Art. -Nr.: HY-170872

PT-129

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PT-129 is a G3BP1/G3BP2 PROTAC degrader. PT-129 inhibits the formation of stress granules, disassembles pre-existing stress granules, disrupts stress granule-mediated ATF4 trafficking via migratory exocytosis, and suppresses cancer cell proliferation. PT-129 is applicable to the research of lung cancer and melanoma.
(Pink: G3BP1 and G3BP2 ligand (HY-170873); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W040165)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.66%
Formel: C₄₆H₄₈N₈O₁₂S
Molecular Weight:936.98

Speicherung:

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

PT-129 Chemical Structure

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

PT-129 is a G3BP1/G3BP2 PROTAC degrader. PT-129 inhibits the formation of stress granules, disassembles pre-existing stress granules, disrupts stress granule-mediated ATF4 trafficking via migratory exocytosis, and suppresses cancer cell proliferation. PT-129 is applicable to the research of lung cancer and melanoma^[1]. (Pink: G3BP1 and G3BP2 ligand (HY-170873); Blue: Cereblon ligand (HY-41547); Black: linker (HY-W040165)).

IC₅₀ & Target

G3BP1/2, ATF4^[1]

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

PT-129 (0.1-10 μM; 0-12 h) induces proteasome-dependent, dose- and time-dependent degradation of G3BP1 and G3BP2 in L929 cells, with maximum degradation (95% for G3BP1) achieved at 5 or 10 μM after 12 h of treatment^[1].
PT-129 (5 μM; 3 h pretreatment) inhibits arsenate-induced stress granule formation in 293T cells expressing GFP-Caprin1, and (10 μM; 0.5-4 h) dissolves preformed stress granules in these cells, reducing granule counts to near 0 by 4 h^[1].
PT-129 (5 μM; 0-24 h) selectively depletes G3BP1/2 and downregulates their associated signaling proteins, as well as core stress granule proteins, in A549 cells, with progressive reductions in target protein levels observed over 24 h of treatment^[1].
PT-129 (5 μM; 12 h) pretreatment of CAFs inhibits the ability of CAFs to promote the proliferation of cocultured A549 mCherry cells^[1].
PT-129 (5 μM; 12 h) pretreatment of L929 TSPAN4-GFP cells disrupts stress granule-dependent transport of ATF4 from fibroblasts to cocultured LLC-RFP cancer cells under arsenate stress conditions^[1].

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

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

5 μM
Incubation Time:

12 h; 0, 4, 8, 12, 24 h (time-course)
Result:

Significantly reduced levels of G3BP1, G3BP2, STAT1, STAT3, EIF4B, JAK1, and RELA in A549 cells.
Decreased levels of G3BP1, G3BP2, STAT1, STAT3, EIF4B, JAK1, and RELA progressively over 24 h, with the largest reductions observed at 24 h.
Downregulated 34 key stress granule core proteins in PT-129-treated A549 cells.

Cell Proliferation Assay^[1]

Cell Line:

A549 mCherry cells, cancer-associated fibroblasts (CAFs)
Concentration:

5 μM (CAF pretreatment)
Incubation Time:

12 h (CAF pretreatment); 48 h (coculture)
Result:

Caused a significant reduction in relative proliferation of A549 mCherry cells cocultured with PT-129-pretreated CAFs compared to cells cocultured with DMSO-pretreated CAFs.

In Vivo

PT-129 (5 μM; 12 h pre-treatment of tumor cells, subcutaneous injection) significantly reduces the volume of lung cancer xenografts in BALB/c mice and decreases the intratumoral expression of G3BP1 and ATF4^[1].
PT-129 (5 μM; 12 h pre-treatment of tumor cells, subcutaneous injection) improves survival rate, reduces the number of pulmonary metastatic nodules, decreases the expression of G3BP1 and ATF4 in lung tissues, and inhibits stress granule formation in cancer-associated fibroblasts (CAFs) in a C57BL/6 mouse melanoma metastasis model^[1].

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

Animal Model:

BALB/c^[1]
Dosage:

5 μM (in vitro pretreatment of CAFs/NFs)
Administration:

in vitro pretreatment; 12 h
Result:

Significantly reduced tumor volume compared to DMSO-pretreated CAFs group.
Significantly reduced G3BP1 and ATF4 protein expression in tumor tissues.

Animal Model:

C57BL/6^[1]
Dosage:

5 μM (in vitro pretreatment of CAFs/NFs)
Administration:

in vitro pretreatment; 12 h
Result:

Improved survival compared to DMSO-pretreated CAFs group.
Significantly reduced number of melanoma metastatic nodules in lung tissues.
Significantly reduced G3BP1 and ATF4 protein expression in lung tissues.
Significantly inhibited stress granule formation in CAFs isolated from lung tissues.

Chemical Information

Appearance Solid
Molecular Weight 936.98
Formel C₄₆H₄₈N₈O₁₂S
Color Light yellow to yellow
SMILES

O=C(NC1=CC=C(NC(CCOCCOCCOCCNC2=CC=CC(C(N3C(CC4)C(NC4=O)=O)=O)=C2C3=O)=O)C=C1)[C@@H](NS(=O)(CC(N5N=CC6=C5C=CC=C6)=O)=O)CC7=CC=CC=C7
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 (106.73 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

1.0673 mL

5.3363 mL

10.6726 mL

5 mM

0.2135 mL

1.0673 mL

2.1345 mL

10 mM

0.1067 mL

0.5336 mL

1.0673 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: ≥ 2.5 mg/mL (2.67 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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]. Dong T, et al. G3BP1/2-Targeting PROTAC Disrupts Stress Granules Dependent ATF4 Migracytosis as Cancer Therapy. J Am Chem Soc. 2025;147(1):446-461. [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	1.0673 mL	5.3363 mL	10.6726 mL	26.6815 mL
	5 mM	0.2135 mL	1.0673 mL	2.1345 mL	5.3363 mL
	10 mM	0.1067 mL	0.5336 mL	1.0673 mL	2.6681 mL
	15 mM	0.0712 mL	0.3558 mL	0.7115 mL	1.7788 mL
	20 mM	0.0534 mL	0.2668 mL	0.5336 mL	1.3341 mL
	25 mM	0.0427 mL	0.2135 mL	0.4269 mL	1.0673 mL
	30 mM	0.0356 mL	0.1779 mL	0.3558 mL	0.8894 mL
	40 mM	0.0267 mL	0.1334 mL	0.2668 mL	0.6670 mL
	50 mM	0.0213 mL	0.1067 mL	0.2135 mL	0.5336 mL
	60 mM	0.0178 mL	0.0889 mL	0.1779 mL	0.4447 mL
	80 mM	0.0133 mL	0.0667 mL	0.1334 mL	0.3335 mL
	100 mM	0.0107 mL	0.0534 mL	0.1067 mL	0.2668 mL

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PT-129

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Anti-Lung Cancer Compound Library

Osteogenesis Compound Library

PROTAC Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PT-129

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Anti-Lung Cancer Compound Library

Osteogenesis Compound Library

PROTAC Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PT-129 Related Classifications

HY-170872 Related Classifications