PROTAC TG2 degrader-1
PROTAC TG2 degrader-1 is a tissue transglutaminase (TG2) PROTAC degrader with a Kd of 68.9 μM. PROTAC TG2 degrader-1 recruits the VHL E3 ubiquitin ligase to the fibronectin-binding site of TG2, forms a ternary complex, and induces proteasome-dependent degradation of TG2. PROTAC TG2 degrader-1 inhibits ovarian cancer cell migration and adhesion to fibronectin, without producing a significant inhibitory effect on cell proliferation. PROTAC TG2 degrader-1 can be used in related research on ovarian cancer.
For research use only. We do not sell to patients.
- CAS No.: 3033465-55-0
- Formula: C55H73N9O10S
- Molecular Weight:1052.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
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VHL |
In Vitro
PROTAC TG2 degrader-1 (compound 11) (0.1-10 μM; 6-24 h) induces concentration-dependent degradation of TG2 in OVCAR5 human ovarian cancer cells at 6 h after a single administration, while intermittent repeated administration within 24 h sustains the reduction of TG2 protein levels[1].
PROTAC TG2 degrader-1 (1-10 μM; 6-24 h) induces concentration-dependent degradation of TG2 in human ovarian cancer SKOV3 cells at 6 h after a single administration, and repeated intermittent administration within 24 h sustains the reduction of TG2 protein levels[1].
PROTAC TG2 degrader-1 (0.1-30 μM; 2-24 h) induces TG2 protein degradation in a time- and concentration-dependent manner[1].
PROTAC TG2 degrader-1 directly binds to purified full-length human TG2 with a Kd of 68.9 μM[1].
PROTAC TG2 degrader-1 (10 μM; 6-18 h) significantly reduces the fibronectin adhesion capacity and migration ability of human ovarian cancer cell lines OVCAR5 and SKOV3[1].
PROTAC TG2 degrader-1 (0.1-30 μM; 5 days) does not exert significant cytotoxicity in OVCAR5 and SKOV3 human ovarian cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OVCAR5 human ovarian cancer cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:6, 24 h
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Result:Reduced TG2 protein levels in OVCAR5 cells in a concentration-dependent manner after 6 h of incubation.
Showed no reduction in TG2 levels after 24 h of single-dose incubation.
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Cell Line:SKOV3 human ovarian cancer cells
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Concentration:1, 10 μM
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Incubation Time:6, 24 h
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Result:Reduced TG2 protein levels in SKOV3 cells in a concentration-dependent manner after 6 h of incubation.
Showed no reduction in TG2 levels after 24 h of single-dose incubation.
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Cell Line:SKOV3 human ovarian cancer cells
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Concentration:0.1, 0.3, 1, 3, 10, 30 μM
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Incubation Time:0, 2, 6, 12, 24 h
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Result:Induced time‑ and concentration‑dependent TG2 protein degradation.
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Cell Line:OVCAR5 human ovarian cancer cells, SKOV3 human ovarian cancer cells
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Concentration:0.1, 0.3, 1, 3, 10, 30 μM
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Incubation Time:5 days (dosed every 6-8 h)
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Result:Showed no significant cell death or reduction in cell viability in either OVCAR5 or SKOV3 cells across all tested concentrations over the 5 day incubation period.
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Cell Line:OVCAR5 human ovarian cancer cells, SKOV3 human ovarian cancer cells
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Concentration:10 μM
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Incubation Time:18 h
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Result:Reduced the migration ability of human ovarian cancer cell lines OVCAR5 and SKOV3.
Chemical Information
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CAS No. 3033465-55-0
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Molecular Weight 1052.29
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Formula C55H73N9O10S
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SMILES
O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCOCCOCCOCCOCCOCCN(C2=NC(NC3=CC=C(NC(CC4=CC=CC=C4)=O)C=C3)=NC(C)=C2)C)=O)=O)C[C@H](O)C1)NCC5=CC=C(C6=C(C)N=CS6)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)