Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research[1].
IC50 & Target
IC50: 8.39 nM (proteasome)[1]
体外研究 (In Vitro)
Proteasome-IN-4 (compound 43) (0-20 nM; 72 hours) has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively[1]. Proteasome-IN-4 (10-1000 nM; 3 hours) causes massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM[1]. Proteasome-IN-4 (2μM) has high metabolic stability in mouse blood, with T1/2 of 329.21 min[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line:
MM-1S, RPMI 8226 and MV-4-11 cells[1]
Concentration:
0-20 nM
Incubation Time:
72 hours
Result:
Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively.
Western Blot Analysis
Cell Line:
MM-1S[1]
Concentration:
10, 100 and 1000 nM
Incubation Time:
3 hours
Result:
Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM.
体内研究 (In Vivo)
Proteasome-IN-4 (5 mg/kg; i.v.; single) has superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h in model mice[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
ICR mice (6-8 weeks)[1]
Dosage:
5 mg/kg
Administration:
i.v.; single
Result:
Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h.
分子量
750.97
Formula
C44H58N6O5
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]. Cao Y, et al. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211.
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research[1].
IC50 & Target
IC50: 8.39 nM (proteasome)[1]
体外研究 (In Vitro)
Proteasome-IN-4 (compound 43) (0-20 nM; 72 hours) has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively[1]. Proteasome-IN-4 (10-1000 nM; 3 hours) causes massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM[1]. Proteasome-IN-4 (2μM) has high metabolic stability in mouse blood, with T1/2 of 329.21 min[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay
Cell Line:
MM-1S, RPMI 8226 and MV-4-11 cells[1]
Concentration:
0-20 nM
Incubation Time:
72 hours
Result:
Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively.
Western Blot Analysis
Cell Line:
MM-1S[1]
Concentration:
10, 100 and 1000 nM
Incubation Time:
3 hours
Result:
Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM.
体内研究 (In Vivo)
Proteasome-IN-4 (5 mg/kg; i.v.; single) has superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h in model mice[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
ICR mice (6-8 weeks)[1]
Dosage:
5 mg/kg
Administration:
i.v.; single
Result:
Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h.
分子量
750.97
Formula
C44H58N6O5
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]. Cao Y, et al. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211.
Proteasome-IN-4 is an excellent and non-covalent proteasome inhibitor (IC50=8.39 nM). Proteasome-IN-4 has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines. Proteasome-IN-4 can be used for cancer research[1].
IC50 & Target
IC50: 8.39 nM (proteasome)[1]
体外研究 (In Vitro)
Proteasome-IN-4 (compound 43) (0-20 nM; 72 hours) has potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively[1]. Proteasome-IN-4 (10-1000 nM; 3 hours) causes massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM[1]. Proteasome-IN-4 (2μM) has high metabolic stability in mouse blood, with T1/2 of 329.21 min[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 Proliferation Assay
Cell Line:
MM-1S, RPMI 8226 and MV-4-11 cells[1]
Concentration:
0-20 nM
Incubation Time:
72 hours
Result:
Displayed potent antiproliferative activities against RPMI-8226, MM-1S and MV-4-11 cell lines, with IC50 of 15.290, 9.067 and 2.740 nM respectively.
Western Blot Analysis
Cell Line:
MM-1S[1]
Concentration:
10, 100 and 1000 nM
Incubation Time:
3 hours
Result:
Caused massive accumulation of polyubiquitinated proteins at the concentration from 10 nM to 1000 nM.
体内研究 (In Vivo)
Proteasome-IN-4 (5 mg/kg; i.v.; single) has superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h in model mice[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.
Animal Model:
ICR mice (6-8 weeks)[1]
Dosage:
5 mg/kg
Administration:
i.v.; single
Result:
Displayed superior activities with intracellular proteasome inhibitory rates of about 50% after administration of 1 h.
分子量
750.97
Formula
C44H58N6O5
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]. Cao Y, et al. Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment. Eur J Med Chem. 2022;233:114211.
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.
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity[1][2].
IC50 & Target
IC50: 1 μM (20S proteasome)[1]
体外研究 (In Vitro)
Proteasome inhibitor IX (AM114; 0.1-10 µM; 14 days; HCT116 p53+/+ cells) treatment causes a loss of cell survival in the p53+/+ and p53-/- cells by approximately 70 and 20%, respectively at a concentration of 1 µM[1]. Proteasome inhibitor IX (AM114) exhibits potent activity against p53+/+ cells in colony formation assay, with an IC50 value of 0.6 µM[1]. Incubation of HCT116 p53+/+ cells with 1 µM Proteasome inhibitor IX (AM114) causes 28% of the cells to exhibit positive Annexin V staining at 48 h, and this fraction of dead cells increased to 76% at 72 h[1]. Proteasome inhibitor IX (AM114) treatment inhibits the chymotrypsin-like activity of the 20S proteasome in vitro, leading to a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells[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.
分子量
377.01
Formula
C20H21B2NO5
CAS 号
856849-35-9
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Geetha Achanta , et al. A Boronic-Chalcone Derivative Exhibits Potent Anticancer Activity Through Inhibition of the Proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33.
[2]. Encouse B Golden, et al. Green Tea Polyphenols Block the Anticancer Effects of Bortezomib and Other Boronic Acid-Based Proteasome Inhibitors. Blood. 2009 Jun 4;113(23):5927-37.