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Search Results for " proteasomal "

33

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6275	Obatoclax Mesylate Obatoclax,GX15-070,奥巴克拉甲磺酸盐	BCL; Parasite; Autophagy	Apoptosis; Autophagy; Microbiology/Virology
	Obatoclax Mesylate (GX15-070) 是泛 BCL-2家族蛋白抑制剂，对 BCL-2 的 Ki 值为 220 nM。它是 BH3 模拟物，具有抗癌和广谱抗寄生虫活性。它诱导自噬依赖性细胞死亡，并靶向细胞周期蛋白 D1 进行蛋白酶体降解。
T1602	Valproic acid sodium salt 丙戊酸钠,Sodium Valproate	Mitophagy; Gamma-secretase; HIV Protease; GABA Receptor; HDAC; Autophagy	Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells
	Valproic acid sodium salt (Sodium Valproate) 是一种HDAC 抑制剂，可抑制HDAC1的活性，诱导HDAC2的降解。它激活Notch1信号并抑制小细胞肺癌细胞的增殖。它可研究癫痫、偏头痛和双相情感障碍等。
T6474	Divalproex Sodium Valproate semisodium,Epival,双丙戊酸钠	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Divalproex Sodium (Valproate semisodium) 结合并抑制 γ-氨基丁酸 (GABA) 转氨酶，其抗惊厥活性可通过增加 GABA 脑浓度和抑制分解 GABA 或阻止 GABA 再摄取到神经胶质和神经末梢的酶来发挥。它也是一种 HDAC 抑制剂。由丙戊酸钠和丙戊酸组成，具有抗惊厥和抗癫痫活性。 Divalproex 还可以通过抑制电压敏感的钠通道来抑制重复的神经元放电。
T60202	MMRi62 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol	Ferroptosis	Apoptosis
	MMRi62 (7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol) 是一种铁死亡 (ferroptosis) 诱导剂，靶向 MDM2-MDM4 (抑癌基因 p53 负调控因子)。MMRi62 对胰腺导管腺癌 (PDAC) 细胞显示出 p53 独立的促凋亡 (apoptosis) 活性，并诱导其自噬 (autophagy)。MMRi62 诱导铁死亡，伴随着活性氧增加和铁蛋白重链 (FTH1) 溶酶体降解。MMRi62 还可导致突变型 p53 的蛋白酶体降解，并对具有 KRAS 和 TP53 高频突变特征的原位异种移植 PDAC 小鼠模型具有体内药效。
T70082	Pyrithione cadmium
	Pyrithione cadmium suppresses tumor growth in vitro and in vivo through inhibition of proteasomal deubiquitinase
T30562	BP
	BP is a rare class enhancer of proteasomal activation in the absence of a heat shock response.
T30795	CEP-1612 CEP 1612,UNII-9K6U075027
	CEP-1612 is a proteasomal inhibitor responsible for the proteolysis of proteins that regulate important cell cycles and apoptosis. CEP-1612 can induce p21WAF1 and p27KIP1 expression and apoptosis, and inhibit tumor growth of human lung cancer.
T71393	(S)-FTY-720 Vinylphosphonate
	(S)-FTY-720 Vinylphosphonate inhibits sphingosine kinase 1 and promotes its proteasomal degradation in human pulmonary artery smooth muscle, breast cancer cells, and androgen-independent prostate cancer cells.
T16568	PR-924	Proteasome	Proteases/Proteasome; Ubiquitination
	PR-924 is a selective inhibitor of tripeptide epoxyketone immunoproteasome subunit LMP-7 (IC50: 22 nM). PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 covalently modifies proteasomal N-terminal threonine active sites.
T70704	RB-005
	RB-005 is a potent sphingosine kinase isoform 1 (SK1) inhibitor, which may serve as therapeutic agent for proliferative diseases, including hypertension. RB-005, (IC(50) = 3.6 μM), which also induced proteasomal degradation of SK1 in human pulmonary arterial smooth muscle cells.
T80211	Ac-KQL-AMC
	Ac-KQL-AMC是量化蛋白酶体样活性的荧光底物，其被裂解时释放可检测的荧光信号。
T10875	CP5V	Others	Others
	CP5V, a PROTAC, induces mitotic inhibition, and suppresses cancer cell proliferation. It specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation.
T11975	PROTAC Mcl1 degrader-1	BCL	Apoptosis
	PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
T60030	NCT02
	NCT02 是一种细胞周期蛋白 K 降解剂，可诱导细胞周期蛋白 K (CCNK) 的泛素化和 CCNK 及其复合物 CDK12 的蛋白酶体降解。NCT02具有研究转移性结直肠癌 (CRC) 的潜力。
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%。
T81696	NBI-961
	NBI-961为高效NEK2抑制剂，能阻断蛋白酶体降解作用。该化合物在弥漫性大B细胞淋巴瘤(DLBCL)细胞中诱导G2/有丝分裂停滞及细胞凋亡(apoptosis)。
T35670	Miro1 Reducer
	Promotes proteasomal degradation of Miro1 (mitochondrial Rho GTPase 1). Reduces Miro1 levels in fibroblasts from Parkinson's disease (PD) patients (IC50 = 7.8 μM). Exhibits no significant effect on related outer mitochondrial membrane protein Mitofusin. Reduces stress-induced degeneration of dopaminergic neurons derived from PD patient iPSCs. Rescues age-dependent neuronal loss and prolongs lifespan in fly PD models.
T13743	JH-XI-10-02	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrader of CDK8, with an IC50 of 159 nM, based on PROTAC.
T81372	Proteasome-activating peptide 1
	Proteasome-activating peptide 1 是一种肽，其作用是提升胰凝乳蛋白酶样蛋白酶体（proteasome）的催化活性，有效增强体外及细胞培养环境下的蛋白质降解效率。此外，该肽能阻止肌萎缩侧索硬化症（Amyotrophic Lateral Sclerosis, ALS）细胞模型中蛋白质的过度聚集。
T68760	Luminespib mesylate
	Luminespib, also known as AUY-922, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines.
T68383	BIIB028
	BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to o...
T82610	DA-PROTAC	PROTACs	PROTAC
	DA-PROTAC是Atox1和CCS铜离子转运蛋白的有效PROTAC降解剂。该化合物能够与Atox1和CCS结合形成复合体，进而与E3连接酶相结合，引起Atox1和CCS的泛素化水平增加，最终通过蛋白酶体途径导致这两种蛋白的降解。DA-PROTAC在三阴性乳腺癌的研究中有应用潜力。
T74992	NU223612
	NU223612 是一种有效的PROTAC(PROTACs)，可降解吲哚胺 2,3-双加氧酶 1 (IDO1) (Indoleamine 2,3-Dioxygenase (IDO))，Kd 为 640 nM。NU223612 通过CRBN 介导的蛋白酶体降解有效降解IDO1蛋白。NU223612 以 290 nM 的亲和力与 CRBN 结合。NU223612 可以穿过血脑屏障 (BBB)。
T76243	Proteasome-activating peptide 1 TFA
	Proteasome-activating peptide 1 TFA 是一种肽类蛋白酶体激活剂，能显著增强胰凝乳蛋白酶样蛋白酶体的催化活性，进而提升体外及培养环境中的蛋白质水解效率。此外，Proteasome-activating peptide 1 TFA 还能有效阻止肌萎缩侧索硬化症细胞模型内的蛋白质聚集现象。
T74557	α1A-AR Degrader 9c	PROTACs	PROTAC
	α1A-AR Degrader 9c（化合物 9c）是一种高效、选择性且可逆的α1A-AR PROTAC降解剂，DC50值为2.86 μM。它通过蛋白酶体途径诱导α1A-AR的降解，并且在抑制PC-3细胞增殖方面表现出活性，IC50为6.12 μM。此外，α1A-AR Degrader 9c展现出在前列腺癌研究中的抗肿瘤潜力。
T35773	Gliotoxin-13C13 Gliotoxin-13C13
	Gliotoxin-13C13is intended for use as an internal standard for the quantification of gliotoxin by GC- or LC-MS. Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains ofAspergillusand other fungi with diverse biological activities.1,2,3,4,5,6,7,8It inhibits 20S proteasomal chymotrypsin activity (IC50= 10 μM), blocking the degradation of IκBα and preventing the activation of NF-κB.2,3Gliotoxin induces apoptosis in monocytes and dendritic cells and reduces phagocytosis by neutr...
T80686	γ-AA peptide P6
	γ-AA peptide P6 作为E6相关蛋白(E6AP)的有效激活剂, 在体外重组反应中能够促进E6AP的自我泛素化以及催化底物的泛素化作用。此外，γ-AA peptide P6 在细胞内部能够增强E6AP底物的泛素化，并加速其通过蛋白酶体的降解过程。
T80523	Azurin p28 peptide
	Azurin p28 peptide是一种具有肿瘤穿透能力和抗肿瘤活性的肽。它通过与p53结合形成p28:p53复合物，从而降低p53在蛋白酶体中的降解，进而诱导细胞凋亡(apoptosis)或使细胞周期停滞。此外，Azurin p28 peptide通过抑制VEGFR-2、FAK和Akt的磷酸化表现出抗血管生成效果，抑制p53阳性肿瘤的生长。
T68275	MV151
	MV151 is a fluorescent broad-spectrum proteasome inhibitor for labeling proteasomes in vitro and in vivo. MV151 specifically targets all active subunits of the proteasome and immunoproteasome in living cells, allowing for rapid and sensitive in-gel detection. The inhibition profile of a panel of commonly used proteasome inhibitors could be readily determined by MV151 labeling. Administration of MV151 to mice allowed for in vivo labeling of proteasomes, which correlated with inhibition of proteas...
T69288	CEP-7055
	CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 represses the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha (IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation of a variety of cel...
T83726	Tat-βsyn-degron TFA
	Tat-βsyn-degron是一种降低α-synuclein表达的肽。其结构包括HIV-1 Tat质膜跨导域、与β-synuclein氨基酸36-45相对应的α-synuclein结合域βsyn，以及蛋白酶体定向域degron。在肽-蛋白结合实验中，Tat-βsyn-degron能够与重组α-synuclein结合，并在大鼠初级皮质神经元培养中降低α-synuclein水平，这一效应可以通过蛋白酶体抑制剂MG132阻止。体内研究显示，Tat-βsyn-degron (40 mg/kg)能够在过表达人类A53T突变体α-synuclein的M38转基因小鼠的大脑中降低α-synuclein水平，并且在黑质和脑桥中降低磷酸化α-synuclein水平，以及在通过α-synuclein预成纤维诱导的扩散性α-synuclein病理模型小鼠中减少神经炎症。此外，Tat-βsyn-degron (6 µmol/kg, i.p.)在MPTP诱导的帕金森病小鼠模型中，保护多巴胺能神经元，缓解运动缺陷。
T75133	NRX-0492
	NRX-0492 是一种口服有效的 BTK 降解剂。NRX-0492 催化 BTK 泛素化和蛋白酶体降解 (DC50≤0.2 nM，DC90≤0.5 nM)。NRX-0492 抑制 B 细胞受体 (BCR) 介导的信号、转录程序和趋化因子分泌。NRX-0492 能够把非共价 BTK 结合域连接到 Cereblon。Cereblon 是 E3泛素连接酶复合物的一种衔接蛋白。
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

Obatoclax Mesylate

Cat.No: T6275

Synonym: Obatoclax,GX15-070,奥巴克拉甲磺酸盐

Target: BCL, Parasite, Autophagy

Valproic acid sodium salt

Cat.No: T1602

Synonym: 丙戊酸钠,Sodium Valproate

Target: Mitophagy, Gamma-secretase, HIV Protease, GABA Receptor, HDAC, Autophagy

Divalproex Sodium

Cat.No: T6474

Synonym: Valproate semisodium,Epival,双丙戊酸钠

Target: HDAC

Cat.No: T60202

Synonym: 7-[(2,3-dichlorophenyl)-(pyridin-2-ylamino)methyl]quinolin-8-ol

Target: Ferroptosis

Pyrithione cadmium

Cat.No: T70082

Cat.No: T30562

Cat.No: T30795

Synonym: CEP 1612,UNII-9K6U075027

(S)-FTY-720 Vinylphosphonate

Cat.No: T71393

Cat.No: T16568

Target: Proteasome

Cat.No: T70704

Cat.No: T80211

Cat.No: T10875

Target: Others

PROTAC Mcl1 degrader-1

Cat.No: T11975

Target: BCL

Cat.No: T60030

Cat.No: T74559

Cat.No: T81696

Cat.No: T35670

Cat.No: T13743

Target: EGFR

Proteasome-activating peptide 1

Cat.No: T81372

Luminespib mesylate

Cat.No: T68760

Cat.No: T68383

Cat.No: T82610

Target: PROTACs

Cat.No: T74992

Proteasome-activating peptide 1 TFA

Cat.No: T76243

α1A-AR Degrader 9c

Cat.No: T74557

Target: PROTACs

Gliotoxin-13C13

Cat.No: T35773

Synonym: Gliotoxin-13C13

γ-AA peptide P6

Cat.No: T80686

Azurin p28 peptide

Cat.No: T80523

Cat.No: T68275

Cat.No: T69288

Tat-βsyn-degron TFA

Cat.No: T83726

Cat.No: T75133

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
T7064	Valproic Acid Sodium valproate,2-Propylpentanoic Acid,丙戊酸,VPA,Depakine,2-Propylvaleric Acid	Mitophagy; Gamma-secretase; HIV Protease; GABA Receptor; Sodium Channel; HDAC; Autophagy	Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience; Proteases/Proteasome; Stem Cells
	Valproic Acid (2-Propylpentanoic Acid) 是一种 HDAC 抑制剂，可抑制 HDAC1 活性，诱导 HDAC2 降解，具有口服活性。Valproic Acid 可以用于癫痫和躁郁症的研究。
T3391	Corosolic acid Corsolic acid,2α-Hydroxyursolic acid,科罗索酸,Glucosol,Colosolic acid,Colosic acid	FAK; Autophagy	Angiogenesis; Autophagy; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Corosolic acid (Colosic acid) 是从大花紫薇中提取的一种天然产物，具有抗肿瘤活性。
T5679	(E)-Ferulic acid trans-Ferulic acid,反式阿魏酸,(E)-Coniferic acid	BCL; Ferroptosis; Wnt/beta-catenin; Endogenous Metabolite	Apoptosis; Cytoskeletal Signaling; Metabolism; Stem Cells
	(E)-Ferulic acid ((E)-Coniferic acid) 是阿魏酸的异构体，阿魏酸是在植物细胞壁中丰富存在的芳香族天然产物。它引起 β-catenin 的磷酸化，导致其蛋白酶体降解，增加促凋亡因子 Bax 的表达，降低促生存因子的表达。它在人肺癌细胞系 H1299 中发挥抗增殖和抗迁移作用。
T4S1615	Sanggenon C 桑根酮C,桑根酮 C,Sanggenone C	NF-κB	NF-κB
	Sanggenon C (Sanggenone C) 是一种从桑属的根皮中分离得到的黄烷酮 Diels-Alder 加合物化合物。它可抑制NF-κB 活性，抑制 RAW264.7 细胞中诱导型一氧化氮合酶的表达，以及肿瘤坏死因子-α 刺激的细胞粘附和血管细胞粘附分子-1 的表达。它具有抗氧化和抗炎作用，也有抑制胰脂肪酶作用。
T16719	Radicicol 根赤壳菌素,Monorden	HSP	Cytoskeletal Signaling; Metabolism
	Radicicol is an antifungal antibiotic, impairs mitochondrial replication by targeting P. falciparum topoisomerase VIB. Radicicol is an inhibitor of Hsp90 (IC50: 1 μM). Radicicol binds to the ATPase domain of Hsp90 and prevents maturation of Hsp90 clients,

天然产物

Cat.No: T7064

Synonym: Sodium valproate,2-Propylpentanoic Acid,丙戊酸,VPA,Depakine,2-Propylvaleric Acid

Target: Mitophagy, Gamma-secretase, HIV Protease, GABA Receptor, Sodium Channel, HDAC, Autophagy

Cat.No: T3391

Synonym: Corsolic acid,2α-Hydroxyursolic acid,科罗索酸,Glucosol,Colosolic acid,Colosic acid

Target: FAK, Autophagy

(E)-Ferulic acid

Cat.No: T5679

Synonym: trans-Ferulic acid,反式阿魏酸,(E)-Coniferic acid

Target: BCL, Ferroptosis, Wnt/beta-catenin, Endogenous Metabolite

Cat.No: T4S1615

Synonym: 桑根酮C,桑根酮 C,Sanggenone C

Target: NF-κB

Cat.No: T16719

Synonym: 根赤壳菌素,Monorden

Target: HSP

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