country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-187924

Copy Link Print Information

Proteasome-IN-9

Proteasome-IN-9 is an inhibitor of the Proteasome β5 subunit of the Plasmodium falciparum 20S proteasome (K_i = 371.7 nM). Proteasome-IN-9 preferentially binds the Plasmodium β5 catalytic subunit by recognizing differences in binding pocket residues, exhibits antimalarial activity against asexual blood-stage Plasmodium and stage V gametocytes, and shows synergistic effects when combined with Artemisinin (HY-B0094). Proteasome-IN-9 can be used for research on malaria.

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

CAS No.: 1418206-58-2
Formula: C₂₆H₄₇N₃O₅
Molecular Weight:481.67

Storage:

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

Proteasome-IN-9 Chemical Structure

CAS No.: 1418206-58-2

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

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

Biological Activity

Description

IC₅₀ & Target

^[1]

Plasmodium falciparum sporozoites

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC50	1240 nM	Cytotoxicity against human HepG2 cells assessed by bioluminescence viability after 48 hrs. Cytotoxicity against human HepG2 cells assessed by bioluminescence viability after 48 hrs.	28696697

In Vitro

Parasitic InfectionProtein/Amino Acid Metabolism

Parasitic Infection

Proteasome-IN-9 (6.7 μM-0.11 nM; 72 h) exhibits potent asexual blood-stage activity against P. falciparum Dd2 (IC₅₀: 3.27 nM), with low cytotoxicity against HepG2 cells (IC₅₀: 1240 nM) and a selectivity index of 379.2^[1].
Proteasome-IN-9 (12.5 μM) inhibits P. falciparum stage V gametocytes with an IC₅₀ of 130 nM^[1].
Proteasome-IN-9 (0.5-1 nM) acts synergistically with artemisinin in P. falciparum Dd2, enhancing artemisinin sensitivity at 0.5 and 1 nM, while producing no significant inhibition of parasite growth when used alone^[1].

Parasitic Infection

Protein/Amino Acid Metabolism

Proteasome-IN-9 (analog 18) (50-450 nM; 60-120 min) selectively inhibits the β5 subunit of the Plasmodium falciparum 20S proteasome, with a k_inact/K_I of 158.1 M^-1 s^-1 for Pf20S and a k_inact/K_I of 15.8 M^-1 s^-1 for human c20S^[1].
Proteasome-IN-9 (95 nM; 4 h) inhibits P. falciparum β5 proteasome activity by 40-60% in intact trophozoites^[1].

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

Chemical Information

CAS No. 1418206-58-2
Molecular Weight 481.67
Formula C₂₆H₄₇N₃O₅
SMILES

CCCCCC(N[C@H](C(C)C)C(N[C@@H](CCCC)C(N[C@@H](CC(C)C)C([C@]1(CO1)C)=O)=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

Handling Instructions (2659 KB)

References

[1]. LaMonte GM, et al. Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity. Journal of medicinal chemistry. 2017 Aug 10;60(15):6721-6732. [Content Brief]

Calculators

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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

Get Quote In-stock

Other size

Get Quote