DTP3 TFA
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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
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