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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MEK (MAP2K)-DTP3
DTP3

Chemical Structure : DTP3

CAS No.: 1809784-29-9

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DTP3 (MKK7 inhibitor DTP3)

货号: 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 ￥1480 In stock
10 mg ￥2280 In stock
25 mg ￥3880 In stock
50 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 525.61
分子式 C26H35N7O5
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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