-BI2536 (62.5-250 nM; 3 weeks) reduces the proportion of TP53^Y220C-mutated 293T cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:

TP53^Y220C-mutant 293T cells
Concentration:

0.75 μM, 1.5 μM
Incubation Time:

1 day
Result:

Specifically increased the proportion of early and apoptotic cells in p53-Y220C-expressing cells.

Cell Cycle Analysis^[1]

Cell Line:

TP53^Y220C-mutant 293T cells and parental 293T cells (synchronized by palbociclib (HY-50767))
Concentration:

0.375 μM, 0.75 μM, 1.5 μM
Incubation Time:

1 day
Result:

Induced significant G2/M cell cycle arrest in p53-Y220C-expressing cells, and caused genome doubling (increased 8N DNA content) at higher doses.

Western Blot Analysis^[1]

Cell Line:

TP53^Y220C-mutant 293T cells and parental 293T cells (synchronized by double thymidine block)
Concentration:

1.5 μM
Incubation Time:

8.5 h
Result:

Caused a massive accumulation of Cyclin B1 and decreased the level of phospho-PLK-binding motif in p53-Y220C-expressing cells, confirming the inhibition of PLK1 activity.

Related Protocols :

Chemical Information

Appearance Solid
Molecular Weight 1189.35
Formel C₅₉H₇₅F₃N₁₀O₁₁S
Color Light yellow to light brown
SMILES

O=C(NCCOCCOCCOCCOCCC(N1CCC(NC2=CC=CC3=C2C=C(C#CCNC4=CC=C(S(=O)(C)=O)C=C4OC)N3CC(F)(F)F)CC1)=O)C5=CC=C(NC(N=C6N(C7CCCC7)[C@@H]8CC)=NC=C6N(C)C8=O)C(OC)=C5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (84.08 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

0.8408 mL

4.2040 mL

8.4080 mL

5 mM

0.1682 mL

0.8408 mL

1.6816 mL

10 mM

0.0841 mL

0.4204 mL

0.8408 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: ≥ 5 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

Solubility: ≥ 5 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). 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 (50.0 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 (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Sadagopan A, et al. Mutant p53 protein accumulation is selectively targetable by proximity-inducing drugs. Nat Chem Biol. 2026 May;22(5):783-792. doi: 10.1038/s41589-025-02051-7. Epub 2025 Nov 3. Erratum in: Nat Chem Biol. 2026 May;22(5):840. [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	0.8408 mL	4.2040 mL	8.4080 mL	21.0199 mL
	5 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2040 mL
	10 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL
	15 mM	0.0561 mL	0.2803 mL	0.5605 mL	1.4013 mL
	20 mM	0.0420 mL	0.2102 mL	0.4204 mL	1.0510 mL
	25 mM	0.0336 mL	0.1682 mL	0.3363 mL	0.8408 mL
	30 mM	0.0280 mL	0.1401 mL	0.2803 mL	0.7007 mL
	40 mM	0.0210 mL	0.1051 mL	0.2102 mL	0.5255 mL
	50 mM	0.0168 mL	0.0841 mL	0.1682 mL	0.4204 mL
	60 mM	0.0140 mL	0.0701 mL	0.1401 mL	0.3503 mL
	80 mM	0.0105 mL	0.0525 mL	0.1051 mL	0.2627 mL

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PMV6-PEG4-BI2536

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen