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Cat. No.: HY-150590

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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.

For research use only. We do not sell to patients.

CAS No.: 2028300-31-2
Formula: C₃₀H₄₄N₄O₈S
Molecular Weight:620.76

Storage:

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

Data Sheet (275 KB)

20S Proteasome-IN-2 Chemical Structure

CAS No.: 2028300-31-2

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.88 μM Compound: 11m	Cytotoxicity against human A-375 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]
A549	IC₅₀	1.3 μM Compound: 11m	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]
BGC-823	IC₅₀	0.77 μM Compound: 11m	Cytotoxicity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human BGC-823 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]
HCT-116	IC₅₀	0.28 μM Compound: 11m	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]
HEK293	IC₅₀	>50 μM Compound: 11m	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]
HeLa	IC₅₀	0.67 μM Compound: 11m	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]
HT-29	IC₅₀	0.73 μM Compound: 11m	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by Cell Titer-Glo assay	[PMID: 32146375]

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	C_max (μg/L)	AUC_0-t (μg/L•h)	T_1/2 (min)	MRT (min)	CL (L/h/kg)	V_ss (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.

Chemical Information

CAS No. 2028300-31-2
Molecular Weight 620.76
Formula C₃₀H₄₄N₄O₈S
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
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

Select Batch:

Purity: 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)

References

[1]. Sun Q, et al. Design and synthesis of tripeptidyl furylketones as selective inhibitors against the β5 subunit of human 20S proteasome. Eur J Med Chem. 2020 Apr 15. 192:112160. [Content Brief]

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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.

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