6RK73 (C09-1167-235)

6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC 50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC 50 =236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancerIn Vitro6RK73 (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. ?/n6RK73(5 μM; 24-48 hours) results migration significantly slower than the DMSO control group in MDA-MB-436 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: MDA-MB-436 cells Concentration: 5 µM Incubation Time: 24, 48 hours Result: Migrated significantly slower than the DMSO control group Western Blot AnalysisCell 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.In Vivo6RK73 displays a potent inhibition of breast cancer extravasation in zebrafish . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 0.23 µM (UCHL1), 236 µM (UCHL3). Specification: 0.99 Molecular Formula: C13H17N5O2S Molecular Weight: 307.37 PubChem CID: 121248200 Isomeric SMILES: C1CN(C[C@H]1C(=O)NC2=NC=C(S2)N3CCOCC3)C#N