DG-172 (hydrochloride)
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.
DG-172 (hydrochloride) is an orally available inverse agonist of PPARβ/δ with IC50 value of 27 nM [1].
Peroxisome proliferator-activated receptors (PPARs) are a member of the class II subset of nuclear receptors. The three PPAR subtypes (PPARα, PPARβ/δ, and PPARγ) regulate their target genes through binding to specific DNA elements (PPREs) as obligatory heterodimers with the retinoid X receptor. PPRE-bound PPARβ/δ complexes have functions in both transcriptional repression and transcriptional activation [1].
DG-172 is a novel PPARβ/δ-selective ligand and an orally available PPARβ/δ inverse agonist with IC50 value of 27 nM. In a cell-based assay, DG-172 efficiently antagonized ligand activation of PPARβ/δ. In C2C12 mouse myoblasts, DG-172 inhibited the expression of PPARβ/δ target gene Angptl4 with IC50 value of 9.5 nM. In WPMY-1 human myofibroblasts, DG-172 induced an enhanced recruitment of HDAC3 to the ANGPTL4 gene [1]. DG172 strongly increased GM-CSF-induced differentiation of primary BMCs into two specific populations, mature and immature dendritic cells (DCs) [2]. DG172 strongly inhibited the serum- and transforming growth factor b (TGFb)-induced invasion of MDA-MB-231 human breast cancer cells into a three-dimensional matrigel matrix [3].
References:
[1]. Lieber S, Scheer F, Meissner W, et al. (Z)-2-(2-bromophenyl)-3-{[4-(1-methyl-piperazine)amino]phenyl}acrylonitrile (DG172): an orally bioavailable PPARβ/δ-selective ligand with inverse agonistic properties. J Med Chem. 2012 Mar 22;55(6):2858-68.
[2]. Lieber S, Scheer F, Finkernagel F, et al. The inverse agonist DG172 triggers a PPARβ/δ-independent myeloid lineage shift and promotes GM-CSF/IL-4-induced dendritic cell differentiation. Mol Pharmacol. 2015 Feb;87(2):162-73.
[3]. Adhikary T, Brandt DT, Kaddatz K, et al. Inverse PPARβ/δ agonists suppress oncogenic signaling to the ANGPTL4 gene and inhibit cancer cell invasion. Oncogene. 2013 Oct 31;32(44):5241-52.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 455.2 |
Cas No. | 1361504-77-9 |
Formula | C20H20BrN3·2HCl |
Solubility | ≤20mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide |
Chemical Name | 2-bromo-αZ-[[4-(4-methyl-1-piperazinyl)phenyl]methylene]-benzeneacetonitrile, dihydrochloride |
SDF | Download SDF |
Canonical SMILES | CN1CCN(C2=CC=C(/C=C(C#N)/C3=C(Br)C=CC=C3)C=C2)CC1.Cl.Cl |
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。 |