875165-39-2
Chemical Structure
TCL1
- CAS No.: 875165-39-2
- Formula:C19H14BrClN4O2S
- Molecular Weight:477.76
InChIKey: BWGPJTANFXCCTH-UHFFFAOYSA-N
SMILES: O=C(CC1SC2=NN=C(CC3=CC=C(C=C3)Br)N2N=C1C4=CC=C(Cl)C=C4)O
Biological Activity: TCL1 is a selective non-covalent inhibitor targeting the Pru domain of the Rpn-13 subunit in the 19S regulatory particle (19S RP) of the proteasome with an IC50 value of approximately 26 μM. TCL1 interferes with the recognition and transport of ubiquitinated proteins by Rpn-13, inhibits the degradation of proteins by the proteasome, and thus affects the balance of intracellular protein metabolism. TCL1 is promising for research of hematological malignancies[1][2][3].
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TCL1 | TCL1 is a selective non-covalent inhibitor targeting the Pru domain of the Rpn-13 subunit in the 19S regulatory particle (19S RP) of the proteasome with an IC50 value of approximately 26 μM. TCL1 interferes with the recognition and transport of ubiquitinated proteins by Rpn-13, inhibits the degradation of proteins by the proteasome, and thus affects the balance of intracellular protein metabolism. TCL1 is promising for research of hematological malignancies. | |||||||||||||||||||||
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- [1]. Loy CA, et al. ByeTAC: Bypassing E-Ligase-Targeting Chimeras for Direct Proteasome Degradation. J Med Chem. 2025 May 8;68(9):9694-9705. [Content Brief]
- [2]. Winton VJ, et al. Deleterious Consequences of UDP-Galactopyranose Mutase Inhibition for Nematodes. ACS Chem Biol. 2017 Sep 15;12(9):2354-2361. [Content Brief]
- [3]. Loy CA, et al. Discovery of a non-covalent ligand for Rpn-13, a therapeutic target for hematological cancers. Bioorg Med Chem Lett. 2023 Oct 15;95:129485. [Content Brief]
Keywords
