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24

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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)。
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。
T39837	PROTAC ERRα Degrader-3
	PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins.
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].
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].
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。
T74559	PROTAC_ERRα
	PROTAC_ERRα 是一种有效的选择性 ERRα降解剂。PROTAC_ERRα 诱导蛋白酶体降解，并且能够特异性降解 ERRα蛋白 >80%。
T74840	ERRγ agonist-2
	ERRγagonist-2 是一种有效的选择性 ERRγ反向激动剂，Kd 值为 6.5 μM。ERRγagonist-2 抑制铁调素、纤维蛋白原和糖异生基因的表达。ERRγagonist-2 具有抗菌、抗凝血和抗糖尿病活性。
T60772	ERRγ agonist-1
	ERRγ agonist-1 可用于研究神经心理障碍。ERRγ agonist-1 增加ERRγ的转录活性，是 ERRγ的有效激动剂。
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。
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。
T77552	SLU-PP-1072	Apoptosis; Estrogen/progestogen Receptor	Apoptosis; Endocrinology/Hormones
	SLU-PP-1072 是一种 ERRα和ERRγ 反向双重激动剂，破坏 PCa 细胞代谢，通过细胞周期失调诱导凋亡 (apoptosis)。SLU-PP-1072 用于研究前列腺癌 (PCa) 。
T2250	DY131 DY 131,GSK 9089,DY-131	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Smo	Endocrinology/Hormones; Stem Cells
	DY131 (DY-131) 是选择性的 ERRγ 和 ERRβ 激动剂，对 ERRα，ERα 和 ERβ 无效。它对Smo 的信号传导具有抑制作用。
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。
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]。
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。
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).
T73152	SLU-PP-915
	SLU-PP-915 是一种ERR 激动剂。SLU-PP-915 对 ERRα、ERRβ 和ERRγ的EC50值约为 400 nM。SLU-PP-915 在维持氧化代谢、心力衰竭中有潜在的应用。
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。
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.
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).
T12329	Ospemifene D4 FC-1271a D4	Estrogen/progestogen Receptor	Endocrinology/Hormones
	Ospemifene D4 is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active modulator of estrogen receptor.

化合物

PROTAC ERRα ligand 2

Cat.No: T5835

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

PROTAC ERRα ligand 1

Cat.No: T15191

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor

ERRα antagonist-1

Cat.No: T11230

Synonym: ERR+/- antagonist-1,ERRa antagonist-1

Target: Estrogen/progestogen Receptor

PROTAC ERRα Degrader-3

Cat.No: T39837

PROTAC ERRα Degrader-2

Cat.No: T18609

Target: Others

(rel)-PROTAC ERRα Degrader-1

Cat.No: T18651

Target: Others

ERRα Ligand-Linker Conjugates 1

Cat.No: T17941

Target: Others

ERRα antagonist-2

Cat.No: T61923

Cat.No: T74559

ERRγ agonist-2

Cat.No: T74840

ERRγ agonist-1

Cat.No: T60772

Cat.No: T0593

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Autophagy

Cat.No: T77577

Target: Estrogen/progestogen Receptor

Cat.No: T77552

Target: Apoptosis, Estrogen/progestogen Receptor

Cat.No: T2250

Synonym: DY 131,GSK 9089,DY-131

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Smo

Cat.No: T8370

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Reactive Oxygen Species

Cat.No: T60441

Cat.No: T60674

Cat.No: T40349

Cat.No: T73152

Cat.No: T60759

(S,R,S)-AHPC-C7-amine

Cat.No: T39838

Synonym: VH032-C7-amine,(S,R,S)-AHPC-C7-amine

(S,R,S)-AHPC-C5-NH2

Cat.No: T39651

Synonym: (S,R,S)-AHPC-C5-NH2,VH032-C5-NH2

Cat.No: T12329

Synonym: FC-1271a D4

Target: Estrogen/progestogen Receptor

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。
T2177	Kaempferol Kempferol,山柰酚,山奈酚,Robigenin	Apoptosis; Estrogen Receptor/ERR; Mitophagy; Estrogen/progestogen Receptor; HIV Protease; Endogenous Metabolite; Parasite; Autophagy	Apoptosis; Autophagy; Endocrinology/Hormones; Metabolism; Microbiology/Virology; Proteases/Proteasome
	Kaempferol (Robigenin) 属于天然类黄酮，是一种 ERRα 和 ERRγ 的反向激动剂。Kaempferol 具有抗肿瘤、抗炎、抗氧化、抗菌和抗病毒等多种活性。

天然产物

Cat.No: T0760

Synonym: Cholesterin,Cholesteryl alcohol,胆固醇

Target: Estrogen Receptor/ERR, MRP, Endogenous Metabolite, ROR

Cat.No: T2177

Synonym: Kempferol,山柰酚,山奈酚,Robigenin

Target: Apoptosis, Estrogen Receptor/ERR, Mitophagy, Estrogen/progestogen Receptor, HIV Protease, Endogenous Metabolite, Parasite, Autophagy

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