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DTP3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DTP3图片
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
DTP3 TFA 是一种有效的选择性 GADD45β/MKK7 抑制剂。 DTP3 TFA 靶向 NF-κB 通路下游的一个重要的癌症选择性细胞存活模块。
化学名(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide
Canonical SMILESCC(N[C@H](CC1=CC=C(O)C=C1)C(N[C@H](CCCNC(N)=N)C(N[C@H](CC2=CC=CC=C2)C(N)=O)=O)=O)=O
分子式C26H35N7O5
分子量525.6
溶解度Soluble in DMSO
储存条件-20°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

DTP3 is an inhibitor of GADD45β/MKK7 complex [1].

GADD45β is an antiapoptotic factor regulated by NF-kB. MAP kinase kinase 7 (MKK7) is a JNK kinase. GADD45β/MKK7 complex is the downstream module of NF-κB and becomes a therapeutic target in multiple myeloma (MM) [1].

DTP3 is an inhibitor of GADD45β/MKK7 complex. DTP3 interacted with and caused a significant conformational change of GADD45β/MKK7 complex in a dose dependent way, as well as of the isolated MKK7 protein. DTP3 bound to MKK7 with KD value of 64.81 nM. By binding to MKK7, DTP3 dissociated the GADD45b/MKK7 complex through an allosteric mechanism and caused conformational rearrangement of the kinase. In both MM and non-MM cell lines with high expression of GADD45B, DTP3 inhibited cell growth and displayed potent and selective activity and was completely inactive in tumor cell lines with low GADD45B expression. Also, DTP3 effectively activated tumor necrosis factor α (TNFα, a potent inducer of JNK) and JNK [1].

In mice bearing myeloma xenografts, DTP3 (14.5 mg/kg/day) significantly inhibited tumor growth through induction of JNK activation and apoptosis [1].

Reference:
[1].  Tornatore L, Sandomenico A, Raimondo D, et al. Cancer-Selective Targeting of the NF-kB
Survival Pathway with GADD45b/MKK7 Inhibitors.  Cancer Cell, 2014, 26(4): 495-508.