化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 25mg 100mg |
CAS | 2645-32-1 |
别名 |
|
化学名 | (2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate |
分子式 | C7H5N5S2 |
分子量 | 223.28 |
溶解度 | ≥ 11.15mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
(2,6-diamino-5-thiocyanatopyridin-3-yl) thiocyanate, also designated as PR-619, is a broad-range reversible and cell-permeable inhibitor of deubiquitylating enzyme (DUB)[1][2][3], potently suppresses the activity of almost all cysteine protease DUBs[4], but shows selectivity toward DUBs over other proteases, such as calpain 1, or cathepsins[3]. PR-619 induces (tumor) cell death with EC50 values in the low micromolar range [1].
Deubiquitylating enzyme (DUB), also called ubiquitin isopeptidase or deubiquitinating proteins, performs deubiquitination of target proteins. Ubiquitination, followed by proteasomal degradation, is a process of ubiquitin proteasome system (UPS). Failure of the ubiquitin proteasome system (UPS) and/or the autophagy pathway may result in aggregation of proteins, a pathological hallmark of many neurodegenerative diseases [2].
In OLN-t40 cells, 7-10 μM as the concentration range for PR-619 to exert its cytotoxicity was suggested, half maximal cytotoxicity was observed after a 24h-treatment with 9-10 μM PR-619. Similar to MG-132, PR-619 caused an increase in the abundance of ubiquitinated proteins within 24 h at the concentration range of 7-12.5μM. Tested with OLN-t40 cells, PR-619, unlike MG-132, did not inhibit the enzymatic activity of the proteasome in cellular lysates but only when taken up by living cells[2]. An in vitro system showed that PR-619 was able to stabilize the microtubule network and led to small tau aggregates surrounding the microtubule organizing center [5].
There is still not any available result regarding in vivo treatment in an animal body.
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。
标签:PR-619
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