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K777

Catalog No. T15641Cas No. 233277-99-1
Alias APC-3316

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

K777

K777

Purity: 99.14%
Catalog No. T15641Alias APC-3316Cas No. 233277-99-1
K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.
Pack SizePriceAvailabilityQuantity
1 mg$78In Stock
5 mg$189In Stock
10 mg$297In Stock
25 mg$496In Stock
50 mg$728In Stock
1 mL x 10 mM (in DMSO)$436In Stock
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Purity:99.14%
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Product Introduction

Bioactivity
Description
K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.
Targets&IC50
CYP3A4:60 nM (IC50)
In vitro
K777 is a broad-spectrum antiviral and inhibits SARS-CoV, HCoV-229E, NL63, MERS-CoV, EBOV, SUDV, TAFV, RESTV, BEBOV, MARV and Nipah pseudovirus entry with IC50 values of 0.68 nM, 1.48 nM, 6.78 nM, 46.12 nM, 0.87 nM, 1.14 nM, 2.26 nM, 3.37 nM, 5.91 nM, 1.9 nM and 0.42 nM, respectively. K777 alone demonstrates up to 70% inhibition of 229E-S-mediated transduction in TMPRSS2 expressing cells. Simultaneous treatment with Camostat and K777 increases inhibition to ~ 90%[1]. K777 inhibits both CCL17 binding and CCL17-induced chemotaxis in Hut78 cells with IC50s of 57 and 8.9 nM, respectively. The K777-mediated inhibition of chemotaxis is potent even in the presence of a 10-fold higher concentration of CCL17. K777 induces CCR4 internalization with a 50% reduction of cell surface CCR4[3].
In vivo
In C57BL/6 IFN-γR-KO mice, K777 ( 35-105 mg/kg; p.o.) rescues mice from otherwise lethal infections[4].
AliasAPC-3316
Chemical Properties
Molecular Weight574.73
FormulaC32H38N4O4S
Cas No.233277-99-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 90 mg/mL (156.6 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.7399 mL8.6997 mL17.3995 mL86.9974 mL
5 mM0.3480 mL1.7399 mL3.4799 mL17.3995 mL
10 mM0.1740 mL0.8700 mL1.7399 mL8.6997 mL
20 mM0.0870 mL0.4350 mL0.8700 mL4.3499 mL
50 mM0.0348 mL0.1740 mL0.3480 mL1.7399 mL
100 mM0.0174 mL0.0870 mL0.1740 mL0.8700 mL

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