K777 - 10mM in DMSO , CAS No.233277-99-1

CAS: 233277-99-1 Cat. No.: K654582 Formula: C₃₂H₃₈N₄O₄S Peso molecolare: 574.73 PubChem CID: 9851116

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC 50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi , and cathepsins B and L . K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC 50 values of 0.68 nM and 0.87 nM, respectively

In Vitro

K777 (K11777) can inhibit entry driven by other viral envelope proteins, including HIV-based pseudotypes bearing spikes from coronaviruses (SARS-CoV, HCoV-229E, NL63, MERS-CoV) or glycoproteins from filoviruses (EBOV, SUDV, TAFV, RESTV, BEBOV and MARV). K777 inhibits SARS-CoV, HCoV-229E, NL63, MERS-CoV, EBOV, SUDV, TAFV, RESTV, BEBOV, MARV and Nipah pseudovirus entry with IC 50 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. In contrast, 100 nM K777 does not inhibit infection mediated by envelope glycoproteins from an alphavirus (CHIKV), a rhabdovirus (VSV), a flavivirus (HCV), the retroviruses MLV-A and XMRV or two arenaviruses, Lassa and Junin virus. K777 alone demonstrates up to ~ 70% inhibition of 229E-S-mediated transduction. Simultaneous treatment with Camostat and K777 increases inhibition to ~ 90%. Similar inhibition patterns are obtained using the human intestinal epithelial cell line Caco-2, which express endogenous TMPRSS2 and cathepsins. K777 inhibits both CCL17 binding and CCL17-induced chemotaxis in Hut78 cells (IC 50 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. K777 does not inhibit CXCR4-induced chemotaxis or internalization and did not bring about Ca 2+ mobilization by itself. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

K777 (K11777; 35-105 mg/kg; oral administration; twice a day; for 10 days; C57BL/6 IFN-γR-KO mice) treatment rescues mice from otherwise lethal infections. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 IFN-γR-KO mice (6-8 weeks of age) injected with Cryptosporidium parvumDosage: 35 mg/kg, 70 mg/kg, and 105 mg/kg Administration: Oral administration; twice a day; for 10 days Result: Rescued mice from otherwise lethal infections.

IC50& Target:CCR4 CYP3

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC 50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

INHIBITOR

Nomi e identificatori

• Isomeri SMILES: CN1CCN(CC1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCC3=CC=CC=C3)/C=C/S(=O)(=O)C4=CC=CC=C4
• CAS alternativo: 502960-90-9
• PubChem CID: 9851116
• Termini MeSH: 4-methyl-N-((S)-1-oxo-3-phenyl-1-(((S)-1-phenyl-5- (phenylsulfonyl)pentan-3-yl)amino)propan-2-yl)piperazine-1-carboxamide;4-methylpiperazine-1-carboxylic acid(1-((3-benzenesufonyl-1-phenethylallyl)carbamoyl)-2-phenylethyl)amide;APC 3316;APC-3316;APC3316;C
• Peso molecolare: 574.73

Obiettivi associati (umani)

CTSL Tclin Cathepsin L1 (3 Activities)

Discover Target: CTSL

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CTSS Tchem Cathepsin S (1 Activities)

Discover Target: CTSS

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CTSB Tchem Cathepsin B (3 Activities)

Discover Target: CTSB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 233277-99-1, the molecular formula is C32H38N4O4S, and the molecular weight is 574.73 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.