533514 GADD45b/MKK7 Inhibitor, DTP3 - Calbiochem

533514
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₆H₃₅N₇O₅·TFA

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      5.33514.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell permeable, bioavailable D-tripeptide that specifically binds to MKK7 in 1:1 stoichiometry and disrupts the GADD45b/MKK7 complex in an allosteric mechanism (Kd = 65 nM, IC50 = 160 pM). Does not affect the activity of 142 other protein kinases. Exhibits potent and selective activity in both multiple myeloma (MM) and non-MM cell lines expressing high levels of GADD45b, however, it is completely inactive in tumor cells featuring low GADDb expression. Displays potency similar to bortezomib, but has about 100-fold greater selectivity for cancer cells, and unlike bortezomib, it does not display any toxic effects in normal cell lines. Shown to activate JNK, but does not affect p38, ERK, or IKK/NF-κB signaling in sensitive GADD45b dependent MM cell lines. Abolishes the growth of myeloma xenografts in mice (14.5 mg/kg/day) and retains anticancer activity in an orthotopic xenograft model of MM. Displays desirable pharmacokinetic profile (t1/2 = 1.26 h and AUC = 6.43 mg/h/ml; at ~10 mg/kg, i.v).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533514
          Brand Family Calbiochem®
          Synonyms(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide trifluoroacetate, GADD45b-MKK blocker
          References
          ReferencesTomatore, L., et al. 2014. Cancer Cell. 26, 495.
          Product Information
          FormWhite solid
          FormulationSupplied as a HCl salt.
          Hill FormulaC₂₆H₃₅N₇O₅·TFA
          Chemical formulaC₂₆H₃₅N₇O₅·TFA
          Hygroscopic Hygroscopic
          ReversibleY
          Applications
          Biological Information
          Primary TargetGADD45b/MKK7
          Primary Target K<sub>i</sub>65 nM, IC₅₀
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          Peptide SequenceAc-YRF-NH2
          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 +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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          GADD45b/MKK7 Inhibitor, DTP3 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Tomatore, L., et al. 2014. Cancer Cell. 26, 495.
          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.

          Revision09-December-2016 JSW
          Synonyms(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide trifluoroacetate, GADD45b-MKK blocker
          DescriptionA cell permeable, bioavailable D-tripeptide that specifically binds to MKK7 in 1:1 stoichiometry and disrupts the GADD45b/MKK7 complex in an allosteric mechanism (Kd = 65 nM, IC50 = 160 pM). Does not affect the activity of 142 other protein kinases. Exhibits potent and selective activity in both multiple myeloma (MM) and non-MM cell lines expressing high levels of GADD45b, however, it is completely inactive in tumor cells featuring low GADDb expression. Displays potency similar to bortezomib, but has about 100-fold greater selectivity for cancer cells, and unlike bortezomib, it does not display any toxic effects in normal cell lines. Shown to activate JNK, but does not affect p38, ERK, or IKK/NF-κB signaling in sensitive GADD45b dependent MM cell lines. Abolishes the growth of myeloma xenografts in mice (14.5 mg/kg/day) and retains anticancer activity in an orthotopic xenograft model of MM. Displays desirable pharmacokinetic profile (t1/2= 1.26 h and AUC = 6.43 mg/h/ml; at ~10 mg/kg, i.v).
          FormWhite solid
          FormulationSupplied as a HCl salt.
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₆H₃₅N₇O₅·TFA
          Peptide SequenceAc-YRF-NH2
          Purity≥98% by HPLC
          SolubilityDMSO (100 mg/ml) or H₂O (100 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesTomatore, L., et al. 2014. Cancer Cell. 26, 495.