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533514 GADD45b/MKK7 Inhibitor, DTP3 - Calbiochem

Disrupts the GADD45b/KKK7 complex (Kd = 65 nM; IC₅₀ = 160 pM) and effectively and selectively kills multiple

GADD45b/MKK7 Inhibitor, DTP3 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: GADD45b/MKK7
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₆H₃₅N₇O₅·TFA

Products

Catalog NumberPackaging Qty/Pack
5.33514.0001 Glass bottle 10 mg
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
Global Trade Item Number
Catalog Number GTIN
5.33514.0001 04055977286984

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 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 3 months at -20°C.
Toxicity Standard Handling
ReferencesTomatore, L., et al. 2014. Cancer Cell. 26, 495.