2. Anti-infection Metabolic Enzyme/Protease Apoptosis
  3. SARS-CoV Cathepsin Apoptosis Caspase
  4. Z-FA-FMK

Z-FA-FMK  (Synonyms: (1S)-Z-FA-FMK)

Cat. No.: HY-P0109A Purity: 98.54%
COA Handling Instructions

Z-FA-FMK ((1S)-Z-FA-FMK) is a potent Cathepsin B and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host.

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

Z-FA-FMK Chemical Structure

Z-FA-FMK Chemical Structure

CAS No. : 197855-65-5

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5 mg USD 264 In-stock
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Based on 2 publication(s) in Google Scholar

Z-FA-FMK Related Antibodies

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Description

Z-FA-FMK ((1S)-Z-FA-FMK) is a potent Cathepsin B and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host[1][2][3].

IC50 & Target[1]

Cathepsin B

 

cathepsin L

 

Caspase-2

 

Caspase-3

 

Caspase-6

 

Caspase-7

 

In Vitro

Z-FA-FMK ((1S)-Z-FA-FMK; 5-100 μM; 1 h; Jurkat cells) reduces levels of DEVDase activity and DNA fragmentation. Z-FA-FMK inhibits the externalization of phosphatidylserine induced by either MX2870-1 or MX781[1].
Z-FA-FMK (100 μM; 1 h; Jurkat cells) inhibits apoptosis. Z-FA-FMK inhibited the induction of DEVDase activity not only by the RRMs but also by other apoptotic insults, including etoposide-, ceramide-, and CD95/Fas receptor-mediated pathways[1].
Z-FA-FMK (0-100 μM; 1 h; Jurkat cells) inhibits caspases 2, -3, -6, and -7 activity through repressed induction of DEVDase activity in Jurkat cells[1].
Z-FA-FMK (0-20 μM; 48 h; HT1080 and mouse embryonic stem cells) blocks reoviral replication and cures cells of a persistent infection with reovirus in vitro[2].
Z-FA-FMK (20 μM; 48 h; HT1080 cells) induces defects in reoviral maturation[2].

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

Z-FA-FMK Related Antibodies
In Vivo

Z-FA-FMK (1 mg/kg; intratumor injection; every 2 d, for 27 d; SCID mice with HT1080 xenograft) blocks reovirus infection in vivo[2].
Z-FA-FMK (8 mg/kg; i.v.; every 2 d, once; male BALB/c mice) markedly lessens the degree of impairment seen in D-GalN/TNF-α-induced kidney injury[3].

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

Animal Model: SCID mice with HT1080 xenograft (6-8 weeks)[2]
Dosage: 1 mg/kg
Administration: Intratumor injection; every 2 days, for 27 days
Result: Blocked reovirus replication activity in both tumor and heart tissues.
Animal Model: Male BALB/c mice[3]
Dosage: 8 mg/kg
Administration: Intravenous injection; once, 1 hour later, intraperitoneal injection D-GalN (700 mg/kg) and TNF-α (15 μg/kg).
Result: Decreased in the D-GalN/TNF-α-induced degenerative changes.
Decreased in the number of activated caspase-3-positive tubular epithelial cell.
Increased in kidney GSH levels, CAT, SOD and GPx activities and decreased in kidney LPO levels, LDH activity, serum AST and ALT activities, uric acid, and urea levels were determined.
Molecular Weight

386.42

Appearance

Solid

Formula

C21H23FN2O4
CAS No.
SMILES

O=C(OCC1=CC=CC=C1)N[C@@H](CC2=CC=CC=C2)C(NC(C)C(CF)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (646.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5879 mL 12.9393 mL 25.8786 mL
5 mM 0.5176 mL 2.5879 mL 5.1757 mL
10 mM 0.2588 mL 1.2939 mL 2.5879 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.54%

COA (247 KB) HNMR (271 KB) RP-HPLC (96 KB)

Handling Instructions (2659 KB)
References
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Z-FA-FMK Related Classifications

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.

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Keywords:

Z-FA-FMK197855-65-5(1S)-Z-FA-FMKSARS-CoVCathepsinApoptosisCaspaseSARS coronavirusRRMsDEVDaseDNA fragmentationexternalization of phosphatidylserinereovirus replicationInhibitorinhibitorinhibit

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