PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].
体外研究 (In Vitro)
PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1]. PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1]. PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1]. PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (5 nM)[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay[1]
Cell Line:
BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time:
24 h
Result:
Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).
Western Blot Analysis[1]
Cell Line:
HBL6 cells
Concentration:
50 nM
Incubation Time:
6 h
Result:
Decreased the NF-κB activity by 52%.
分子量
618.76
Formula
C32H50N4O8
CAS 号
158442-41-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.
PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].
体外研究 (In Vitro)
PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1]. PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1]. PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1]. PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (5 nM)[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay[1]
Cell Line:
BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time:
24 h
Result:
Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).
Western Blot Analysis[1]
Cell Line:
HBL6 cells
Concentration:
50 nM
Incubation Time:
6 h
Result:
Decreased the NF-κB activity by 52%.
分子量
618.76
Formula
C32H50N4O8
CAS 号
158442-41-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.
PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor. PSI inhibits the proliferation of primary effusion lymphoma (PEL) cells. PSI has the potential for the research of Kaposi’s sarcoma-associated herpesvirus (KSHV) infection and KSHV-associated lymphomas[1].
体外研究 (In Vitro)
PSI (24 h) inhibits the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively)[1]. PSI (50 nM; 6 h) increases caspase-3/7 activity by 8-fold compared with control[1]. PSI (50 nM; 6 h) decreases the transcriptional activity of NF-κB by 52%[1]. PSI (1, 5 nM; 3 days) inhibits the growth of BC3 cells at a high concentration (5 nM)[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay[1]
Cell Line:
BC3, BCBL1, Ramos, BJAB cells
Concentration:
Incubation Time:
24 h
Result:
Inhibited the proliferation of primary effusion lymphoma (PEL) cells at low nanomolar concentrations (CC50s of 205, 190, 22.0, 53.0 nM FOR BJAB, Ramos, BC3, BCBL1 cells, respectively).
Western Blot Analysis[1]
Cell Line:
HBL6 cells
Concentration:
50 nM
Incubation Time:
6 h
Result:
Decreased the NF-κB activity by 52%.
分子量
618.76
Formula
C32H50N4O8
CAS 号
158442-41-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Saji C, et al. Proteasome inhibitors induce apoptosis and reduce viral replication in primary effusion lymphoma cells. Biochem Biophys Res Commun. 2011; 415(4):573-8.
PSI-697 is an oral P-selectin inhibitor with an IC50 of 125 μM[1].
IC50 & Target
IC50: 125 μM (P-selectin)[1]
体外研究 (In Vitro)
PSI-697 inhibits the binding of a soluble human P-selectin to PSGL-1, in a reproducible concentration-dependent manner inhibiting 50% of binding at a concentration of 125 μM in vitro[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
PSI-697 (0-50 mg/kg; p.o.) significantly reduces the number of rolling leukocytes by 39% versus vehicle control[1]. PSI-697 (100 mg/kg; p.o.) reduces thrombus weight by 18% relative to vehicle, without prolonging bleeding time in a rat venous thrombosis model[1]. PSI-697 (30 mg/kg; p.o.; daily; 6 days) promotes thrombus resolution and decreases inflammation in a baboon model of venous thrombosis[2]. PSI-697 ((30 mg/kg; i.g.; daily) decreases vein wall injury in a rat stenosis model of venous thrombosis[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
4-5 weeks male Sprague-Dawley rat (50-100 g)[1]
Dosage:
0 mg/kg, 30 mg/kg, 50 mg/kg
Administration:
Oral administration
Result:
At an oral dose of 50 mg/kg reduced the number of rolling leukocytes by 39% versus vehicle control.
Clinical Trial
分子量
367.83
Formula
C21H18ClNO3
CAS 号
851546-61-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Bedard PW et al. Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis. J Pharmacol Exp Ther.
[2]. Myers DD Jr et al. Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selectin (PSI-697) without anticoagulation. Thromb Haemost. 2007 Mar;97(3):400-7.
[3]. Myers DD Jr et al. Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosis model of venous thrombosis. J Vasc Surg. 2006 Sep;44(3):625-32.
PSI-7409 is the active 5′-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.
体外研究 (In Vitro)
PSI-7409 inhibits the enzymatic activities of these NS5BΔ21 polymerases in a dose-dependent manner. The IC50s for PSI-7409 against GT 1b, 2a, 3a, and 4a NS5B polymerases are 1.6 μM, 2.8 μM, 0.7 μM, and 2.6 μM, respectively. PSI-7409 is a weak inhibitor of DNA Pol α (IC50=550 μM). DNA Pol β and γ are not inhibited by 1 mM PSI-7409. A significant amount of RNA product is made in the presence of 500 μM PSI-7409, about 85%[1]. In clone A cells, the levels of PSI-7409 gradually increases to a maximum concentration of about 25 μm over a period of 48 h. PSI-7409 forms at a much faster rate in primary human hepatocytes, achieving a maximum intracellular concentration of ∼100 μM at 4 h and remains at that concentration for 48 h[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
500.16
Formula
C10H16FN2O14P3
CAS 号
1015073-42-3
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Lam AM, et al. PSI-7851, a pronucleotide of beta-D-2′-deoxy-2′-fluoro-2′-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96.
[2]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.
