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

Beclin-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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Atg6 Activator I, Beclin1-GAPR-1 Interaction Blocker I, Vps30 Activator I, H₂N-YGRKKRRQRRR-GG-TNVFNATFEIWHDGEFGT-CO₂H, Autophagy Inducer IV

Primary Target: GAPR-1/GLIPR2
506048
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₆₄H₂₅₁N₅₇O₄₅

Products

Catalogue NumberPackaging Qty/Pack
5.06048.0001 Glass bottle 10 mg
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
Quality LevelMQ100
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
Global Trade Item Number
Catalogue Number GTIN
5.06048.0001 04055977262704

Documentation

Beclin-1 Activator I, TAT-Beclin-1 - Calbiochem 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 Protect from light
+2°C to +8°C
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.
Toxicity Standard Handling
ReferencesLiu, Y., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 20634.
Shoji-Kawata, S., et al. 2013. Nature. 494, 201.