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Search Results for " proteasome in 1 "

44

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12561	Proteasome-IN-1	Proteasome	Proteases/Proteasome; Ubiquitination
	Proteasome-IN-1 is an inhibitor of proteasome.
T81373	Proteasome β2c/i-IN-1	Proteasome	Proteases/Proteasome; Ubiquitination
	Proteasomeβ2c/i-IN-1（compound 37）为针对β2c和β2i亚基的选择性蛋白酶抑制剂。
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。
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。
T63321	20S Proteasome activator 1	Proteasome	Proteases/Proteasome; Ubiquitination
	20S Proteasome activator 1 是一种 20S 蛋白酶激活剂，对胰蛋白酶样位点、胰凝乳蛋白酶样位点和半胱天冬酶位点的 IC50 分别为 0.3 μM、0.7 μM 和 1.8 μM。20S Proteasome activator 1 通过在细胞系统中翻译来防止致病性 α-synuclein A53T 突变体积累从而减少疾病发生的概率。20S Proteasome activator 1 可用于研究神经退行性疾病。
T77620	LMTK3-IN-1	c-Met/HGFR	Tyrosine Kinase/Adaptors
	LMTK3-IN-1 是一种有效的 ATP 竞争性狐猴酪氨酸激酶 3 (LMTK3) (Kd=2.5 μM) 抑制剂，通过泛素蛋白酶体途径降解 LMTK3 发挥特性。LMTK3-IN-1 在多种癌细胞系和体内 BC 小鼠模型中展现出抗癌活性。 LMTK3-IN-1（10-20 μM）可诱导 BC 细胞系凋亡。
T12818	S119-8	Influenza Virus	Microbiology/Virology
	S119-8 是一种广谱甲型和乙型流感病毒抑制剂，抑制多种乙型流感病毒和耐奥司他韦的甲型流感病毒。
T81371	Proteasome-IN-5	Proteasome	Proteases/Proteasome; Ubiquitination
	Proteasome-IN-5（compound 5）是一款有效的蛋白酶体抑制剂。
T16795	Rpn11-IN-1 Capzimin intermediate	Others	Others
	Rpn11-IN-1 is an effective and selective inhibitor of proteasome subunit Rpn11 (IC50: 390 nM).
T62255	20S Proteasome-IN-4
	20S Proteasome-IN-4 (Compound 7) 是一种能透过血脑屏障的、寄生虫选择性的、具有口服活性的20Sproteasome 抑制剂，对T. b. brucei20S 蛋白酶体的IC50为 6.3 nM。20S Proteasome-IN-4 可用于非洲人类锥虫病的研究。
T75870	PR-39 TFA
	PR-39 TFA 是富含脯氨酸和精氨酸的天然抗菌肽，是一种非竞争性，可逆和变构的蛋白酶体 (proteasome) 抑制剂。PR-39 TFA 可逆地结合到蛋白酶体的 α7 亚基上，并通过泛素-蛋白酶体途径阻断 NF-κB 抑制剂 IκBα 的降解。PR-39 TFA 刺激小鼠的血管生成，抑制炎症反应并显着减小心肌梗死面积。
T78847	BC-05	Others	Others
	BC-05为一CD13及20S蛋白酶体的口服有效抑制剂，分别对人CD13和20S蛋白酶体的IC50值为0.13 μM与1.39 μM。该化合物适用于进行多发性骨髓瘤相关研究。
T80129	Baceridin	Proteasome	Proteases/Proteasome; Ubiquitination
	Baceridin是环状六肽类proteasome抑制剂，可从Epiphytic Bacillus培养基中提取。该化合物能够通过p53独立途径阻断细胞周期并促进肿瘤细胞凋亡，因而常用于癌症研究。
T79474	GSPT1 degrader-1	Apoptosis	Apoptosis
	GSPT1 degrader-1 (compound 9q) 是通过泛素蛋白酶体系统有效实现 G1 至 S 相变 1 (GSPT1) 降解的化合物。此外，该化合物能诱导G0/G1 期细胞停滞及细胞凋亡 (apoptosis)。
T68869	TP-110
	TP-110 is a new proteasome inhibitor, which shows potent growth inhibition in various tumor cell lines. Treatment with TP-110 for 24 h in vitro induced apoptosis in multiple myeloma cell line RPMI8226. TP-110 reduced the intrinsic inhibitor of apoptosis proteins (IAPs), cIAP-1 and XIAP, that suppress executioner caspases.
T40255	VCP/p97 inhibitor-1 VCP/p97 inhibitor-1
	VCP/p97 inhibitor-1, a highly effective compound, inhibits VCP/p97 (also known as Cdc48, CDC-48, or Ter94) with an IC 50 of 54.7 nM. This inhibitor induces a disruption in protein homeostasis and interferes with the degradation process of misfolded polypeptides by the ubiquitin-proteasome system (UPS).
T76038	Ac-Nle-Pro-Nle-Asp-AMC
	Ac-Nle-Pro-Nle-Asp-AMC 是26S 蛋白酶体(26Sproteasome)的特异性底物，适用于分析26S 蛋白酶体中caspase样活性。
T69880	YW2065
	YW2065 has excellent anti-colorectal cancer effects in vitro and in vivo. YW2065 achieves its inhibitory activity for Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin. Simultaneously, YW2065 also led to the activation of the tumor suppressor AMPK, providing an additional anticancer mechanism. In addition, YW2065 showed favorable pharmacokinetic properties without obvious toxicity.
T75869	PSI TFA
	PSI (TFA) 是一种有效的蛋白酶体proteasome 抑制剂。PSI (TFA) 抑制原发性渗出性淋巴瘤 (PEL) 细胞的增殖。PSI (TFA) 可用于卡波济氏肉瘤相关疱疹病毒 (KSHV) 感染和 KSHV 相关淋巴瘤的研究。
T74878	Enzyme-IN-1
	Enzyme-IN-1（compound 1）为基于肽的N端亲核试剂（Ntn）水解酶抑制剂，特别针对20S蛋白酶体的糜胰蛋白酶样活性（CT-L）进行抑制，可能展现出抗炎特性。
T17646	Boc-C1-PEG3-C4-OBn	Others	Others
	Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PEG-based PROTAC linker employed in the synthesis of various PROTACs, including PROTAC SGK3 degrader-1. PROTACs are composed of two distinct ligands connected by a linker; one ligand binds to an E3 ubiquitin ligase, while the other specifically interacts with the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs can selectively degrade target proteins[1].
T77974	PROTAC BCR-ABL Degrader-1	PROTACs	PROTAC
	PROTACBCR-ABLDegrader-1（化合物PROTAC1）是一种含有2-oxoethyl linker的PROTAC。该化合物能通过泛素蛋白酶体（ubiquitinproteasom）系统诱导Bcr-Abl的降解，并对K562细胞表现出抗增殖效果，显示出其在癌症研究中的应用潜力。
T35481	DD 03-171
	Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.
T18543	Phthalimide-PEG4-MPDM-OH	Others	Others
	Phthalimide-PEG4-MPDM-OH, a PROTAC linker with a PEGs composition, has applications in the synthesis of various PROTACs. These PROTACs consist of a linker connecting two distinct ligands: one binds to an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively induce the degradation of target proteins [1].
T18649	(±)15-HETE	Others	Others
	(±)15-HETE is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
T74755	TUS-007
	TUS-007是一种经蛋白酶体抑制剂修饰的CANDDY分子。尽管如此，TUS-007几乎不影响蛋白酶体活性。它是口服有效的KRASG12D/V降解剂，适用于KRAS G12D/V的无细胞化学敲除，并展现出抑制肿瘤的效果。【CANDDY：具亲和力及降解动力学的化学敲除】。
T18544	Phthalimide-PEG4-PDM-OTBS	Others	Others
	Phthalimide-PEG4-PDM-OTBS is a PROTAC linker comprised of polyethylene glycols (PEGs). This compound is utilized in the synthesis of a range of PROTACs, which consists of two distinct ligands connected by a linker. One ligand binds to an E3 ubiquitin ligase, while the other ligand binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively degrade target proteins[1].
T17647	Boc-C1-PEG3-C4-OH	Others	Others
	Boc-C1-PEG3-C4-OH is an Alkyl/ether-based PROTAC linker utilized in the synthesis of PROTACs, which are characterized by their structure comprising two distinct ligands tethered by a linker. One ligand of PROTACs binds to an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs facilitate the targeted degradation of specific proteins[1].
T18542	Phthalimide-PEG3-C2-OTs	Others	Others
	Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker composed of PEGs. It is utilized in the synthesis of various PROTACs, which involve the connection of two distinct ligands through a linker. One ligand is specific for an E3 ubiquitin ligase, while the other ligand is designed for targeting the specific protein of interest. Through leveraging the intracellular ubiquitin-proteasome system, PROTACs are capable of selectively degrading target proteins [1].
T79505	PROTAC TG2 degrader-1	PROTACs	PROTAC
	PROTACTG2 degrader-1（化合物 11）是一种靶向组织转谷氨酰胺酶 (TG2) 的VHL基PROTAC，具有68.9 μM的KD值。该化合物通过蛋白酶体途径降低卵巢癌细胞中TG2的水平。
T74300	MS143
	MS143 是一种有效的AKT 降解剂，在 PC3 细胞中DC50=46 nM，GI50=0.8 µM。MS143 通过劫持泛素-蛋白酶体系统，以浓度和时间依赖性的方式诱导快速、稳定的AKT 降解。MS143 能抑制癌细胞生长。
T77939	WBC100 14-D-Valine-TPL	c-Myc	Cell Cycle/Checkpoint
	WBC100（14-D-Valine-TPL），一款高效、选择性和具口服活性的c-Myc小分子降解剂，通过针对泛素E3连结酶CHIP介导的26S蛋白酶体途径实现其作用。主要应用于c-Myc过表达肿瘤的研究领域。
T74508	SS47
	SS47 是一种基于PROTAC 的HPK1降解剂，可发挥蛋白酶体介导的 HPK1 降解。SS47 降解 HPK1 也显着增强了 BCMA CAR-T 细胞研究的体内抗肿瘤功效。HPK1 是一种免疫抑制调节激酶，是肿瘤免疫疗法的有潜力靶点。
T36321	C6 Urea Ceramide
	C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the ...
T74792	USP28-IN-2
	USP28-IN-2是一种高选择性的USP28抑制剂(IC50=0.3 μM)，能够特异性作用于USP2、USP7、USP8、USP9x、UCHL3 和 UCHL5。在体外实验中，USP28-IN-2对癌细胞表现出细胞毒性，作用机制为通过泛素-蛋白酶体途径降低c-Myc蛋白水平，并能减少Ankyrase-1/2的表达。此外，USP28-IN-2能增强结直肠癌细胞对药物瑞戈非尼的敏感性。
T81421	Pomalidomide-C5-Dovitinib	PROTACs	PROTAC
	Pomalidomide-C5-Dovitinib（compound 2）是链接Pomalidomide与Dovitinib的PROTAC，且与CRBN结合。该化合物在FLT3-ITD+ AML细胞中表现出增强的抗增殖能力，通过泛素-蛋白酶体依赖性途径促进FLT3-ITD和KIT蛋白的降解，并彻底抑制其下游信号传导，显示出研究FLT3-ITD+急性髓系白血病的潜力。
T81747	MS6105	PROTACs	PROTAC
	MS6105是一种具有抗癌活性的LDH蛋白水解靶向嵌合体(PROTAC)，能够依赖时间及泛素蛋白酶体系统高效地降解LDHA和LDHB。同时，MS6105也是一个点击化学试剂，含有Alkyne基团，能与含Azide基团的分子通过铜催化的叠氮-炔环加成反应(CuAAc)发生反应。
T37329	PROTAC IDO1 Degrader-1 PROTAC IDO1 Degrader-1
	PROTAC IDO1 Degrader-1 is the first potent IDO1 (indoleamine 2,3-dioxygenase 1) degrader that hijacks IDO1 to CRBN E3 ligase to introduce IDO1 into UPS and eventually achieve ubiquitination and degradation (DC50=2.84 μM). PROTAC IDO1 Degrader-1 moderately improves the tumor-killing activity of H ER2 CAR-T cells[1]. PROTAC IDO1 Degrader-1 (compound 2c) (10 μM; 24 hours) notably decreases IDO1 level induced by IFN-γ[1].PROTAC IDO1 Degrader-1 and IFN-γ (5 ng/mL) are incubated with HeLa cells for 24...
T74635	MS9449	PROTACs	PROTAC
	MS9449 是一种高效的 PROTAC EGFR 降解剂，其对野生型 EGFR 和突变型 EGFR L858R 的 Kd 值分别为 17 nM 和 10 nM。该化合物通过 UPS (泛素/蛋白酶体系统) 和自噬/溶酶体途径，有效促进突变型 EGFRs 的降解，并对 NSCLC（非小细胞肺癌）细胞增殖显示出显著的抑制效果，适用于抗癌研究。
T74634	MS9427 TFA
	MS9427 TFA 是一种有效的 PROTACEGFR 降解剂，对野生型 EGFR 和突变型 EGFRL858R 的 Kd 分别为 7.1 nM 和 4.3 nM。MS9427 TFA 通过泛素/蛋白酶体系统 (UPS) 和自噬/溶酶体途径选择性地降解突变体，但不降解 WTEGFR。MS9427 TFA 对 NSCLC 细胞增殖有较强的抑制作用。MS9427 TFA 可用于抗癌研究。
T74633	MS9427
	MS9427 是一种有效的PROTACEGFR 降解剂，对野生型EGFR 和突变型EGFRL858R 的Kd 分别为 7.1 nM 和 4.3 nM。MS9427 通过泛素/蛋白酶体系统 (UPS) 和自噬/溶酶体途径选择性地降解突变体，但不降解WTEGFR。MS9427 对 NSCLC 细胞增殖有较强的抑制作用。MS9427 可用于抗癌研究。
T79718	CaMKIIα-PHOTAC	CaMK	Neuroscience
	CaMKIIα-PHOTAC是一种靶向Ca2+/钙调蛋白依赖性蛋白激酶IIα（CaMKIIα）的光化学靶向嵌合体（PHOTAC）。该分子在特定波长光照射下实现靶蛋白的泛素化及通过蛋白酶体催化的降解。CaMKIIα-PHOTAC能在光照条件下显著降低小鼠海马区域的诱发LTP反应强度，减弱突触功能，并对维护亚细胞级别的树突结构域、长时程增强及记忆能力起到关键作用。
T83856	AP-1
	AP-1是一种微型化的蛋白质水解靶向嵌合体（PROTAC），由吲哚美辛（±）连接的间变性淋巴瘤激酶（ALK）配体和E3泛素连接酶配体通过超短连接器相连。在10至300 nM浓度范围内使用时，AP-1能高效降解Karpas-299细胞中高表达的ALK融合蛋白NPM-ALK，此效应可被蛋白酶体抑制剂MG-132阻断。它还能降解在SN-N-SH和NCI H3122细胞中表达的ALK融合蛋白EML4-ALK及含有苯丙氨酸至亮氨酸替换突变（ALKF1174L）的ALK。AP-1对依赖ALK的Karpas-299细胞具有细胞毒性（IC50 = 0.1265 nM），但对非ALK依赖的THP-1细胞无细胞毒性（IC50 = 2,704 nM）。在给药剂量为25, 50, 和100 mg/kg时，能减小NCI H3122小鼠移植瘤模型中的肿瘤体积。
T37419	Zetomipzomib
	KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhib...

化合物

Proteasome-IN-1

Cat.No: T12561

Target: Proteasome

Proteasome β2c/i-IN-1

Cat.No: T81373

Target: Proteasome

Proteasome-activating peptide 1

Cat.No: T81372

Proteasome-activating peptide 1 TFA

Cat.No: T76243

20S Proteasome activator 1

Cat.No: T63321

Target: Proteasome

Cat.No: T77620

Target: c-Met/HGFR

Cat.No: T12818

Target: Influenza Virus

Proteasome-IN-5

Cat.No: T81371

Target: Proteasome

Cat.No: T16795

Synonym: Capzimin intermediate

Target: Others

20S Proteasome-IN-4

Cat.No: T62255

Cat.No: T75870

Cat.No: T78847

Target: Others

Cat.No: T80129

Target: Proteasome

GSPT1 degrader-1

Cat.No: T79474

Target: Apoptosis

Cat.No: T68869

VCP/p97 inhibitor-1

Cat.No: T40255

Synonym: VCP/p97 inhibitor-1

Ac-Nle-Pro-Nle-Asp-AMC

Cat.No: T76038

Cat.No: T69880

Cat.No: T75869

Cat.No: T74878

Boc-C1-PEG3-C4-OBn

Cat.No: T17646

Target: Others

PROTAC BCR-ABL Degrader-1

Cat.No: T77974

Target: PROTACs

Cat.No: T35481

Phthalimide-PEG4-MPDM-OH

Cat.No: T18543

Target: Others

Cat.No: T18649

Target: Others

Cat.No: T74755

Phthalimide-PEG4-PDM-OTBS

Cat.No: T18544

Target: Others

Boc-C1-PEG3-C4-OH

Cat.No: T17647

Target: Others

Phthalimide-PEG3-C2-OTs

Cat.No: T18542

Target: Others

PROTAC TG2 degrader-1

Cat.No: T79505

Target: PROTACs

Cat.No: T74300

Cat.No: T77939

Synonym: 14-D-Valine-TPL

Target: c-Myc

Cat.No: T74508

C6 Urea Ceramide

Cat.No: T36321

Cat.No: T74792

Pomalidomide-C5-Dovitinib

Cat.No: T81421

Target: PROTACs

Cat.No: T81747

Target: PROTACs

PROTAC IDO1 Degrader-1

Cat.No: T37329

Synonym: PROTAC IDO1 Degrader-1

Cat.No: T74635

Target: PROTACs

Cat.No: T74634

Cat.No: T74633

CaMKIIα-PHOTAC

Cat.No: T79718

Target: CaMK

Cat.No: T83856

Cat.No: T37419

Cat. No.	Product Name	Target	Signaling Pathways
T2S1837	Steviol 甜菊醇,NSC 226902,Hydroxydehydrostevic acid	Others	Others
	Steviol (NSC-226902) 是一种甜菊糖甙的主要代谢物。它能降低 AQP2 的表达，并促进 AQP2 的降解，从而减缓肾囊肿的生长。
T75488	Leptosphaerodione
	Leptosphaerodione，可从 Remotididymellasp. 中分离得到，是一种有效的泛素-蛋白酶体系统 (UPS) 抑制剂。Leptosphaerodione 在 HeLa 细胞中具有细胞毒性，IC50为 3.2 μM。抗肿瘤剂。

天然产物

Cat.No: T2S1837

Synonym: 甜菊醇,NSC 226902,Hydroxydehydrostevic acid

Target: Others

Leptosphaerodione

Cat.No: T75488

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