20S Proteasome-IN-4_product_DataBase

Bioactivity	20S Proteasome-IN-4 (Compound 7) is a brain-penetrant, parasite-selective, orally active 20S proteasome inhibitor with an IC50 of 6.3 nM against T. b. brucei 20S proteasome. 20S Proteasome-IN-4 can be used for the research of human African trypanosomiasis (HAT)[1].
Target	IC50: 6.3 nM (T. b. brucei 20S proteasome)
Invitro	20S Proteasome-IN-4 (Compound 7) (24 h) inhibits T. b. brucei growth with an EC50 of <2.5 nM[1].
In Vivo	20S Proteasome-IN-4 (Compound 7) (3 mg/kg; i.g.; once a day for 4 days) cures a stage I mouse model of human African trypanosomiasis[1].20S Proteasome-IN-4 (15 mg/kg; i.g.; twice a day for 1 week) cures a stage II mouse model of human African trypanosomiasis[1]. Animal Model:
Name	20S Proteasome-IN-4
CAS	2827061-47-0
Formula	C20H18ClF2N3O3
Molar Mass	421.83
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Koester DC, et al. Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT). J Med Chem. 2022 Aug 22.

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