| Bioactivity | PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis[1][2][3][4]. | ||||||||||||
| Invitro | PR-619, a deubiquitylase inhibitor, prevents degradation, indicating KCa3.1 is targeted for degradation by ubiquitylation[2].PR-619 affects the microtubule network and led to the accumulation of small punctuated tau deposits around. PR-619 causes the dephosphorylation of tau[3].PR-619 (7-12.5 μM) causes an increase in the abundance of ubiquitinated proteins within 24 h. PR-619 leads to the induction of heat shock proteins and to an increase of ubiquitinated proteins[3].PR-619 (9 μM) affects the organization of the microtubule network in OLN-t40 cells[3].PR-619 (5, 7.5, and 10 μM) induces ER Stress and ER-Stress related apoptosis on T24 and BFTC-905 cells. PR-619 induces polyubiquitination, Bcl-2 downregulation, and concurrent PARP cleavage in a dose-dependent manner. PR-619 induces G0/G1 arrest in UC cells[4]. Cell Cytotoxicity Assay[1] Cell Line: | ||||||||||||
| Name | PR-619 | ||||||||||||
| CAS | 2645-32-1 | ||||||||||||
| Formula | C7H5N5S2 | ||||||||||||
| Molar Mass | 223.28 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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