X4753
XCT790
≥98% (HPLC), ERRα agonist, solid
别名:
3-[4-（2,4-双-三氟甲基苄氧基）-3-甲氧基苯基]-2-氰基-N-（5-三氟甲基-1,3,4-噻二唑-2-基）丙烯酰胺
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关于此项目
经验公式（希尔记法）:
C23H13F9N4O3S
化学文摘社编号:
分子量:
596.42
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
XCT790, ≥98% (HPLC), solid
SMILES string
COc1cc(ccc1OCc2ccc(cc2C(F)(F)F)C(F)(F)F)\C=C(/C#N)C(=O)Nc3nnc(s3)C(F)(F)F
InChI key
HQFNFOOGGLSBBT-AWNIVKPZSA-N
InChI
1S/C23H13F9N4O3S/c1-38-17-7-11(6-13(9-33)18(37)34-20-36-35-19(40-20)23(30,31)32)2-5-16(17)39-10-12-3-4-14(21(24,25)26)8-15(12)22(27,28)29/h2-8H,10H2,1H3,(H,34,36,37)/b13-6+
assay
≥98% (HPLC)
form
solid
color
yellow
solubility
DMSO: ≥10 mg/mL
storage temp.
2-8°C
Quality Level
相关类别
Application
XCT790已被用于：
- 在C2C12肌管中作为雌激素相关受体（ERR）α 的反向激动剂
- 作为雌激素相关受体（ERR）α 反向激动剂以阐明ERR的蜕膜功能α 子宫内膜胚胎干细胞中
- 作为人类神经母细胞瘤SH-SY5Y和HeLa细胞系中的自噬诱导剂。
Biochem/physiol Actions
XCT 790是一种5′腺苷单磷酸激活蛋白激酶（AMPK）激活剂。它还可充当线粒体中的质子离子载体和氧化磷酸化的解偶联剂。XCT790会破坏血管内皮生长因子（VEGF）和血管生成素2（Ang-2）的表达，并通过雌激素相关受体（ERRα）抑制表现出对子宫内膜肿瘤的抑制作用。XCT790可介导细胞周期停滞并促进三阴性乳腺癌（TNBC）的凋亡。
XCT790 是一种强效、特异性的 ERRα 反向激动剂。XCT790 具有选择性，在浓度低于 10 μM 时，对相关核受体（如 ERRγ 或 ERα）无明显拮抗活性。在使用 GAL4-ERR LBD 或全长 ERR 和 mSHP 启动子的瞬时转染试验中，IC 50 值为 300-500 nM。
XCT790 是一种强效、特异性的 ERRα 反向激动剂。选择性；在 10 μM 以下浓度时，对相关核受体，如 ERRγ 或 ERα 显示无明显拮抗活性。
hcodes
pcodes
Hazard Classifications
Aquatic Chronic 4
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
PengMing Sun et al.
Cancer management and research, 10, 2521-2535 (2018-08-22)
To explore the targeted therapy of estrogen-related receptor α (ERRα) in endometrial cancer (EC) cells and its potential mechanisms. The mRNA and protein expression levels of ERRα and estrogen receptor α (ERα) were detected by qPCR and Western blotting in
Sin-Aye Park et al.
British journal of cancer, 123(6), 988-999 (2020-06-24)
Gremlin-1 (GREM1), one of the bone morphogenetic protein antagonists, is involved in organogenesis, tissue differentiation and kidney development. However, the role of GREM1 in cancer progression and its underlying mechanisms remain poorly understood. The role of GREM1 in breast cancer
Banu Eskiocak et al.
Biochemistry, 53(29), 4839-4846 (2014-07-08)
XCT 790 is widely used to inhibit estrogen-related receptor α (ERRα) activity as an inverse agonist. Here, we report that XCT 790 potently activates AMP kinase (AMPK) in a dose-dependent and ERRα-independent manner, with active concentrations more than 25-fold below
Zhenyu Xu et al.
Theranostics, 10(9), 4201-4216 (2020-04-01)
Enhanced intratumoral androgen biosynthesis and persistent androgen receptor (AR) signaling are key factors responsible for the relapse growth of castration-resistant prostate cancer (CRPC). Residual intraprostatic androgens can be produced by de novo synthesis of androgens from cholesterol or conversion from
W F Theeuwes et al.
Biochimica et biophysica acta. Molecular cell research, 1867(2), 118610-118610 (2019-11-19)
In muscle cells, the peroxisome proliferator-activated receptor γ co-activator 1 (PGC-1) signaling network, which has been shown to be disturbed in the skeletal muscle in several chronic diseases, tightly controls mitochondrial biogenesis and oxidative substrate metabolism. Previously, we showed that
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