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PR-924
PR-924 是一种选择性三肽环氧酮免疫蛋白酶亚单位 LMP-7 的抑制剂，IC50 为 22 nM。PR-924 共价修饰蛋白酶体的 N 端苏氨酸活性位点。PR-924 在多发性骨髓瘤细胞中抑制细胞生长并触发凋亡 (apoptosis)，并具有抗肿瘤活性。
PR-924 Chemical Structure
CAS No. : 1416709-79-9
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 生物活性 |
PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities[1][2].
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IC50 & Target |
IC50: 22 nM (LMP7), 8.2 μM (LMP2)[2]
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体外研究
(In Vitro) |
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 significantly decreases 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].
PR-924 (3 μM; 48 hours; MM.1S and MM.1R cells) treatment triggers apoptosis in MM cells[1].
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[1].
PR-924 induces BID cleavage and its translocation to mitochondria, as well as cyto-c release BID, a proapoptotic BH-3 family protein, is linked to mitochondria-mediated apoptotic signaling pathways via cyto-c release[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
| Cell Line: |
MM.1S, MM.1R, RPMI-8226, KMS12, LR-5, DOX40, INA-6, OPM1 and OPM2 cells |
| Concentration: |
1-20 μM |
| Incubation Time: |
24 hours, 48 hours, and 72 hours |
| Result: |
Significantly decreased 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). |
Apoptosis Analysis[1]
| Cell Line: |
MM.1S and MM.1R cells |
| Concentration: |
3 μM |
| Incubation Time: |
48 hours |
| Result: |
Triggered a significant increase in the Annexin V+/PI-apoptotic cell population. |
Western Blot Analysis[1]
| Cell Line: |
MM.1S and MM.1R cells |
| Concentration: |
3 μM |
| Incubation Time: |
48 hours |
| Result: |
Triggered activation of caspase-3, caspase-8 and caspase-9, and significantly down-regulated the expression of Bcl-2 protein. |
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体内研究
(In Vivo) |
PR-924 (6 mg/kg; intravenous injection; twice a week; for 21 days; CB-17 SCID-mice) treatment significantly inhibits tumour growth in human plasmacytoma xenografts[1].
PR-924 treatment significant reduces the shIL-6R levels in SCID-hu model. Treatment of tumour-bearing mice with PR-924, prolongs survival[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
CB-17 SCID-mice injected with MM.1S cells[1] |
| Dosage: |
6 mg/kg |
| Administration: |
Intravenous injection; twice a week; for 21 days |
| Result: |
Inhibited tumour growth in human plasmacytoma xenografts. |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[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.
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