1. Metabolic Enzyme/Protease
  2. Proteasome
  3. 20S Proteasome-IN-2

20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M.

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20S Proteasome-IN-2 Chemical Structure

20S Proteasome-IN-2 Chemical Structure

CAS No. : 2028300-31-2

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Description

20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M[1].

IC50 & Target

IC50: 0.18 μM (β5 subunit of 20S Proteasome)

In Vitro

20S Proteasome-IN-2 (compoun 11m) inhibits 20S proteasome by forming no irreversible covalent modification on it[1].
20S Proteasome-IN-2 (compoun 11m) (1.56, 3.13, 6.25, 12.5, and 25 μM) shows high binding affinity with purified human 20S proteasome, the equilibrium dissociation constants is 4.8 μM[1].
20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) inhibits tumor cells in a low concerntration with IC50 values of 0.88, 0.77, 0.67, 0.73, 1.3, 0.57, and 0.28 μM for A375, BGC-823, Hela, HT-29, A549, PCM1E8, HCT-116, resepectively[1].
20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) arrests the cell cycle at G2/M[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: Human colorectal cancer cell line HCT-116 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Arrested the cell cycle at G2/M.
In Vivo

20S Proteasome-IN-2 (compoun 11m) is (i.v.; 5 mg/kg; single injection) rapidly cleared from the plasma with an average terminal plasma half-life of 14 min, thus it exhibits extensive tissue permeability and low clearance rate (CL) of 2.0 L/h/k, and is largely eliminated extrahepatically[1].
20S Proteasome-IN-2 (compoun 11m) (i.v.; 10 mg/kg; twice one week; 4 weeks) shows antitumor efficacy combat solid tumors[1].
Pharmacokinetic parameters of 20S Proteasome-IN-2 (compoun 11m)[1]

Administrations Cmax (μg/L) AUC0-t (μg/L•h) T1/2 (min) MRT (min) CL (L/h/kg) Vss (L/kg)
iv, 5 mg/kg 2007 680 13.83 20.20 2.0 0.66

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: HCT-116 cell xenograft nude mice model[1]
Dosage: 10 mg/kg
Administration: Intravenous injection; twice weekly for consecutive four weeks
Result: Inhibited tumor growth in vivo and was well tolerated.
Molecular Weight

620.76

Formula

C30H44N4O8S

CAS No.
SMILES

O=C(N[C@@H](COC)C(N[C@@H](CC(C)C)C(C1=CC=CO1)=O)=O)[C@@H](NS(=O)(C2=CC=C(C)C=C2)=O)CC(NCC(C)(C)C)=O

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

Purity & Documentation
References
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20S Proteasome-IN-2 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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20S Proteasome-IN-2
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HY-150590
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