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质量水平
检测方案
≥98% (HPLC)
形式
solid
颜色
yellow
溶解性
DMSO: ≥10 mg/mL
储存温度
2-8°C
SMILES字符串
COc1cc(ccc1OCc2ccc(cc2C(F)(F)F)C(F)(F)F)\C=C(/C#N)C(=O)Nc3nnc(s3)C(F)(F)F
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+
InChI key
HQFNFOOGGLSBBT-AWNIVKPZSA-N
应用
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。
生化/生理作用
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。
危险声明
预防措施声明
危险分类
Aquatic Chronic 4
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
G Vargas et al.
Oncogene, 38(7), 950-964 (2018-11-28)
Bone is the most common metastatic site for breast cancer. Estrogen-related-receptor alpha (ERRα) has been implicated in cancer cell invasiveness. Here, we established that ERRα promotes spontaneous metastatic dissemination of breast cancer cells from primary mammary tumors to the skeleton.
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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