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DTP3

Chemical Structure : DTP3

CAS No.: 1809784-29-9

DTP3 (MKK7 inhibitor DTP3)

Catalog No.: PC-72696Not For Human Use, Lab Use Only.

DTP3 (MKK7 inhibitor DTP3) is a specific D-tripeptide that disrupts the GADD45β/MKK7 complex (Kd=64.8 nM), kills MM cells effectively, and lacks toxicity to normal cells.

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Biological Activity

DTP3 (MKK7 inhibitor DTP3) is a specific D-tripeptide that disrupts the GADD45β/MKK7 complex (Kd=64.8 nM), kills MM cells effectively, and lacks toxicity to normal cells.
DTP3 bind to MKK7, but not to GADD45β, DTP3 dissociates the GADD45β/MKK7 complex via an allosteric mechanism, potentially involving a conformational rearrangement of the kinase.
DTP3 demonstrated potent and cancer-selective activity in MM cells from patients, effectively kills MM cells by inducing MKK7/JNK-dependent apoptosis, displayed synergistic activity with bortezomib in different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells.
DTP3 exhibited potent therapeutic activity against MM in vivo, in the absence of any apparent side effects.

Physicochemical Properties

M.Wt 525.61
Formula C26H35N7O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide

References

1. Laura Tornatore, et al. Cancer Cell. 2014 Oct 13;26(4):495-508.

2. Laura Tornatore, et al. Toxicol Rep. 2019 Apr 19;6:369-379.

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