PT-129

CAT: 0804-HY-170872-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-170872-01Size:5 mg
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AVAILABILITY: InStock
24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
PT-129 is an RPOTAC degrader targeting the NTF2 domain (protein-RNA interaction site) of G3BP1/2, which mediates the disassembly of intracellular stress granules. PT-129 can inhibit the formation of stress granules in stressed cells and disassemble existing stress granules, and can disrupt the transmission of ATF4, thereby inhibiting the proliferation of cancer cells. Stress granules (SGs) are membrane-less cytoplasmic compartments formed under stress stimuli. SGs promote the transmission of ATF4 from fibroblasts to tumor cells through a migratory effect, mediating fibroblast-related tumor growth. And G3BP1/2 is a central protein of the SGs network, and the inhibition of G3BP1/2 may reduce the stress resistance of cancer cells in the tumor microenvironment. PT-129 is composed of a target protein ligand (red part) G3BP1/2-Targeting ligand-1 (HY-170873), an E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a PROTAC linker (black part) Amino-PEG3-C2-acid (HY-W040165) ; among them, the E3 ligase ligand + linker form a complex Thalidomide-NH-PEG3-propionic acid (HY-136166) [1].
UNSPSC
12352005
Target
DNA/RNA Synthesis; PROTACs
Related Pathways
Cell Cycle/DNA Damage; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Purity
98.66
Solubility
DMSO : 100 mg/mL (ultrasonic)
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
Molecular Formula
C46H48N8O12S
Molecular Weight
936.98
References & Citations
[1]Dong T, et al. G3BP1/2-Targeting PROTAC Disrupts Stress Granules Dependent ATF4 Migracytosis as Cancer Therapy. J Am Chem Soc. 2025 Jan 8;147 (1) :446-461.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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