2. Metabolic Enzyme/Protease Anti-infection
  3. Proteasome Parasite
  4. 20S Proteasome-IN-4

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).

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

20S Proteasome-IN-4 Chemical Structure

20S Proteasome-IN-4 Chemical Structure

CAS No. : 2827061-47-0

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20S Proteasome-IN-4 Related Antibodies

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Description

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].

IC50 & Target

IC50: 6.3 nM (T. b. brucei 20S proteasome)[1]
In Vitro

20S Proteasome-IN-4 (Compound 7) (24 h) inhibits T. b. brucei growth with an EC50 of <2.5 nM[1].

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

20S Proteasome-IN-4 Related Antibodies
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].

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

Animal Model: NMRI mice, hemolymphatic mice model (Stage I)[1]
Dosage: 3 mg/kg
Administration: Oral gavage, once a day for 4 days
Result: Achieved complete cure of the stage I infection.
Animal Model: CD1 mice, meningoncephalic mice model (stage II)[1]
Dosage: 15 mg/kg
Administration: Oral gavage, twice a day for 1 week
Result: Achieved complete cure of the stage II infection.
Animal Model: BALB/c mice and Wistar rats[1]
Dosage: 1 mg/kg or 3 mg/kg
Administration: Intravenous or oral administration (Pharmacokinetic Analysis)
Result: ADME and PK Data for 20S Proteasome-IN-4 (Compound 7)[1]
cmp solubility pH 6.8 μM LM CLint (m/r) [μL/min/mg] LM scaled CLint [mL/min/kg] (m/r) fu plasma [%] (m/r) CLp [mL/min/kg] (m/r) CLu [mL/min/kg] (m/r) AUCPO [μM•h] (m/r) AUCIV [μM•h] (m/r) %F m/r
20S Proteasome-IN-4 12 79/66 311/119 1.0/1.6 17/9 1700/563 5.2/17 2.3/4.4 76/128

Solubility: Miniaturized shake flask solubility in phosphate buffer; fu,plasma from PPB; LM scaled Clint = (LM Clint•SF1•SF2)/1000 with SF1 (mg protein per g liver) m,r = 45, SF2 (g liver per kg BW); m = 87.5, SF2 r = 40. Unbound clearance: Clp = Clu/fu, with Clp observed clearance. Mouse and rat PK 1 mpk IV/3 mpk PO.
Molecular Weight

421.83

Formula

C20H18ClF2N3O3
CAS No.
SMILES

ClC1=CC=C2C(C(NC3=CC=CC(F)=C3F)=CC(C(NC[C@H](CO)OC)=O)=N2)=C1
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
References
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20S Proteasome-IN-4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    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.

Keywords:

20S Proteasome-IN-42827061-47-0ProteasomeParasitehuman African trypanosomiasisHATAfrican sleeping sicknessbrain-penetrantparasite-selectiveorally active20S proteasomeT. b. bruceiInhibitorinhibitorinhibit

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