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Art. -Nr.: HY-144369

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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.

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CAS. Nr.: 3033388-83-6
Formel: C₄₄H₅₈N₆O₅
Molecular Weight:750.97

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

Proteasome-IN-4 Chemical Structure

CAS. Nr.: 3033388-83-6

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 8.39 nM (proteasome)^[1]

Cellular Effect

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]

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 T_1/2 of 329.21 min^[1].

MedChemExpress (MCE) 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.

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].

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.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

Chemical Information

CAS. Nr. 3033388-83-6
Molecular Weight 750.97
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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