6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer.
体外研究
6RK73 (5 µM; 1-3 hours) treatment displays strong inhibition of the TGFβ-induced pSMAD2 and pSMAD3, and a decrease of TβRI and total SMAD protein levels in MDA-MB-436 cells.
6RK73(5 µM; 24-48 hours) results migration significantly slower than the DMSO control group in MDA-MB-436 cells.
Cell Viability Assay
Cell Line:
MDA-MB-436 cells
Concentration:
5 µM
Incubation Time:
24, 48 hours
Result:
Migrated significantly slower than the DMSO control group
Western Blot Analysis
Cell Line:
MDA-MB-436 cells
Concentration:
5 µM
Incubation Time:
1, 2, 3 hours
Result:
Displayed strong inhibition of the TGFβ-induced pSMAD2 and pSMAD3, and a decrease of TβRI and total SMAD protein levels.
体内研究
6RK73 displays a potent inhibition of breast cancer extravasation in zebrafish.
分子式
C13H17N5O2S
分子量
307.37
CAS号
1895050-66-4
运输条件
Room temperature in continental US; may vary elsewhere.