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530181 Prohibitin 2 Activator, ERAP - Calbiochem

530181
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Tableau de caractéristiques principal

Empirical Formula
C₁₃₉H₂₆₁N₆₉O₃₅S

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      Description
      OverviewA synthetic 13 aa peptide derived from the prohibitin 2 (PHB2)-binding domain of brefeldin A-inhibited guanine nucleotide-exchange protein 3 (BIG3; 165-QMLSDLTLQLRQR-177) linked to membrane-permeable polyarginine residues (11R) via a 3 glycine spacer. Enhances anti-tumor effects of tamoxifen in tamoxifen-resistant breast cancer cell lines. Directly targets PHB2 and blocks the formation of BIG-PHB2 complex in a reversible manner (Kd = 18.9 µM) and thereby reduces estrogen-dependent ERα phosphorylation in MCF-7 and KLP-3C cells. Synergistically suppresses estrogen-induced ERα transcriptional activity and growth of tumor cells (IC50 = 2.2 and 1.7 µM in MCF-7 and KPL-3C cells, respectively) by causing apoptosis and G1 arrest. Effective against a wide variety of breast cancer cell lines expressing ERα, BIG3, and PHB2 (Zr-75-1, HCC1500, BT-474, YMB-1, T47D, KPL-1, and HBC4), but does not affect MCF-10A normal mammary epithelial cells. Also shown to suppress the growth of tamoxifen-resistant MCF-7 and T47D xenografts in nude mice (14 mg/kg, i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530181
      Brand Family Calbiochem®
      SynonymsERα Activity-regulator Synthetic Peptide, Estrogen Receptor Signaling Regulator III; PHB2 Activator, 11R-GGG-QMLSDLTLQLRQR; (R)₁₁-(G)₃-QMLSDLTLQLRQR, H₂N-RRRRRRRRRRR~GGG~QMLSDLTLQLRQR-CO₂H
      References
      ReferencesYoshimaru, T., et al. 2013. Nat. Commun. 4, 2443.
      Product Information
      FormWhite solid
      Hill FormulaC₁₃₉H₂₆₁N₆₉O₃₅S
      Chemical formulaC₁₃₉H₂₆₁N₆₉O₃₅S
      Hygroscopic Hygroscopic
      ReversibleY
      Applications
      Biological Information
      Primary TargetPHB2
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Peptide SequenceH-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly~Gly-Gly~Gln-Met-Leu-Ser-Asp-Leu-Thr-Leu-Gln-Leu-Arg-Gln-Arg-OH
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      Prohibitin 2 Activator, ERAP - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Yoshimaru, T., et al. 2013. Nat. Commun. 4, 2443.
      Fiche technique

      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.

      Revision03-July-2014 JSW
      SynonymsERα Activity-regulator Synthetic Peptide, Estrogen Receptor Signaling Regulator III; PHB2 Activator, 11R-GGG-QMLSDLTLQLRQR; (R)₁₁-(G)₃-QMLSDLTLQLRQR, H₂N-RRRRRRRRRRR~GGG~QMLSDLTLQLRQR-CO₂H
      DescriptionThe BIG3, Brefeldin A-inhibited guanine nucleotide-exchange protein 3, prohibitin 2-/PHB2-binding sequence, BIG3165-177, is linked N-terminally to 11-Arg via a 3-Gly spacer to allow effective competition against BIG3 for PHB2 binding (Kd = 18.9 µM in binding studies using His-tagged human PHB27-244) and cellular delivery, freeing PHB2 from BIG3 for Estrogen Receptor-α/ERα binding, which in turn prevents Oestrogen-/E2-induced ERα phosphorylation and functional signaling complexes assemblies in breast cancer cultures (10 µM). PHB2-bound ERα is shown to associate with HDAC1 and corepressor NcoR, instead of the co-activator SRC-1, at TFF1 ERE and CCND1 AP-1-targeting sites in the nuclear and form a complex with IGF-1Rβ without Shc at the plasma membrane, negatively regulating E2-induced, ERα-dependent gene transcriptions and IGF-1Rβ-initiated signaling events, including PI 3-K/Akt and MAPK pathway activation. ERAP is reported to inhibit E2-dependent breast cancer growths both in cultures in vitro (Emax 5 to10 µM) and in mice in vivo (14 mg/kg via daily i.p.), including the Tamoxifen- (579000) resistant/TAM-R MCF-7 and T47D, without any apparent animal toxicity.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₃₉H₂₆₁N₆₉O₃₅S
      Peptide SequenceH-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Gly~Gly-Gly~Gln-Met-Leu-Ser-Asp-Leu-Thr-Leu-Gln-Leu-Arg-Gln-Arg-OH
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml) or H₂O (100 mg/ml). Use degassed H₂O.
      Storage -20°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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesYoshimaru, T., et al. 2013. Nat. Commun. 4, 2443.