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Cat. No.: HY-182443

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PEX5-PEX14 PPI-IN-4

PEX5-PEX14 PPI-IN-4 is a potent PEX14-PEX5 PPI inhibitor, with EC₅₀ values of 7.78 μM, 27.5 μM and 9.31 μM against the protein-protein interactions of TbPEX14-PEX5, TcPEX14-PEX5 and HsPEX14-PEX5, respectively. PEX5-PEX14 PPI-IN-4 exhibits trypanocidal activity against Trypanosoma brucei rhodesiense and Trypanosoma cruzi. PEX5-PEX14 PPI-IN-4 shows cytotoxic activity against mammalian cells. PEX5-PEX14 PPI-IN-4 can be used in the research of human African trypanosomiasis and Chagas disease.

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

CAS No.: 1884470-47-6
Formula: C₃₆H₄₁N₅O₃
Molecular Weight:591.74

Storage:

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

PEX5-PEX14 PPI-IN-4 Chemical Structure

CAS No.: 1884470-47-6

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Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	6.5 μM Compound: 61	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 66 hrs by resazurin dye based fluorescence assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 66 hrs by resazurin dye based fluorescence assay	[PMID: 31860309]

In Vitro

PEX5-PEX14 PPI-IN-4 (Compound 61) inhibits T. brucei growth with an EC₅₀ of 0.503 μM and HepG2 cell growth with an EC₅₀ of 6.50 μM, yielding a selectivity index of 12.9^[1].
PEX5-PEX14 PPI-IN-4 inhibits T. b. rhodesiense, T. cruzi, and L6 cell growth with IC₅₀ values of 0.029 μM, 2.20 μM, and 1.82 μM, respectively, and has a selectivity index of <1 relative to T. cruzi^[1].

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

Chemical Information

CAS No. 1884470-47-6
Molecular Weight 591.74
Formula C₃₆H₄₁N₅O₃
SMILES

O=C(C1=NN(CCNC(C)(CO)C)C2=C1CN(CC2)CC3=CC=C(C4=C3C=CC=C4)OC)NCC5=CC=CC6=C5C=CC=C6
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]. Dawidowski M, et al. Structure–activity relationship in pyrazolo [4, 3-c] pyridines, first inhibitors of PEX14–PEX5 protein–protein interaction with trypanocidal activity. Journal of medicinal chemistry. 2019 Dec 20;63(2):847-79.

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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.

Keywords

100 mg

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