DTP3 TFA
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
DTP3是一种GADD45β/MKK7复合体的抑制剂[1].
GADD45β是一种受NF-κB调控的抗凋亡因子.MAP激酶激酶7(MKK7)是一种JNK激酶.GADD45β/MKK7复合体是NF-κB的下游模块,是多发性骨髓瘤(MM)的治疗靶点[1].
DTP3是GADD45β/MKK7复合体的抑制剂.DTP3可以剂量依赖的方式与GADD45β/MKK7复合体及分离的MKK7蛋白相互作用并引起显著的构象变化.DTP3可结合MKK7,KD值为64.81 nM.通过结合MKK7,DTP3通过别构机制使GADD45b/MKK7复合体解离,引起酶的构象重排.在高表达GADD45B的MM和非MM细胞系中,DTP3可抑制细胞生长,具有有效和选择性的活性,但在低表达GADD45B的肿瘤细胞系中完全失活.另外,DTP3可有效活化肿瘤坏死因子α(TNFα,一种有效的JNK诱导物)和JNK[1].
在骨髓瘤异种移植小鼠中,DTP3(14.5 mg/kg/天)可诱导JNK激活和细胞凋亡,显著抑制肿瘤生长[1].
参考文献:
[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.
Storage | Store at -20°C |
M.Wt | 639.63 |
Cas No. | 1809784-29-9 (free-base) |
Formula | C28H36F3N7O7 |
Solubility | ≥52.7 mg/mL in DMSO; ≥50.5 mg/mL in EtOH; ≥49.7 mg/mL in H2O |
Chemical Name | (R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide 2,2,2-trifluoroacetate |
SDF | Download SDF |
Canonical SMILES | O=C(C)N[C@H](CC1=CC=C(O)C=C1)C(N[C@H](CCCNC(N)=N)C(N[C@@H](C(N)=O)CC2=CC=CC=C2)=O)=O.OC(C(F)(F)F)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
![DTP3 TFA](http://www.apexbt.com//media/diy/images/struct/B4886.png)