21
2
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7904 |
SR 19881
|
Estrogen/progestogen Receptor | Endocrinology/Hormones |
SR 19881 是 ERRγ 的完全激动剂(结合试验中的 EC50 值为 0.39 μM,基于细胞的试验中 EC50 值为 4.7 μM)。 | |||
T5835 |
PROTAC ERRα ligand 2
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
PROTAC ERRα ligand 2 是雌激素相关受体 α (ERRα)反向激动剂。它对 ERRα (IC50=5.67 nM) 的抑制作用比 XCT790 (IC50=61.3 nM) 高效约 11 倍。 | |||
T15191 |
PROTAC ERRα ligand 1
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor | Endocrinology/Hormones |
PROTAC ERRα ligand 1 是一种雌激素相关受体 α (ERRα) 拮抗剂,能够作用于 ERRα (IC50:0.04 μM)和 ERRγ (IC50:2.8 μM)。 | |||
T0593 |
XCT790
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Autophagy | Autophagy; Endocrinology/Hormones |
XCT790 是 ERRα的一种选择性反向激动剂,IC50值为 0.37 μM。它在化疗过程中诱导癌细胞死亡。 | |||
T8370 |
GSK5182
|
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Reactive Oxygen Species | Endocrinology/Hormones; Immunology/Inflammation; Metabolism; NF-κB |
GSK5182 是高效选择性,具有口服活性的 ERRγ反向激动剂,其 IC50=79 nM,且不与其他核受体相互作用,包括 ERRα 和 ERα。它还能增加肝癌细胞中 reactive oxyen species (ROS)的产生。 | |||
T7709 |
(E/Z)-GSK5182
GSK5182(Z/E) |
Estrogen/progestogen Receptor; ROS | Endocrinology/Hormones; Immunology/Inflammation |
(E/Z)-GSK5182 (GSK5182(Z/E)) 是 (E)-GSK5182 和 (Z)-GSK5182 的外消旋体。GSK5182 是一种具有高效选择性和口服活性的ERRγ的反向激动剂,其IC50值为 79 nM。GSK5182 还诱导肝癌细胞中活性氧 (ROS)的产生。 | |||
T11230 |
ERRα antagonist-1
ERR+/- antagonist-1,ERRa antagonist-1 |
Estrogen/progestogen Receptor | Endocrinology/Hormones |
ERRα antagonist-1 (ERR+/- antagonist-1) 是一种选择性的,高亲和力的雌激素相关受体α (ERRα) 拮抗剂。ERRα antagonist-1 抑制 ERRα 与增殖物激活的受体γ共激活因子 1α (PGC-1α) 和 PGC-1β 的相互作用,IC50 值分别为 170 nM 和 180 nM。ERRα antagonist-1 不抑制 ERRβ 或 ERRγ 与 PGC-1α 和 PGC-1β 共激活剂的相互作用,也不抑制 ERα 或 ERβ 与 PGC-1α 或 SRC-1 的相互作用。 | |||
T77577 |
SLU-PP-332
|
Estrogen/progestogen Receptor | Endocrinology/Hormones |
SLU-PP-332 是一种泛雌激素受体相关受体 (ERR) 激动剂,其对 ERRα, ERRβ 以及 ERRγ 具有很高的亲和力,EC50 值分别为 98、230 以及 430 nM。SLUPP-332 可增强骨骼肌细胞系的线粒体功能和细胞呼吸,增加 IIa 型氧化骨骼肌纤维并增强了运动耐力。SLU-PP-332 具有研究代谢性疾病以及肌肉功能改善的潜力,可能用于改善代谢紊乱和衰老。 | |||
T18609 |
PROTAC ERRα Degrader-2
|
Others | Others |
PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1]. | |||
T13700 |
GDC-0927 Racemate
SRN-927 Racemate |
Others | Others |
GDC-0927 Racemate is a degrader of estrogen receptor, is used in the research of ER-related diseases, potently inhibits ER-α activity, with an IC50 of 0.2 nM. | |||
T18651 | (rel)-PROTAC ERRα Degrader-1 | Others | Others |
(rel)-PROTAC ERRα Degrader-1 is a relative configuration of PROTAC ERRα Degrader-1, which is an estrogen-related receptor alpha (ERRa) degrader. PROTAC ERRα Degrader-1 consists of an MDM2 ligand binding moiety, a linker and an ERRa binding moiety [1]. | |||
T40349 |
DS45500853
|
||
DS45500853, an estrogen-related receptor α (ERRα) agonist, acts as an inhibitor of the binding interaction between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM), exhibiting an IC50 of 0.80 μM. This compound holds potential for research pertaining to metabolic disorders, particularly type 2 diabetes mellitus (T2DM). | |||
T39651 |
(S,R,S)-AHPC-C5-NH2
(S,R,S)-AHPC-C5-NH2,VH032-C5-NH2 |
||
(S,R,S)-AHPC-C5-NH2, also known as VH032-C5-NH2, is a synthetic compound designed as an E3 ligase ligand-linker conjugate. This compound combines the VH032-based von Hippel-Lindau (VHL) ligand with a linker, enabling it to function as a PROTAC degrader for estrogen-related receptor α (ERRα). | |||
T11231 | ERRγ Inverse Agonist 1 | Estrogen/progestogen Receptor | Endocrinology/Hormones |
ERRγ Inverse Agonist 1 (Compound 12) 是有效的、选择性的、口服生物可利用的雌激素相关受体 γ (ERRγ)的反向激动剂,IC50值为 40 nM。 | |||
T39838 |
(S,R,S)-AHPC-C7-amine
VH032-C7-amine,(S,R,S)-AHPC-C7-amine |
||
(S,R,S)-AHPC-C7-amine, also known as VH032-C7-amine, is a chemically synthesized conjugate that functions as an E3 ligase ligand-linker. This compound combines the VH032-based VHL ligand with a specific linker designed for the degradation of estrogen-related receptor α (ERRα) PROTAC. | |||
T60674 | DK1 | ||
DK1 是有效的雌激素相关受体调节剂。DK1 影响 ERRα 受体的活性,具有降低血糖的能力。DK1 显示出研究糖尿病的潜力。 | |||
T60441 | DK3 | ||
DK3 是雌激素相关受体 α(ERRα)的一种有效的选择性激动剂,ERRα是癌症和代谢性疾病的潜在药物靶点[1]。 | |||
T17941 |
ERRα Ligand-Linker Conjugates 1
|
Others | Others |
ERRα Ligand-Linker Conjugates 1 refers to a chemical compound that consists of a ligand targeting estrogen-related receptor alpha (ERRα), and a PROTAC linker that facilitates the recruitment of E3 ligases MDM2. It finds utility in the synthesis of a range of PROTACs, including one known as PROTAC ERRalpha Degrader-1. With its capability to induce degradation of ERRα, PROTAC ERRalpha Degrader-1 functions as an ERRα degrader[1]. | |||
T61923 |
ERRα antagonist-2
|
||
ERRα antagonist-2 (Compound 11) 是潜在的ERRα (雌激素受体相关受体 α)反向激动剂(IC50= 0.80 μM)。ERRα antagonist-2 对 ER 阴性 MDA-MB-231 细胞的迁移和侵袭具有抑制作用。ERRα antagonist-2 抑制体内乳腺癌的生长。 | |||
T63045 |
(1S,3R)-GNE-502
|
||
(1S,3R)-GNE-502 (compound 179) 是一种 Erα 的有效降解剂,能够在 MCF7 HCS 细胞中降解 ERα (EC50: 13 nM)。(1S,3R)-GNE-502 可以用于与雌激素受体相关癌症的研究。 | |||
T60759 |
DS20362725
|
||
DS20362725 是可用于代谢紊乱研究,如二型糖尿病的雌激素相关受体 α (ERRα) 激动剂。DS20362725 抑制受体相互作用蛋白 140 (RIP140) 辅助抑制肽 (10 nM) 和 GST-ERRα 配体结合结构域 (LBD; 1.2 μM) 之间的结合的 IC50值为 0.6 μM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T0760 |
Cholesterol
Cholesterin,Cholesteryl alcohol,胆固醇 |
Estrogen Receptor/ERR; MRP; Endogenous Metabolite; ROR | Endocrinology/Hormones; Immunology/Inflammation; Metabolism |
Cholesterol (Cholesteryl alcohol) 属于天然产物,是哺乳动物中的主要固醇,是一种雌激素相关受体 α (ERRα) 的激动剂。Cholesterol 广泛存在于动物的细胞膜,也是合成几种重要荷尔蒙及胆酸的材料。 | |||
TMA0424 |
Martynoside
|
ROS | Immunology/Inflammation |
Martynoside is a natural selective estrogen receptor modulator, which has antioxidative, anti-muscle fatigue, anticancer and antimetastatic activities. Martynoside has the potential of antagonizing sports anaemia, the mechanism of this effect might be rel |