PROTAC TG2 Degrader-3
PROTAC TG2 Degrader-3 is a TG2 (TGM2) PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer.
(Pink: TGM2 ligand (HY-128595); Blue: VHL ligand (HY-47851); Black: linker (HY-W013731)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3054388-18-7
- Formule: C51H62FN9O7S2
- Masse moléculaire:996.22
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
VHL |
TGM2 |
In Vitro
PROTAC TG2 Degrader-3 (Compound P374) (0.1-10 μM; 24-72 h) induces potent, proteasome-dependent degradation of TG2 in SKOV3/OVCAR5 ovarian cancer cells[1].
PROTAC TG2 Degrader-3 (0-30 μM; 24 h) does not significantly reduce the cell viability of SKOV3 or OVCAR5 ovarian cancer cells[1].
PROTAC TG2 Degrader-3 (10 μM; 6-18 h) inhibits the fibronectin adhesion and migration capacities of SKOV3 and OVCAR5 ovarian cancer cells[1].
PROTAC TG2 Degrader-3 (1-10 μM) significantly inhibits the phosphorylation of FAKTyr397 and SrcTyr416 in SKOV3 ovarian cancer cells, and disrupts the downstream integrin signaling pathway by degrading TG2[1].
PROTAC TG2 Degrader-3 (10 μM; 24 h) induces extensive proteomic changes in SKOV3 ovarian cancer cells, including decreased levels of TG2, AKT, p-AKT, SOX2, ATRX and HER2/ErbB2, as well as dysregulation of multiple signaling pathways associated with cell adhesion and cancer progression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SKOV3/OVCAR5 ovarian cancer cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24 h, 72 h
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Result:Induced significant, time- and concentration-dependent TG2 degradation, reaching approximately 80% maximal degradation at 24 h at 10 μM, with TG2 levels remaining suppressed through 72 h.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUClast |
|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.p. | 4.2 h | 600.8 nM | 1631.3 nM·h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (6-8 weeks old, female; ovarian cancer model via intraperitoneal injection of OVCAR5 cells)[1]
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Dosage:55 μg/kg
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Administration:i.p.; three times per week; 4 weeks
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Result:Exhibited significantly reduced tumor weights, tumor volumes, and tumor numbers compared to vehicle controls.
Confirmed reduced TG2 expression in tumors from treated mice.
Significantly lowered TG2 enzymatic activity in ascites fluid compared to controls.
Chemical Information
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CAS No. 3054388-18-7
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Masse moléculaire 996.22
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Formule C51H62FN9O7S2
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SMILES
CN(CCOCCOCCSC(C)(C)[C@@H](C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)NC(C4(F)CC4)=O)C5=NC(NC6=CC=C(NC(CC7=CC=CC=C7)=O)C=C6)=NC(C)=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC TG2 Degrader-3 Related Classifications
HY-181732 Related Classifications
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