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Chemical Structure : DTP3
CAS No.: 1809784-29-9
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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|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
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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.
| M.Wt | 525.61 | |
| Formula | C26H35N7O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide |
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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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