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Search Results for " ubiquitination "

66

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13244	Ubiquitination-IN-1	Others	Others
	Ubiquitination-IN-1 是一种有效的泛素化和Cksl-Skp2蛋白互作抑制剂 (IC50=0.17 μM) 抑制剂，增加 p27 水平，可通过阻断肿瘤抑制因子的降解发挥作用。
T75030	Ubiquitination-IN-2
	Ubiquitination-IN-2是一种高效的E1-E2蛋白-蛋白相互作用(PPI)抑制剂，其对泛素E1(UBA1)的Kd值为0.72μM。该化合物有效抑制泛素从E1到E2的转移，适用于癌症研究。
T8773	MID-1	Others; IGF-1R	Others; Tyrosine Kinase/Adaptors
	MID-1 是 MG53-IRS-1 相互作用的抑制剂，能够破坏 MG53 与 IRS-1 的分子缔合，并消除 MG53 诱导的 IRS-1 泛素化和骨骼肌降解，升高 IRS-1 表达水平，增加胰岛素信号传导和葡萄糖摄取。
T21773	SP-141 SP 141	Mdm2	Apoptosis
	SP-141 是一种 MDM2 抑制剂，可促进 MDM2 自身泛素化和降解，具有抗癌活性。
T2026	CYM5442	S1P Receptor; LPL Receptor	GPCR/G Protein
	CYM5442 是高选择性和口服活性的鞘氨醇 1-磷酸受体激动剂，EC50为 1.35 nM。它激活依赖 S1P1的 p42/p44-MAPK 磷酸化，具有视网膜神经保护作用，可轻松穿过中枢神经系统。
T6697	TCID UCH-L3 Inhibitor	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	TCID (UCH-L3 Inhibitor) 是一种有效的选择性神经元泛素 C 末端水解酶 L3 的 DUB 抑制剂，IC50为 0.6 μM。它对 L1 具有 125 倍的选择性，可减少脑干和脊髓原代神经元中的甘氨酸转运蛋白 GlyT2 泛素化。
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。
T9758	dCeMM3 2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide	Others	Others
	dCeMM3 (2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide) 是一种胶降解剂，可以诱导 cyclin K 的泛素化和降解。机制是通过促进 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用。
T25465	GS143 GS-143,GS 143	IκB/IKK; E1/E2/E3 Enzyme; NF-κB	NF-κB; Ubiquitination
	GS-143 是选择性的IκBα泛素化抑制剂，抑制 SCFβTrCP1介导的IκBα泛素化作用，IC50=5.2 μM。GS143 抑制NF-κB 的活化和靶基因的转录，并且不抑制蛋白酶体的特性，并具有抗哮喘作用。
T8931L	ICCB-19 hydrochloride ICCB-19 HCl（750621-52-4 free base）	Apoptosis; Others; Autophagy; RIP kinase	Apoptosis; Autophagy; NF-κB; Others
	ICCB-19 hydrochloride (ICCB-19 HCl) 是RIPK1激酶活性的间接抑制剂。它是一种 TRADD 抑制剂，可与 TRADD 的 N 端结构域结合，破坏其与 TRADD-C 和 TRAF2 的结合，诱导自噬和长寿命蛋白质的降解。
T36682	USP30 inhibitor 18	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	USP30 inhibitor 18 是有效的USP30选择性抑制剂，IC50为 0.02 μM。它增加蛋白质泛素化并加速线粒体自噬。
T17187	TZ9	Apoptosis; E1/E2/E3 Enzyme	Apoptosis; Ubiquitination
	TZ9 是一种具有选择性和有效性的 Rad6 抑制剂，具有抗癌和而抗肿瘤活性。TZ9 对 Rad6B 诱导的组蛋白 H2A 泛素化有抑制作用。TZ9 诱导细胞周期停滞和细胞凋亡。
T61477	dCeMM2	Molecular Glues	PROTAC
	dCeMM2 (Compound 2) 是一种胶降解剂。dCeMM2 促使 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用，导致 cyclin K 的泛素化及降解。
T73560	I-138	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	I-138 是一种具有口服活性和有效性的 USP1-UAF1 可逆抑制剂。I-138 促使细胞中 FANCD2 和 PCNA 的单泛素化，抑制细胞中的 USP1 自裂解。
T1919	Tenovin-1 Tenovin 1	Mdm2; Dehydrogenase; Sirtuin; p53; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism
	Tenovin-1 抑制 SirT1 和 SirT2 的蛋白质去乙酰化活性，并防止 MDM2 介导的 p53 降解，这涉及泛素化。它具有癌症的研究潜力。
T37042	SCH529074 SCH 529074	p53	Apoptosis
	SCH529074 是 p53 的选择性激活剂 (Ki = 1 μM)，可用于非小细胞肺癌的研究。 SCH529074 恢复突变 p53 功能并中断 HDM2 介导的野生型 p53 泛素化。
T16904	Smurf1-IN-A01 A01	Others	Others
	Smurf1-IN-A01 (A01) 是泛素连接酶 Smad 泛素化调节因子-1(Smurf1)抑制剂，其kd=3.664 nM。它能够抑制 Smurf1 介导的 Smad1/5 降解，并提高 BMP-2 的反应性。
T17879	E3 ligase Ligand 8	Others; Ligand for E3 Ligase	Others; PROTAC
	E3 ligase Ligand 8 是 E3 泛素连接酶配体。它能够利用 linker 与靶蛋白配体连接，形成 PROTAC 分子。PROTAC 可诱导促癌蛋白发生泛素化降解。
T22263	Bavdegalutamide ARV-110	Androgen Receptor	Endocrinology/Hormones
	Bavdegalutamide (ARV-110) 是一种雄激素受体 (AR) 的 PROTAC 降解剂。 Bavdegalutamide 可用于前列腺癌的研究。 Bavdegalutamide 具有口服活性和选择性，并促进 AR 的泛素化和降解。
T8488	GMB-475	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	GMB-475 是一种基于PROTAC 的BCR-ABL1酪氨酸激酶降解剂，克服了BCR-ABL1依赖的耐药性。 GMB-475 靶向 BCR-ABL1 蛋白并募集 E3 连接酶 Von Hippel Lindau (VHL)。导致泛素化和随后的致癌融合蛋白降解
T64339	Apcin A HCL	APC	Cell Cycle/Checkpoint
	Apcin A HCL 是 Apcin 衍生物。它是一种后期促进复合物 (APC) 抑制剂。它与 Cdc20 强烈相互作用，并抑制 Cdc20 底物的泛素化。它可用于合成 PROTAC CP5V。
T16974	TAK-243 MLN7243	Apoptosis; E1/E2/E3 Enzyme; NF-κB	Apoptosis; NF-κB; Ubiquitination
	TAK-243 (MLN7243) 是一种泛素激活酶 UAE 的抑制剂 (IC50=1 nM)，具有选择性。TAK-243 可阻断泛素结合，破坏单泛素信号传导以及整体蛋白质泛素化。TAK-243 具有抗肿瘤活性，可以促进细胞凋亡。
T67834	C004019	Microtubule Associated; PROTACs	Cytoskeletal Signaling; PROTAC
	C004019是一种小分子 PROTAC ，能够靶向tau，用于从细胞内选择性降解蛋白质，同时招募tau 和E3连接酶（Vhl），选择性增强tau 蛋白的泛素化和蛋白水解。C004019是AD 及相关tau 蛋白疾病的候选药物。
T3317	SZL P1-41	Apoptosis; Others; E1/E2/E3 Enzyme	Apoptosis; Others; Ubiquitination
	SZL P1-41 是 Skp2 抑制剂，可以阻止 Skp2-Skp1 复合物的组装。它选择性地抑制 Skp2 SCF E3 连接酶活性，还在体内外抑制 Skp2 介导的 p27 和 Akt 泛素化。它通过触发细胞衰老和抑制糖酵解来抑制 Y 细胞和 Y 干细胞的存活，有抗肿瘤作用。
T14896	CC0651	Others	Others
	CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently inhibits the ubiquitination of p27Kip1 (IC50: 1.72 μM).
T25738	Linichlorin A Elegin
	Linichlorin A is used as a p27(Kip1) ubiquitination inhibitor.
T27213	DSHN
	DSHN is a small heterodimer partner (SHP) activator. DSHN transcriptionally activates SHP mRNA, and stabilizes the SHP protein by preventing its ubiquitination and degradation.
T70902	AQ-101
	AQ-101 is a inhibitor of MDM2, which induces MDM2 protein degradation through a self-ubiquitination and proteasome-mediated mechanism.
T31834	FMHM
	FMHM is a TRAF6 scavenging agent via ubiquitination-dependent mode.
T10345	Apcin-A	Others	Others
	Apcin-A is an anaphase-promoting complex (APC) inhibitor. It interacts strongly with Cdc20 and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V.
T25889	NSC-689857 NSC 689857,NSC689857
	NSC-689857 is an inhibitor that acts in the Skp2-Cks1 protein-protein interaction and p27Kip1 ubiquitination in vitro.
T34168	PROTAC-I PROTAC I
	PROTAC-I targets steroid hormone receptors for ubiquitination and degradation.
T69977	BC-1485
	BC-1485 is a first-in-class inhibitor of Fibrosis-inducing E3 ligase 1 (FIEL1 ), which disrupts FIEL1-directed PIAS4 ubiquitination.
T17871	E3 ligase Ligand 13	Others	Others
	E3 ligase Ligand 13 is an E3 ubiquitin ligase ligand that can be employed to create PROTACs, which are connected to the ligand for the protein through a linker. PROTACs serve as inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
T75125	ITK degrader 2
	ITKdegrader 2（compound 30），作为一种靶向泛素化的调节剂及靶向蛋白质降解分子，能够降解ITK。
T37646	HB007
	HB007 is a potent degrader of small ubiquitin-related modifier 1 (SUMO1). It mediates the ubiquitination and subsequent degradation of SUMO1, leading to a decrease in tumor growth in vivo. HB007 is a valuable tool for investigating brain, breast, colon, and lung cancers[1][2].
T17872	E3 ligase Ligand 14	Others	Others
	E3 ligase Ligand 14 is a ligand that binds to E3 ubiquitin ligase and can be conjugated to a protein ligand via a linker to create PROTACs. These PROTACs are capable of promoting ubiquitination-mediated degradation of cancer-promoting proteins[1].
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。
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.
T82632	Cys-C-cGMP	AUTACs	PROTAC
	Cys-C-cGMP 为一种AUTACs自噬标签。它能够促进HeLa细胞线粒体K63链式连接的泛素化增加。
T61776	TEAD-IN-2
	TEAD-IN-2 is an innovative, orally bioavailable inhibitor that targets the transcriptional enhancer associate domain (TEAD). It functions by regulating TEAD through ubiquitination and/or degradation by specific compounds. This compound, TEAD-IN-2, holds potential for studying various diseases, disorders, or conditions linked to TEAD [1].
T61057	dCeMM4
	dCeMM4 (Compound 5) 是通过促进 CDK12-cyclin K 与 CRL4B 连接酶复合物的相互作用来诱导 cyclin K 的泛素化和降解的分子胶降解剂。
T70096	AEG40730 HCl
	AEG40730 is a potent and selective IAP antagonist and a BIR-binding tetrapeptide. AEG40730 binds to cIAP1 and cIAP2, facilitates their autoubiquitination and proteosomal degradation, and causes a dramatic reduction in RIP1 ubiquitination. Treatment with nanomolar concentrations of AEG40730 resulted in the loss of both XIAP and c-IAP1 proteins, albeit with different kinetics.
T61688	Nrf2 activator-2
	Nrf2 activator-2 (referred to as compound O15), an Osthole derivative, is a highly potent Nrf2 agonist exhibiting an EC 50 of 2.9 μM in 293 T cells. By effectively disrupting the binding between Keap1 and Nrf2, Nrf2 activator-2 activates the Nrf2 pathway. Furthermore, this compound significantly reduces the ubiquitination of Nrf2 in cells, indicating its potential in regulating Nrf2 activity [1].
T69701	HS-152
	HS-152 is a novel reversible inhibitor of smurf1, directly targeting the catalytic activity of smurf hect domains, significantly blocking auto-ubiquitination and the transfer of ubiquitin from hect domain to the substrates to form isopeptide bond
T17876	E3 ligase Ligand 18	Others	Others
	E3 ligase Ligand 18 is a ligand that binds to E3 ubiquitin ligase, and it can be chemically attached to a protein ligand through a linker to create PROTACs. The resulting PROTACs function as inducers of ubiquitination-mediated degradation, targeting cancer-promoting proteins[1].
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.
T17880	E3 ligase Ligand 9	Others	Others
	E3 ligase Ligand 9 is a compound that serves as a ligand for E3 ubiquitin ligase. It can be linked to the protein ligand through a linker, forming PROTACs or SNIPERs. These PROTACs are known to induce the degradation of cancer-promoting proteins through ubiquitination-mediated mechanisms[1].
T17363	β-Naphthoflavone-CH2-OH β-NF-CH2-OH	Others	Others
	β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) serves as an AhR E3 ligase ligand, forming chimeric molecules when connected to a protein ligand through a linker, resulting in PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1). These chimeric molecules recruit the AhR E3 ligase complex by incorporating AhR ligands. By inducing ubiquitination-mediated degradation, PROTACs effectively target and degrade cancer-promoting proteins [1].
T76372	TRAF6 peptide
	TRAF6 peptide 是一种特异性的TRAF6-p62相互作用抑制剂。TRAF6 peptide 能消除 NGF 依赖性TrkA 泛素化。TRAF6 peptide 在诸如阿尔茨海默症 (AD)、帕金森、ALS、头部外伤、癫痫和中风等神经系统性疾病中具有较好的研究潜力。

化合物

Ubiquitination-IN-1

Cat.No: T13244

Target: Others

Ubiquitination-IN-2

Cat.No: T75030

Cat.No: T8773

Target: Others, IGF-1R

Cat.No: T21773

Synonym: SP 141

Target: Mdm2

Cat.No: T2026

Target: S1P Receptor, LPL Receptor

Cat.No: T6697

Synonym: UCH-L3 Inhibitor

Target: DUB

Cat.No: T1862

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

Target: Apoptosis, DUB, Autophagy

Cat.No: T9758

Synonym: 2-(1H-benzimidazol-2-ylsulfanyl)-N-(5-chloropyridin-2-yl)acetamide

Target: Others

Cat.No: T25465

Synonym: GS-143,GS 143

Target: IκB/IKK, E1/E2/E3 Enzyme, NF-κB

ICCB-19 hydrochloride

Cat.No: T8931L

Synonym: ICCB-19 HCl（750621-52-4 free base）

Target: Apoptosis, Others, Autophagy, RIP kinase

USP30 inhibitor 18

Cat.No: T36682

Target: DUB

Cat.No: T17187

Target: Apoptosis, E1/E2/E3 Enzyme

Cat.No: T61477

Target: Molecular Glues

Cat.No: T73560

Target: DUB

Cat.No: T1919

Synonym: Tenovin 1

Target: Mdm2, Dehydrogenase, Sirtuin, p53, Autophagy

Cat.No: T37042

Synonym: SCH 529074

Target: p53

Cat.No: T16904

Synonym: A01

Target: Others

E3 ligase Ligand 8

Cat.No: T17879

Target: Others, Ligand for E3 Ligase

Bavdegalutamide

Cat.No: T22263

Synonym: ARV-110

Target: Androgen Receptor

Cat.No: T8488

Target: Bcr-Abl

Cat.No: T64339

Target: APC

Cat.No: T16974

Synonym: MLN7243

Target: Apoptosis, E1/E2/E3 Enzyme, NF-κB

Cat.No: T67834

Target: Microtubule Associated, PROTACs

Cat.No: T3317

Target: Apoptosis, Others, E1/E2/E3 Enzyme

Cat.No: T14896

Target: Others

Cat.No: T25738

Synonym: Elegin

Cat.No: T27213

Cat.No: T70902

Cat.No: T31834

Cat.No: T10345

Target: Others

Cat.No: T25889

Synonym: NSC 689857,NSC689857

Cat.No: T34168

Synonym: PROTAC I

Cat.No: T69977

E3 ligase Ligand 13

Cat.No: T17871

Target: Others

Cat.No: T75125

Cat.No: T37646

E3 ligase Ligand 14

Cat.No: T17872

Target: Others

γ-AA peptide P6

Cat.No: T80686

PROTAC Mcl1 degrader-1

Cat.No: T11975

Target: BCL

Cat.No: T82632

Target: AUTACs

Cat.No: T61776

Cat.No: T61057

Cat.No: T70096

Nrf2 activator-2

Cat.No: T61688

Cat.No: T69701

E3 ligase Ligand 18

Cat.No: T17876

Target: Others

Cat.No: T10875

Target: Others

E3 ligase Ligand 9

Cat.No: T17880

Target: Others

β-Naphthoflavone-CH2-OH

Cat.No: T17363

Synonym: β-NF-CH2-OH

Target: Others

Cat.No: T76372

Cat. No.	Product Name	Target	Signaling Pathways
T4970	LANOSTEROL 羊毛甾醇,3β-Hydroxy-8,24-lanostadiene,8,24-Lanostadien-3β-ol	Endogenous Metabolite	Metabolism
	Lanosterol (3β-Hydroxy-8,24-lanostadiene) 是胆固醇合成的中间产物，能够诱导胆固醇合成的速率控制酶 HMG-CoA 还原酶的泛素化和降解。Lanosterol 可以抑制神经退行性疾病相关错误折叠蛋白的聚集和细胞毒性。
T2140	Parthenolide (-)-Parthenolide,小白菊内酯	Apoptosis; Mitophagy; NF-κB; HDAC; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; NF-κB
	Parthenolide ((-)-Parthenolide) 是一种从药草短舌匹菊中发现的倍半萜内酯。它抑制NF-κB 活化，有抗炎活性。它还可抑制HDAC1蛋白，但不影响其他I/II 类HDAC。
T6S1780	Protosappanin B 原苏木素B,Q-100961,FT-0689654	Apoptosis	Apoptosis
	Protosappanin B (Q-100961) 是从苏木中提取的一种多酚类天然产物，具有抗肿瘤作用。它通过激活 MDM2 依赖性泛素化过程诱导 p53 蛋白降解。它显著提高细胞活力，抑制细胞凋亡并上调生长相关蛋白 43 的表达。

天然产物

Cat.No: T4970

Synonym: 羊毛甾醇,3β-Hydroxy-8,24-lanostadiene,8,24-Lanostadien-3β-ol

Target: Endogenous Metabolite

Cat.No: T2140

Synonym: (-)-Parthenolide,小白菊内酯

Target: Apoptosis, Mitophagy, NF-κB, HDAC, Autophagy

Protosappanin B

Cat.No: T6S1780

Synonym: 原苏木素B,Q-100961,FT-0689654

Target: Apoptosis

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