Proteasome-IN-4
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.
For research use only. We do not sell to patients.
- CAS No.: 3033388-83-6
- Formula: C44H58N6O5
- Molecular Weight:750.97
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 8.39 nM (proteasome)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | IC50 |
9.067 nM
Compound: 43
|
Antiproliferative activity against human MM1.S cells after 72 hrs by MTS assay
Antiproliferative activity against human MM1.S cells after 72 hrs by MTS assay
|
[PMID: 35218994] |
| MV4-11 | IC50 |
2.464 nM
Compound: 43
|
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS assay
Antiproliferative activity against human MV4-11 cells after 72 hrs by MTS assay
|
[PMID: 35218994] |
| RPMI-8226 | IC50 |
15.29 nM
Compound: 43
|
Antiproliferative activity against human RPMI-8226 cells after 72 hrs by MTS assay
Antiproliferative activity against human RPMI-8226 cells after 72 hrs by MTS assay
|
[PMID: 35218994] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
-
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.
MedChemExpress (MCE) 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.
Chemical Information
-
CAS No. 3033388-83-6
-
Molecular Weight 750.97
-
Formula C44H58N6O5
-
SMILES
CCN(C1=CC=CC=C1)C(C2CCN(CC2)C(N[C@H](C(N[C@H](C(N[C@@H]3CCCC4=C3C=CC=C4)=O)CCC5=CC=CC=C5)=O)CC(NCC(C)(C)C)=O)=O)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)