530181 Prohibitin 2 Activator, ERAP - Calbiochem

530181
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₃₉H₂₆₁N₆₉O₃₅S

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      5.30181.0001
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          Glass bottle 10 mg
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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 SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Yoshimaru, T., et al. 2013. Nat. Commun. 4, 2443.
          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.

          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.