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PR-924

PR-924

产品编号 T16568   CAS 1416709-79-9

PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.

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PR-924 Chemical Structure
PR-924, CAS 1416709-79-9
规格 价格/CNY 货期 数量
2 mg ¥ 3,770 5日内发货
产品目录号及名称: PR-924 (T16568)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.
靶点活性 LMP2:8.2 μM, LMP7:22 nM
体外活性 PR-924 causes BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondrial-mediated apoptotic signaling pathways via cyto-c release. PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells. PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers activation of caspase-3, caspase-8, and caspase-9, and significantly down-regulated the expression of Bcl-2 protein, without altering Bax or MCL-1 protein levels. PR-924 (1-20 μM; 24-72 hours; MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1, and OPM2 cells) treatment obviously reduces the viability of all the MM cell lines in a time-and dose-dependent manner (IC 50 range for cell lines: 3-7 μM for 48 h)[1].
体内活性 PR-924 treatment obviously decreases the shIL-6R levels in SCID-hu model. Treatment of tumor-bearing mice with PR-924 prolongs survival. PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment obviously inhibits tumor growth in human plasmacytoma xenografts [1].
分子量 618.72
分子式 C37H38N4O5
CAS No. 1416709-79-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Singh AV, et al. PR-924, a selective inhibitor of the immunoproteasome subunit LMP-7, blocks multiple myeloma cell growth both in vitro and in vivo. Br J Haematol. 2011 Jan;152(2):155-63. 2. Parlati F, et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. Blood. 2009 Oct 15;114(16):3439-47.
Saikogenin A Bortezomib-pinanediol Teneligliptin hydrobromide MLN9708 Bortezomib Cilastatin Carfilzomib Z-LLF-CHO

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

PR-924 1416709-79-9 Proteases/Proteasome Ubiquitination Proteasome PR924 PR 924 Inhibitor inhibitor inhibit

 

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