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DTP3 JNK activator

Cat.No.S7637

DTP3 is a selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor and is able to restore MKK7/JNK activation. This compound inhibits cancer-selective NF-κB survival pathway.
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Quality Control

Batch: Purity: 99.93%
99.93

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (190.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 525.6 Formula

C26H35N7O5

Storage (From the date of receipt)
CAS No. 1809784-29-9 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES CC(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CC2=CC=CC=C2)C(=O)N

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Mechanism of Action

Targets/IC50/Ki
GADD45β/MKK7
NF-κB
In vitro

DTP3 physically interacts with MKK7, both in isolation and within the complex with GADD45β, and dissociates the GADD45β/MKK7 complex via an allosteric mechanism. This compound selectively kills cells and induces apoptosis in MM cells with functional MKK7 and elevated GADD45β expression without toxicity to normal cells. In addition, it displays synergistic activity with bortezomib in two different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells.

Kinase Assay
DTP3 Binding Assays
The stoichiometry and KD value of the DTP3/MKK7 interaction are determined by tryptophan fluorescence quenching analysis, after fitting the fluorescence data with a nonlinear regression algorithm.
In vivo

DTP3 (14.5 mg/kg/day) exhibits potent antitumor activity against MM in mouse plasmacytoma model.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-06-12)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07005726 ENROLLING_BY_INVITATION
Infant Morbidity; Infant Mortality; Non-Specific Effects of Vaccines; BCG
Bandim Health Project
2025-05-09 PHASE4
NCT00244673 COMPLETED
Mortality; Hospitalization; Adverse Events
Bandim Health Project
2005-10 PHASE4

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