2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs DNA/RNA Synthesis
  4. PT-129

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)).

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

PT-129

PT-129 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PT-129 Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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]
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.

PT-129 Related Antibodies

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.
Molecular Weight

936.98

Formula

C46H48N8O12S
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0673 mL 5.3363 mL 10.6726 mL
5 mM 0.2135 mL 1.0673 mL 2.1345 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
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Concentration
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Volume
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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 (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.

    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% 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:

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mg/kg

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(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
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 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 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:

PT-129PT129PT 129PROTACsDNA/RNA SynthesisATF4proteasomeG3BP2293T cellsBALB/c miceA549 cellsL929 cellsCAFsG3BP1stress granuleInhibitorinhibitorinhibit

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