506048 | Beclin-1 Activator I, TAT-Beclin-1 - Calbiochem

506048
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆₄H₂₅₁N₅₇O₄₅

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.06048.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable Atg6/Beclin1-derived autophagy-inducing peptide (Minimum effective conc. ≤10 µM for 3 h) that effectively activates cellular Beclin1 by competing against Beclin1 for binding to its negative regulator GAPR-1/GLIPR2 on the Golgi surface. Shown to induce autosis, autophagy-dependent death, in cells of human, rat, and murine origin in a dose- and time-dependent manner (Minimum effective conc. >5 µM for 5 h in HeLa cultures), blockable by autophagy inhibitor 3-MA (10 mM, Cat. no.189490; [T-B] = 20 µM) or via Na+/K+-ATPase inhibition, but insensitive to Z-VAD-FMK (Cat. no. 219007) or Nec-1 (Cat. nos. 480065 & 505224) treatment. Non-cytotoxic autophagy induction with lower doses of Tat-Beclin1 and shorter exposure times is therapeutically beneficial in blocking RNA viral replications both in cultures (4 h 10 µM peptide treatment 4 h post viral infection in HeLa cultures; 0.5-5 µM peptide pre-treatment 24 h before HIV infection in human MDM cultures) in vitro and in CHIKV-infected neonatal mice (15 mg/kg/day i.p.) in vivo. While Tat-Beclin1 bioavailability is limited to the peripheral tissues in mice, a peptide based on Tat-Beclin1 retro-inverso sequence (Cat. no. 506416) shows efficacy in a murine model of neonatal WNV CNS infection. Note: increased drug potency is reported in acidified (pH 7.0) serum-free cultures.
          Catalogue Number506048
          Brand Family Calbiochem®
          SynonymsAtg6 Activator I, Beclin1-GAPR-1 Interaction Blocker I, Vps30 Activator I, H₂N-YGRKKRRQRRR-GG-TNVFNATFEIWHDGEFGT-CO₂H, Autophagy Inducer IV
          References
          ReferencesLiu, Y., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20634.
          Shoji-Kawata, S., et al. 2013. Nature. 494, 201.
          Product Information
          DeclarationSold under license of US Patent 8,722,628.
          FormWhite powder
          FormulationSupplied as a trifluoroacetate salt.
          Hill FormulaC₁₆₄H₂₅₁N₅₇O₄₅
          Chemical formulaC₁₆₄H₂₅₁N₅₇O₄₅
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          ApplicationBeclin-1 Activator I, TAT-Beclin-1, is a cell-permeable Atg6/Beclin1-derived autophagy-inducing peptide. Activates Beclin1 by competing against its negative regulator GAPR-1/GLIPR2.
          Biological Information
          Primary TargetGAPR-1/GLIPR2
          Purity≥97% by HPLC
          Physicochemical Information
          Cell permeableY
          Peptide SequenceH-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg~Gly-Gly~Thr-Asn-Val-Phe-Asn-Ala-Thr-Phe-Glu-Ile-Trp-His-Asp-Gly-Glu-Phe-Gly-Thr-OH
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Liu, Y., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20634.
          Shoji-Kawata, S., et al. 2013. Nature. 494, 201.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision26-February-2015 JSW
          SynonymsAtg6 Activator I, Beclin1-GAPR-1 Interaction Blocker I, Vps30 Activator I, H₂N-YGRKKRRQRRR-GG-TNVFNATFEIWHDGEFGT-CO₂H, Autophagy Inducer IV
          DescriptionA cell-permeable autophagy-inducing peptide (Minimum effective conc. ≤10 µM assessed by increased LC3-II/LC3-I ratio & p62 downregulation post 3 h treatment in A549, COS-7, HBEC30-KT, HCC827, HeLa, MEF, THP-1 cultures) that is composed of essential HIV-1 virulence factor Nef-binding sequence derived from human Atg6/Beclin1 (aa 267-284) evolutionarily conserved domain (ECD) with substitutions at three non-species-conserved residues (H275E, S279D, and Q280E) for enhanced solubility and N-terminally fused to the membrane-permeant HIV-1 Tat protein transduction domain (PTD) sequence (aa 47-57) via a -Gly-Gly- linkage to facilitate cellular delivery and Beclin1 activation via competitive binding to its negative regulator "Golgi-associated plant pathogenesis-related protein-1" (GAPR-1/GLIPR2) on the Golgi surface. Shown to effectively induce autosis, autophagy-dependent death morphologically and pharmacologically distinct from apoptosis and necrosis, in various cell cultures of human, rat, and murine origin in a dose- and time-dependent manner (Minimum effective conc. >5 µM post 5 h treatment as assessed by HeLa Trypan blue staining; Fold of control Trypan blue-positive population/20 µM peptide exposure time = 3/1 h, 9/4 h, 20/8 h), blockable by autophagy inhibitor 3-MA (10 mM, Cat. no. 189490; [T-B] = 20 µM) or via Na+/K+-ATPase inhibition by cardiac glycosides, but insensitive to Z-VAD-FMK (Cat. no. 219007) or Nec-1 (Cat. nos. 480065 & 505224) treatment. Autophagy induction by Tat-Beclin1 treatment is also reported to result in clearance of small (<1 µm) CFP-htt103Q aggregates in HeLa cells (59% and 85% reduction, respectively, of aggregates-positive population and average aggregates per cell; 20 µM/4h/d for 2 d) and non-cytotoxic autophagy induction with lower level of Tat-Beclin1 dosage and limited exposure time is demonstrated to be therapeutically beneficial in blocking RNA viral replications both in cultures (4 h, 10 µM peptide treatment 4 h post CHIKV, SINV, or WNV infection in HeLa cultures; 0.5-5 µM peptide pre-treatment 24 h prior to HIV infection in human MDM cultures) in vitro and in CHIKV-inoculated neonatal mice (15 mg/kg/day i.p.) in vivo. While Tat-Beclin1 bioavailability is limited to the peripheral tissues in mice, a peptide based on Tat-Beclin1 retro-inverso sequence (Cat. no. 506416) shows efficacy in a murine model of neonatal WNV CNS infection. Note: increased drug potency is reported in acidified (pH 7.0) serum-free cultures.
          FormWhite powder
          FormulationSupplied as a trifluoroacetate salt.
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₆₄H₂₅₁N₅₇O₄₅
          Peptide SequenceH-Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg~Gly-Gly~Thr-Asn-Val-Phe-Asn-Ala-Thr-Phe-Glu-Ile-Trp-His-Asp-Gly-Glu-Phe-Gly-Thr-OH
          Purity≥97% by HPLC
          SolubilityDMSO (50 mg/ml) or H₂O (50 mg/ml)
          Storage +2°C to +8°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesLiu, Y., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20634.
          Shoji-Kawata, S., et al. 2013. Nature. 494, 201.