3033465-55-0
Chemical Structure
PROTAC TG2 degrader-1
- CAS No.: 3033465-55-0
- Formula:C55H73N9O10S
- Molecular Weight:1052.29
InChIKey: MYUZJYLLOWISNU-WXTQVCCASA-N
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
Biological Activity: 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[1].
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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. | |||||||||||||||||||||
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