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26

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8329	AR 231453	GPR	Endocrinology/Hormones; GPCR/G Protein
	AR 231453 是一种口服具有活性的、特异性的 GPR119激动剂。它能够刺激细胞增殖，改善胰岛 β 细胞的功能。
T10359	AR antagonist 1	Androgen Receptor; Ligand for E3 Ligase; Ligands for Target Protein for PROTAC	Endocrinology/Hormones; PROTAC
	AR antagonist 1 是 AR 拮抗剂，能够与 E3 连接酶配体结合，与 VHL 蛋白结合亲和力较弱，用于 PROTACARD-266 合成。
T6400	AZD3514	Androgen Receptor	Endocrinology/Hormones
	AZD3514 是一种口服雄激素受体下调剂(Ki :2.2 μM)，能够减少 AR 蛋白表达。
T75129	Luxdegalutamide ARV-766	Androgen Receptor; PROTACs	Endocrinology/Hormones; PROTAC
	Luxdegalutamide (ARV-766) 是一种可口服且有效的蛋白水解靶向嵌合体 (PROTAC) 的蛋白质降解剂。Luxdegalutamide降解野生型雄激素受体 AR，也降解包括最普遍的致病性 AR L702H、H875Y 和 T878A 突变相关的 AR LBD 突变体。
T10358	Netarsudil Dihydrochloride AR-13324 Dihydrochloride	ROCK	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) 是 Rho 相关蛋白激酶 (ROCK) 和去甲肾上腺素转运蛋白 (NET) 的抑制剂，可有效降低眼压 (IOP)。
T39695	ARD-2128	Androgen Receptor	Endocrinology/Hormones
	ARD-2128 是高效的雄激素受体降解剂 PROTAC。它可有效降低雄激素受体蛋白并抑制肿瘤组织中雄激素受体调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。它有用于前列腺癌研究的价值。
T39954	AU-15330	Epigenetic Reader Domain; PROTACs	Chromatin/Epigenetic; PROTAC
	AU-15330是SWI/SNF ATPase亚基SMARCA2和SMARCA4的蛋白水解靶向嵌合体（PROTAC）降解剂。AU-15330 能有效抑制肿瘤在前列腺癌异种移植模型中的生长，并与 AR 拮抗剂恩杂鲁胺具有协同作用。AU-15330在去势抵抗性前列腺癌（CRPC）模型中显示出部分治疗效果和AU-15330具有无毒性的特点。
T27601	IMTPPE SID-3712502,SID 3712502,SID3712502
	IMTPPE inhibits transcriptional activity and protein level of AR in C4-2 prostate cancer cells. It also inhibits AR-target gene expression.
T30123	ARD-69
	ARD-69 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent mann
T71120	AR-13503
	AR-13503, is an metabolite of Netarsudil (AR-11324), is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure.
T18596	PROTAC AR Degrader-4	Others	Others
	PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
T10320	Androgen receptor antagonist 1	Others	Others
	Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
T13552	ARD-266	Others	Others
	ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces the degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines (DC50s: 0.2-1 nM).
T39399	ABM-14
	ABM-14, a ligand for the androgen receptor (AR), is utilized as a targeting agent in PROTAC. By binding to a ligand for the von Hippel-Lindau protein (VHL) via a linker, ABM-14 forms ARCC-4, which facilitates the degradation of AR.
T78811	PROTAC AR-NTD degrader 1	Androgen Receptor	Endocrinology/Hormones
	PROTACAR-NTD antagonist 1 (compound 18) 是一款针对雄激素受体AR-V7变体的PROTACs，它特异性地拮抗AR的N末端结构域 (AR-NTD)，能有效诱导前列腺癌细胞凋亡，并在VCaP细胞中以1 μM 和 5 μM的浓度分别实现了62.2%和71.1%的AR-V7蛋白降解率。
T73726	PROTAC AR Degrader-4 TFA
	PROTACAR Degrader-4 包含IAP 配体结合基团，linker 和雄激素受体 (AR) 配体结合基团。基于cIAP1的降解剂也被称为SNIPER。
T81662	N-Nitrosodicyclohexylamine NDCHA	Androgen Receptor	Endocrinology/Hormones
	N-Nitrosodicyclohexylamine (NDCHA) 是一种N-亚硝基化合物，具有抗雄激素活性。它通过与雄激素受体 (AR) 竞争性结合来抑制 5α-二氢睾酮的作用，并能降低 AR 蛋白水平。
T79156	(R)-SKBG-1	Androgen Receptor	Endocrinology/Hormones
	(R)-SKBG-1为RNA结合蛋白NONO的抑制剂，能够抑制雄激素受体表达，并对AR-FL mRNA及AR-V7 mRNA具有IC50。
T13958	VHL Ligand 8	Others	Others
	VHL Ligand 8 是一种 von Hippel-Lindau (VHL) 蛋白配体，可用于合成 ARD-266 。ARD-266 是一种基于 VHL E3 连接酶的高效雄激素受体 (AR) PROTAC 降解剂。ARD-266 在 AR 阳性 LNCaP，VCaP 和 22Rv1 前列腺癌细胞系中有效诱导 AR 蛋白降解，DC50值为 0.2-1 nM。
T74745	A031
	A031 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂，对 AR 蛋白具有降解作用，IC50值小于 0.25 μM。A031 抑制移植人前列腺癌 (VCaP) 的斑马鱼的肿瘤生长。
T78922	ARD-2051	PROTACs	PROTAC
	ARD-2051是一种具有口服活性的高效雄激素受体(AR)蛋白水解靶向嵌合体降解剂。在LNCaP和VCaP前列腺癌细胞系中，ARD-2051实现AR蛋白降解的DC50值仅为0.6 nM，适用于前列腺癌研究。
T78810	BWA-522	Androgen Receptor	Endocrinology/Hormones
	BWA-522是一种口服有效的小分子PROTACs，针对AR-FL和AR-V7显示出显著的降解活性。该化合物通过对Androgen Receptor的AR-NTD进行拮抗，诱发PC细胞的apoptosis。在LNCaP异种移植模型中，BWA-522以每日60 mg/kg的剂量口服给药，实现了76%的肿瘤生长抑制(TGI=76%)。在VCaP和LNCaP细胞系中对AR-V7和AR-FL的降解效率分别达到77.3%(1 μM)和72.0%(5 μM)。
T17689	Boc-Pip-alkyne-Ph-COOH	Others	Others
	Boc-Pip-alkyne-Ph-COOH, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in synthesizing PROTACs including ARD-266. This compound demonstrates significant efficacy in promoting the degradation of androgen receptor (AR) protein across AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, showcasing DC50 values ranging from 0.2-1 nM[1].
T37669	CAY10498
	The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold ...
T71119	Netarsudil free base
	Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudi...
T40869	Moxonidine hydrochloride BDF5895hydrochloride,盐酸莫索尼定
	Moxonidine Hydrochloride is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent. Target: I1-R Moxonidine Hydrochloride is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response...

化合物

Cat.No: T8329

Target: GPR

AR antagonist 1

Cat.No: T10359

Target: Androgen Receptor, Ligand for E3 Ligase, Ligands for Target Protein for PROTAC

Cat.No: T6400

Target: Androgen Receptor

Luxdegalutamide

Cat.No: T75129

Synonym: ARV-766

Target: Androgen Receptor, PROTACs

Netarsudil Dihydrochloride

Cat.No: T10358

Synonym: AR-13324 Dihydrochloride

Target: ROCK

Cat.No: T39695

Target: Androgen Receptor

Cat.No: T39954

Target: Epigenetic Reader Domain, PROTACs

Cat.No: T27601

Synonym: SID-3712502,SID 3712502,SID3712502

Cat.No: T30123

Cat.No: T71120

PROTAC AR Degrader-4

Cat.No: T18596

Target: Others

Androgen receptor antagonist 1

Cat.No: T10320

Target: Others

Cat.No: T13552

Target: Others

Cat.No: T39399

PROTAC AR-NTD degrader 1

Cat.No: T78811

Target: Androgen Receptor

PROTAC AR Degrader-4 TFA

Cat.No: T73726

N-Nitrosodicyclohexylamine

Cat.No: T81662

Synonym: NDCHA

Target: Androgen Receptor

Cat.No: T79156

Target: Androgen Receptor

Cat.No: T13958

Target: Others

Cat.No: T74745

Cat.No: T78922

Target: PROTACs

Cat.No: T78810

Target: Androgen Receptor

Boc-Pip-alkyne-Ph-COOH

Cat.No: T17689

Target: Others

Cat.No: T37669

Netarsudil free base

Cat.No: T71119

Moxonidine hydrochloride

Cat.No: T40869

Synonym: BDF5895hydrochloride,盐酸莫索尼定

Cat. No.	Product Name	Target	Signaling Pathways
T3232	Higenamine hydrochloride Higenamine HCl,Demethylcoclaurine hydrochloride,盐酸去甲乌头碱,norcoclaurine HCl,(+-)-Demethylcoclaurine hydrochloride,Higenamine Hydrochloride	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Higenamine hydrochloride (norcoclaurine HCl) 是一种 β2-AR 激动剂，是用于心力衰竭相关研究的中药乌头的关键成分，具有抗凋亡活性。
T5244	Aminomalonic acid 2-Aminopropanedioic Acid,氨基丙二酸,Aminomalonate	Others; Endogenous Metabolite	Metabolism; Others
	Aminomalonic acid (Aminomalonate) 是氨基内源性代谢产物，在体外能作为来源 Leukemia 5178Y/AR 和小鼠胰腺的 L- 天冬酰胺合成酶的高效抑制剂 (Leukemia 5178Y/AR:Ki= 0.0023 M，小鼠胰腺:Ki= 0.0015 M)。它有潜力用作区分黑素瘤转移的不同阶段生物标志物。
T14317	ar-Turmerone (+)-ar-Turmerone	Others	Others
	ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.

天然产物

Higenamine hydrochloride

Cat.No: T3232

Synonym: Higenamine HCl,Demethylcoclaurine hydrochloride,盐酸去甲乌头碱,norcoclaurine HCl,(+-)-Demethylcoclaurine hydrochloride,Higenamine Hydrochloride

Target: Adrenergic Receptor

Aminomalonic acid

Cat.No: T5244

Synonym: 2-Aminopropanedioic Acid,氨基丙二酸,Aminomalonate

Target: Others, Endogenous Metabolite

Cat.No: T14317

Synonym: (+)-ar-Turmerone

Target: Others

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