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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      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
      Quality LevelMQ100
      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.