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Search Results for " er-stress "

31

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6854	GSK621	Apoptosis; AMPK; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	GSK621 是一种特异性AMPK 激动剂，对 AML 细胞系的IC50值为13-30 μM。它可诱导自噬和凋亡，还可诱导eiF2α磷酸化。
T0159	Pranoprofen 普拉洛芬,Pyranoprofen	Apoptosis; COX; PGE Synthase; Prostaglandin Receptor	Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Pranoprofen (Pyranoprofen) 可抑制COX1/2酶，阻断花生四烯酸转化为二十烷醇，减少前列腺素的合成。它是一种用于眼科的非甾体抗炎试剂。
T1862	PR-619 PR 619,2,6-Diamino-3,5-dithiocyanopyridine	Apoptosis; DUB; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) 是一种 DUB 抑制剂，可诱导内质网应激和内质网应激相关的凋亡，对 USP4、USP8、USP7、USP2和 USP5的 EC50分别为 3.93、4.9、6.86、7.2 和 8.61 μM。
T13867	RH01386	Others	Others
	RH01386是可以预防 ER 应激诱导的β细胞功能障碍和死亡、抑制促凋亡基因表达的小分子。它恢复内质网应激受损的葡萄糖刺激的胰岛素分泌反应。对2型糖尿病具有潜在的研究价值。
T29017	TrxR1-IN-B19 TrxR1INB19,Go Y015,TrxR1 IN B19,Go-Y015	Others	Others
	TrxR1-IN-B19 (TrxR1 IN B19) 是一种 TrxR1 抑制剂，通过靶向 TrxR1 和 ROS 介导的 ER 应激激活，通过小分子选择性杀死胃癌细胞。
T20797	NE-100 hydrochloride NE100 Hydrochloride,NE 100 HCl,NE 100 Hydrochloride,NE-100 Hydrochloride,NE-100 HCl	Sigma receptor	GPCR/G Protein
	NE-100 hydrochloride (NE-100 HCl) 是选择性sigma-1 受体拮抗剂，IC50为 4.16 nM。它在体内具有抗精神病活性。它也能抑制内质网应激诱导的海马细胞死亡。
T8982	RH01687	Others	Others
	RH01687 是可以保护胰腺 β 细胞免受内质网应激诱导的细胞死亡的化合物。它对糖尿病具有潜在的研究价值。
T6993	Tauroursodeoxycholate sodium 牛磺熊脱氧胆酸钠,Sodium tauroursodeoxycholate,Tauroursodeoxycholic acid sodium salt,TUDC,牛磺熊去氧胆酸钠,Sodium Tauroursodeoxycholate (TUDC)	Apoptosis; ERK; Caspase	Apoptosis; MAPK; Proteases/Proteasome
	Tauroursodeoxycholate sodium (TUDC) 是一种内质网应激抑制剂。Tauroursodeoxycholate sodium (TUDC) 抑制ERK，显著降低凋亡分子表达，如caspase-3和caspase-12。
T13219	TTA-Q6	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	TTA-Q6 是一种选择性 T 型 Ca2+ 通道拮抗剂，具有潜在的抗肿瘤和免疫调节活性，可抑制肿瘤细胞摄取细胞外钙离子，诱导细胞内钙缺乏和内质网（ER）应激，用于治疗神经系统疾病。
T9110	Ceapin-A7	Others	Others
	Ceapin-A7 是内质网应激 ATF6α信号的选择性阻断剂(IC50:0.59 μM)，可用于探讨 ATF6α 促细胞活化的机制及其在病理环境中的作用。
T24855	TASIN-1 Hydrochloride 塔辛-1盐酸盐,TASIN-1 HCl,TASIN 1 HCl,TASIN1 HCl	APC	Cell Cycle/Checkpoint
	TASIN-1 Hydrochloride (TASIN-1 HCl) 是一种截短型 APC 的选择性抑制剂，通过降低细胞胆固醇水平和通过结肠癌细胞中的 ER 应激/ROS/JNK 信号传导诱导凋亡细胞死亡来选择性杀死表达截短型 APC 的结肠直肠癌细胞。
T8901	YUM70	Apoptosis; GPR; HSP	Apoptosis; Cytoskeletal Signaling; Endocrinology/Hormones; GPCR/G Protein; Metabolism
	YUM70 是一种选择性葡萄糖调节蛋白 78 抑制剂，抑制全长蛋白的 GRP78 ATPase 活性的IC50值为 1.5 μM。它在胰腺癌中诱导内质网应激介导的细胞凋亡。
T40130	Nur77 modulator 1 Nur77 modulator 1	Others	Others
	Nur77 modulator 1 可与Nur77结合，KD 为 3.58 μM。它上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡，Nur77 modulator 1显示出抗肝癌生物活性。
T9564	IRE1α kinase-IN-1	IRE1	Cell Cycle/Checkpoint
	IRE1α kinase-IN-1 是IRE1α 的选择性抑制剂(IC50为 77 nM)，对 IRE1α 的选择性高于 IRE1β 亚型 100 倍。它抑制内质网诱导的 IRE1α 寡聚和自磷酸化，并抑制 IRE1α RNase 活性 (IC50=80 nM)。
T12009	Telomerase-IN-1	Telomerase	DNA Damage/DNA Repair
	Telomease-IN-1是一种端粒酶抑制剂（IC50：0.19μM）。Telomease-IN-1通过ER 过度反应（EOR）的内质网应激（ERS）激活hTERT 的表达，然后诱导ERS，导致细胞凋亡。Telomease-IN-1通过表达下游信号分子包括CHOP（CAAT /增强子结合蛋白同源蛋白））和线粒体凋亡途径，导致细胞增殖受到抑制。Telomease-IN-1对端粒酶具有较高的抑制活性，对SMMC-7721细胞具有较高的抗增殖能力，对人正常肝细胞无明显毒性作用。Telomease-IN-1 在异种移植肿瘤模型表现出抗肿瘤活性。
T72543	BOLD-100 free base NKP-1339 free base ; IT-139 free base ; KP-1339 free base,KP-1339 free base,NKP-1339 free base,IT-139 free base
	BOLD-100 (NKP-1339; IT-139) free base 是一款钌基抗癌药物。作为GRP78应激诱导上调的抑制剂，它破坏内质网(ER)的稳态，从而诱发ER应激和未折叠蛋白反应(UPR)。此外，BOLD-100 free base 干预了内质网应激反应、溶酶体动力学以及细胞自噬(autophagy)间的复杂交互作用。
T27736	KM10103 KM-10103,KM 10103
	KM10103 exhibits β-cell-protective activities against ER stress, which plays an important role in the decline in pancreatic β cell function and mass observed in type 2 diabetes.
T36328	Termitomycamide B
	Endoplasmic reticulum (ER) stress, caused by accumulation of misfolded proteins and a disruption of calcium homeostasis, has been linked to several neuronal diseases including, Parkinson's, Alzheimer's, and prion diseases. A screen for protective activity against ER stress-dependent cell death identified termitomycamides, extracts from the fruiting bodies of T. titanicus, a notably large edible mushroom that is cultivated symbiotically in the nests of termites Termitomycamide B is a fatty acid i...
T26973	Cefatrizine Cephatriazine,BL-S-640,BLS640,S 640P,BL S 640
	Cefatrizine is an inhibitor of eukaryotic elongation factor-2 kinase, a unique calcium/calmodulin-dependent protein kinase, is well known to regulate apoptosis, autophagy and ER stress in many types of human cancers.
T71151	Z36
	Z36 is a novel Bcl-xL inhibitor, upregulating the expression levels of FAM134B, LC3, and Atg9, inducing autophagy along with autophagic cell death, resulting in ER stress and the unfolded protein response (UPR).
T73096	Z-LEVD-FMK
	Z-LEVD-FMK 是一种细胞渗透性的caspase-4抑制剂。 Z-LEVD-FMK 阻断 ER 应激诱导的癌细胞凋亡。
T75738	Microcystin-RR
	Microcystin-RR (Cyanoviridin RR)，一种有效的口服活性蛋白磷酸酶抑制剂，能诱导细胞凋亡和小鼠肝脏内质网应激。
T78528	ERX-41	Others	Others
	ERX-41是一种口服活性的立体特异性小分子，靶向溶酶体酸性脂肪酶A (LIPA)。该化合物通过诱导内质网(ER)应激从而导致细胞死亡，这一作用表明ERX-41功能独立于LIPA，但依赖于其在内质网的定位。ERX-41主要用于实体瘤靶向研究。
T79013	SLMP53-2
	SLMP53-2是一种可以重建p53转录活性的突变p53再激活因子。该化合物通过促进mutp53-Y220C与Hsp70之间的作用，恢复了mutp53-Y220C的野生型构象和其DNA结合能力。此外，SLMP53-2能够诱导细胞周期停滞、细胞凋亡以及ER应激，展现出了其抗肿瘤的潜力。
T79359	Anticancer agent 147	Ferroptosis	Apoptosis
	Anticanceragent 147（化合物6j），作为槐定碱的衍生物，功能为铁死亡（Ferroptosis）诱导剂。该化合物能促进Fe2+、活性氧（ROS）及丙二醛（MDA）在细胞内的积累，并通过增加内质网（ER）应激和上调转录因子ATF3的表达发挥作用。在体外及体内实验中，Anticanceragent 147展现了出色的抗肝癌活性。
T76254L	CD31 TFA
	CD31 TFA（PECAM-1），血小板内皮细胞粘附分子（platelet endothelial cell adhesion molecule-1），是产气荚膜梭菌b-Toxin (CPB)内皮细胞特异性受体，亦为ER-MP12抗原，链接机械应力、代谢与炎症。该肽通过维持CD31 TFA ITIM686与SHP2的磷酸化，抑制TCR诱导的T细胞活化。
T76254	CD31
	CD31 (PECAM-1)，一种血小板内皮细胞粘附分子（platelet endothelial cell adhesion molecule-1），兼作产气荚膜梭菌b-Toxin (CPB) 的特异性内皮细胞受体。同时，CD31为ER-MP12抗原，桥接机械应力、代谢与炎症。其肽通过维持CD31 ITIM686与SHP2的磷酸化，抑制TCR诱导的T细胞激活。
T78007	Vasonatrin Peptide (VNP) TFA
	Vasonatrin Peptide (VNP) TFA 是一种由心钠素 (ANP) 和C型利钠肽 (CNP) 嵌合而成的肽类化合物。它整合了CNP的静脉扩张功能、ANP的利尿效果，并展现出与ANP或CNP无关的特有动脉扩张特性。Vasonatrin Peptide TFA 透过cGMP-PKG信号途径发挥其对内质网应激介导的糖尿病心脏缺血再灌注损害的保护作用。
T36610	(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine
	(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine (CSTMP) is a stilbene derivative with antioxidant and anticancer activities. It stimulates proliferation of hydrogen peroxide-damaged ECV-304 cells (EC50 = 24.9 nM). CSTMP reduces hydrogen peroxide-induced release of lactate dehydrogenase (LDH) in and increases viability of human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner via inhibition of apoptosis. It reverses hydrogen peroxide-induced release of malondialdehyde ...
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...
T83857	Soluble Epoxide Hydrolase PROTAC 1a sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a
	Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术，通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解，特异性抑制sEH的水解酶活性(IC50 = 0.8 nM)，相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解，并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接，表明能减少ER应激。

化合物

Cat.No: T6854

Target: Apoptosis, AMPK, Autophagy

Cat.No: T0159

Synonym: 普拉洛芬,Pyranoprofen

Target: Apoptosis, COX, PGE Synthase, Prostaglandin Receptor

Cat.No: T1862

Synonym: PR 619,2,6-Diamino-3,5-dithiocyanopyridine

Target: Apoptosis, DUB, Autophagy

Cat.No: T13867

Target: Others

Cat.No: T29017

Synonym: TrxR1INB19,Go Y015,TrxR1 IN B19,Go-Y015

Target: Others

NE-100 hydrochloride

Cat.No: T20797

Synonym: NE100 Hydrochloride,NE 100 HCl,NE 100 Hydrochloride,NE-100 Hydrochloride,NE-100 HCl

Target: Sigma receptor

Cat.No: T8982

Target: Others

Tauroursodeoxycholate sodium

Cat.No: T6993

Synonym: 牛磺熊脱氧胆酸钠,Sodium tauroursodeoxycholate,Tauroursodeoxycholic acid sodium salt,TUDC,牛磺熊去氧胆酸钠,Sodium Tauroursodeoxycholate (TUDC)

Target: Apoptosis, ERK, Caspase

Cat.No: T13219

Target: Calcium Channel

Cat.No: T9110

Target: Others

TASIN-1 Hydrochloride

Cat.No: T24855

Synonym: 塔辛-1盐酸盐,TASIN-1 HCl,TASIN 1 HCl,TASIN1 HCl

Target: APC

Cat.No: T8901

Target: Apoptosis, GPR, HSP

Nur77 modulator 1

Cat.No: T40130

Synonym: Nur77 modulator 1

Target: Others

IRE1α kinase-IN-1

Cat.No: T9564

Target: IRE1

Telomerase-IN-1

Cat.No: T12009

Target: Telomerase

BOLD-100 free base

Cat.No: T72543

Synonym: NKP-1339 free base ; IT-139 free base ; KP-1339 free base,KP-1339 free base,NKP-1339 free base,IT-139 free base

Cat.No: T27736

Synonym: KM-10103,KM 10103

Termitomycamide B

Cat.No: T36328

Cat.No: T26973

Synonym: Cephatriazine,BL-S-640,BLS640,S 640P,BL S 640

Cat.No: T71151

Cat.No: T73096

Cat.No: T75738

Cat.No: T78528

Target: Others

Cat.No: T79013

Anticancer agent 147

Cat.No: T79359

Target: Ferroptosis

Cat.No: T76254L

Cat.No: T76254

Vasonatrin Peptide (VNP) TFA

Cat.No: T78007

(E)-2-(2-Chlorostyryl)-3,5,6-trimethylpyrazine

Cat.No: T36610

Cat.No: T36570

Soluble Epoxide Hydrolase PROTAC 1a

Cat.No: T83857

Synonym: sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a

Cat. No.	Product Name	Target	Signaling Pathways
T3324	Lycorine Galanthidine,Narcissine,石蒜碱,Amarylline,Belamarine,Licorine,番石榴碱	Apoptosis; Virus Protease; Antibacterial; AChR; Fatty Acid Synthase	Apoptosis; Metabolism; Microbiology/Virology; Neuroscience
	Lycorine (Narcissine) 是从金眼科植物科中提取的一种天然生物碱。它是一种具有口服活性的SCAP 抑制剂，Kd 值 15.24 nM。它也是黑色素瘤血管生成抑制剂，有用于前列腺癌和代谢疾病的研究潜力。
T2930	α-Lipoic Acid Lipoic acid,Alphalipoic acid,硫辛酸	NF-κB; HIV Protease; Mitochondrial Metabolism; Endogenous Metabolite	Metabolism; Microbiology/Virology; NF-κB; Proteases/Proteasome
	α-Lipoic Acid (Alphalipoic acid) 抑制 NF-κB 依赖性 HIV-1 LTR 活化。 α-硫辛酸诱导内质网 (ER) 应激介导的肝癌细胞凋亡。α-硫辛酸是一种抗氧化剂，是线粒体酶复合物的重要辅助因子。
T5S1285	(+)-(3R,8S)-Falcarindiol Falcarindiol,镰叶芹二醇	Others	Others
	(+)-(3R,8S)-Falcarindiol 是一种从胡萝卜中得到的聚乙炔，有抗炎、抗肿瘤和抗脂质过氧化活性。它具有抗分歧杆菌作用，对Mycobacterium tuberculosisH37Ra 的 MIC 和 IC50值分别为 24 μM 和 6 μM。
T3395	Timosaponin AIII Filiferin B,知母皂苷 A-III,AneMarsaponin A3,Timosaponin A3	AChE; mTOR	Neuroscience; PI3K/Akt/mTOR signaling
	Timosaponin AIII (Timosaponin A3) 是一种乙酰胆碱酯酶活性抑制剂，其IC50=35.4 μM。
T13430	ABTL-0812 α-羟基油酸,α-Hydroxylinoleic acid	Others	Others
	ABTL-0812 induces endoplasmic reticulum (ER) stress-mediated autophagy, and with anti-cancer activity.
TN6613	Delphinidin-3-O-galactoside chloride
	Delphinidin-3-O-galactoside chloride has anti-obesity and hypolipidemic effects. Delphinidin-3-O-galactoside (D3G) is a water-soluble anthocyanin with antioxidant activity. D3G is capable of masking the EGCG-induced cytotoxicity and ER stress, presumably
T75622	β-Apopicropodophyllin
	β-Apopicropodophyllin 是一种天然产物，可以从Hyptis wticillata 中分离得到。β-Apopicropodophyllin 通过诱导微管破坏、DNA 损伤、细胞周期停滞和 ER 应激来诱导细胞凋亡。β-Apopicropodophyllin 可用于癌症研究。
T21577	Narasin (sodium salt) Naracin sodium salt,naransin sodium,海南霉素,HainanMycin	NF-κB	NF-κB
	Narasin (sodium salt) (HainanMycin) 通过神经胶质瘤细胞中的 ER 应激诱导肿瘤坏死因子相关凋亡诱导配体 (TRAIL) 介导的细胞凋亡，并通过抑制 IκBα 的磷酸化来抑制 NF-κB 信号传导。
TN3719	Cristacarpin	p38 MAPK; ROS; CDK; Antifection; p53	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation; MAPK; Microbiology/Virology
	Cristacarpin exhibits moderate but selective activity towards DNA repair-deficient yeast mutants. It promotes endoplasmic reticulum (ER) stress, leading to sub-lethal reactive oxygen species (ROS) generation and which eventually terminates by triggering s
T75637	Demethylcantharidate disodium
	Demethylcantharidate disodium 是一种内源性代谢产物，能通过诱导内质网应激来促进肝癌细胞的凋亡，并且对多种类型的癌症展现出良好的抗癌活性。
TN6458	Acetylshikonin
	Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.
T72429	α-Lipoic Acid sodium Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium
	α-Lipoic Acid (Thioctic acid) sodium 是一种抗氧化剂，是线粒体酶复合物的重要辅助因子。α-Lipoic Acid sodium 可抑制NF-κB 依赖性的HIV-1LTR 活化。α-Lipoic Acid sodium 诱导内质网应激 (ERS) 介导的肝癌细胞凋亡 (apoptosis)。α-Lipoic Acid sodium 可与CPUL1 合成自组装的纳米聚合体 CPUL1-LA NA，其抗肿瘤效果优于 CPUL1。

天然产物

Cat.No: T3324

Synonym: Galanthidine,Narcissine,石蒜碱,Amarylline,Belamarine,Licorine,番石榴碱

Target: Apoptosis, Virus Protease, Antibacterial, AChR, Fatty Acid Synthase

Cat.No: T2930

Synonym: Lipoic acid,Alphalipoic acid,硫辛酸

Target: NF-κB, HIV Protease, Mitochondrial Metabolism, Endogenous Metabolite

(+)-(3R,8S)-Falcarindiol

Cat.No: T5S1285

Synonym: Falcarindiol,镰叶芹二醇

Target: Others

Timosaponin AIII

Cat.No: T3395

Synonym: Filiferin B,知母皂苷 A-III,AneMarsaponin A3,Timosaponin A3

Target: AChE, mTOR

Cat.No: T13430

Synonym: α-羟基油酸,α-Hydroxylinoleic acid

Target: Others

Delphinidin-3-O-galactoside chloride

Cat.No: TN6613

β-Apopicropodophyllin

Cat.No: T75622

Narasin (sodium salt)

Cat.No: T21577

Synonym: Naracin sodium salt,naransin sodium,海南霉素,HainanMycin

Target: NF-κB

Cat.No: TN3719

Target: p38 MAPK, ROS, CDK, Antifection, p53

Demethylcantharidate disodium

Cat.No: T75637

Cat.No: TN6458

α-Lipoic Acid sodium

Cat.No: T72429

Synonym: Thioctic acid sodium,DL-α-Lipoic acid sodium,Thioctic acid sodium ; (±)-α-Lipoic acid sodium ; DL-α-Lipoic acid sodium,(±)-α-Lipoic acid sodium

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