Boc-D(OMe)-FMK Inhibitor

• Applications: Func, B/N

Boc-D(OMe)-FMK Inhibitor Summary

• Immunogen: BOC-Asp (OMe)-CH2F
  BOC-D(OMe)-FMK
  BOC-D-FMK
• Preparation Method: Molecular Weight: 263
  Formula: C11H18FNO5
  Mass Spec: M+1=468.2
  TLC: Single-Spot (EtOAc: Hexane, 3.7) : Rf:0.5
  NMR: All functional groups are present

Applications/Dilutions

• Dilutions:
  • Block/Neutralize
  • In vitro assay
  • In vivo assay
• Application Notes: Use in blocking/ neutralizing reported in scientific literature (PMID 25096578) 1. This inhibitor is designed as a methyl ester to facilitate cell permeability. If the intended use is on purified or recombinant enzymes, esterase should be added to generate the free carboxyl groups. Please contact us for more details.
  2. For in-vivo or in-vitro experiments extending longer than 12 hrs, fresh inhibitor may have to be added to culture medium or injected into animals.

Packaging, Storage & Formulations

• Storage: Store at -20C. Avoid freeze-thaw cycles.
• Buffer: Form: White Semi-Solid
  Make a stock solution of 5, 10 or 20 mM in high purity DMSO (>99.9%). T

Alternate Names for Boc-D(OMe)-FMK Inhibitor

• BOC-Asp(OMe)-FMK
• BOC-D-FMK [BOC-Asp(OMe)-FMK
• BOC-D-FMK
• Boc-DOMe-FMK

Background

Members of the caspase family play key roles in apoptosis and inflammation. BOC-D(OMe)-FMK is a cell-permeable broad-spectrum caspase peptide inhibitor that irreversibly binds to the catalytic site of caspases proteases, and inhibits caspase-mediated apoptosis by preventing the processing of pro-caspases to their active forms (reviewed in 1-3). The BOC-D(OMe)-FMK peptide is O-methylated in the P position providing enhanced stability and increased cell permeability. BOC-D(OMe)-FMK (BOC-D-FMK) is typically used in assays to inhibit apoptosis. BOC-D-FMK has been used in many different types of apoptosis assays and published using a number of model system. Users may want to consult the literature for additional information regarding applications for BOC-D-FMK. The following search string is recommended for identifying references in PubMed using the BOC-D-FMK peptide inhibitor : BOC-D-FMK or BOC-FMK or BOC-ASP-FMK.

Limitations

This product is for research use only and is not approved for use in humans or in clinical diagnosis. Inhibitors are guaranteed for 1 year from date of receipt.

Publications for Boc-D(OMe)-FMK Inhibitor (NBP2-29395)(4)

Publications using NBP2-29395

• Tomasella A, Blangy A, Brancolini C. A Receptor-interacting Protein 1 (Rip1) Independent Necrotic Death Under The Control Of Protein Phosphatase Pp2a That Involves The Reorganization Of Actin Cytoskeleton And The Action Of Cofilin-1. J Biol Chem. 2014-08-05 [PMID: 25096578] (B/N)
  
  Details:
  BOC-D(OMe)-fmk used as pan-caspase inhibitor at 50 uM concentration in experiments involving U87MG, U-118MG, HT29, IMR90-E1A/Bcl2/C9DN cells and U87MG/Bcl-xL cells.
• Ryu Y, Hall CP, Reynolds CP, Kang MH. Caspase-dependent Mcl-1 cleavage and effect of Mcl-1 phosphorylation in ABT-737-induced apoptosis in human acute lymphoblastic leukemia cell lines. Exp. Biol. Med. (Maywood). 2014-06-20 [PMID: 24951472] (B/N, Human)
  
  Details:
  Fig 1a,b: Human acute lymphoblastic leukemia cell lines. Boc-D-FMK inhibited caspase-dependent Mcl-cleavage as measured by WB.
• Ontiveros SJ, Li Q, Jonsson CB. Modulation of apoptosis and immune signaling pathways by the Hantaan virus nucleocapsid protein. Virology. 2010-06-05 [PMID: 20227103]
• Caserta TM, Smith AN, Gultice AD et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003-08-01 [PMID: 12815277]
  
  Details:
  Inhibition of Actinomycin D or TGF beta induced apoptosis in WEHI 231 mouse cells, human Jurkat, or rat HRP-1 (trophoblast) cells: 1. BOC-D-FMK (IMI-2311): Fig 1 (gel analysis of DNA laddering) 2. Z-VAD-FMK (IMI-2310): Fig 1 (gel analysis of DNA laddering) 3. Q-VD-OPH (IMI-2309): Figs 1, 4, 5, 7 (gel analysis of DNA laddering), Figs 2, 3 (TUNEL assay by flow cytometry), Fig 6 (WB analysis of PARP cleavage), Fig 8 (WB analysis of Caspase-3, Caspase-8, and Caspase-9 cleavage) Note: Q-VD-OPH was extensively characterized in this publication and shown to inhibit the major features of apoptosis including caspase activation, DNA laddering, and caspase substrate cleavage.