2. PROTAC Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. PROTACs Transglutaminase FAK Src Akt
  4. 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)).

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

PROTAC TG2 Degrader-3

PROTAC TG2 Degrader-3 Chemical Structure

CAS No. : 3054388-18-7

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PROTAC TG2 Degrader-3 Related Antibodies

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Description

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[1]. (Pink: TGM2 ligand (HY-128595); Blue: VHL ligand (HY-47851); Black: linker (HY-W013731)).

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.

PROTAC TG2 Degrader-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: SKOV3/OVCAR5 ovarian cancer cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h, 72 h
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

PROTAC TG2 Degrader-3 (55 μg/kg; i.p.; three times per week; 4 weeks) significantly inhibits the growth and metastasis of ovarian tumors, and reduces the expression and enzymatic activity of TG2 in vivo[1].

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

Animal Model: Athymic nude mice (6-8 weeks old, female; ovarian cancer model via intraperitoneal injection of OVCAR5 cells)[1]
Dosage: 55 μg/kg
Administration: i.p.; three times per week; 4 weeks
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.
Molecular Weight

996.22

Formula

C51H62FN9O7S2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC TG2 Degrader-3 Related Classifications

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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:

PROTAC TG2 Degrader-33054388-18-7PROTACsTransglutaminaseFAKSrcAkt转谷氨酰胺酶PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinasePKBProtein kinase BSKOV3 ovarian cancer cellsTG2OVCAR5 ovarian cancer cellscell adhesionproteasomecell migrationovarian cancerInhibitorinhibitorinhibit

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