E3 Ligase

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研究领域

抑制剂选择性比较

E3 Ligase 产品

所有产品 E3 Ligase 抑制剂(11) E3 Ligase 激活剂(1) E3 Ligase 拮抗剂(2)

目录号	产品描述	文献引用	实验数据
S1029	Lenalidomide (CC-5013) Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。	Nat Cell Biol, 2020, 22(5):526-533 Mol Cell, 2020, 5;77(5):1092-1106 e9 Nat Commun, 2020, 17;11(1):359	Effect of lenalidomide treatment (50 mg/kg/day, p.o. for 3 days) on expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), Fas, Fas ligand (FasL), and cleaved caspase-3 in myocardium from lean and ob/ob mice. (a) Representative gel blots of TNF-α, IL-6, Fas, FasL, cleaved caspase-3 and α-Tubulin (as loading control) using specific antibodies. (b) TNF-α.
S1567	Pomalidomide Pomalidomide抑制LPS诱导的TNF-α释放，在PBMCs中IC50为13 nM。Pomalidomide 可以在PROTAC中用作靶向 E3 ligase 和抑制 E3 ligase protein cereblon (CRBN)。Pomalidomide可促进凋亡和细胞周期阻滞。	Leukemia, 2020, 1 Cell Chem Biol, 2020, 18 pii: S2451-9456(20)30117-3 Cell Chem Biol, 2020, 14;S2451-9456(20)30145-8	OPM2 cells stably expressing either NT or CRBN shRNA were seeded and incubated with pomalidomide at the indicated concentration, followed by MTT assay at day 3 after adding drugs. Each experimental condition was performed in triplicate and repeated at least once.
S1193	Thalidomide 沙利度胺作为一种镇静药，免疫调节剂，也用于研究治疗许多癌症的症状。沙利度胺抑制E3泛素连接酶（一种CRBN-DDB1-Cul4A复合物）。	Cell Chem Biol, 2020, 14;S2451-9456(20)30145-8 Cancer Cell Int, 2020, 19;20:58 Leukemia, 2019, 10.1038/s41375-019-0525-6	(E) MM.1S cells were treated with Thal(Thalidomide) or Pom for 48 hours. In each case, western blot was carried out using cell lysates and the indicated Abs.
S8449^New	VH298 VH298 是一种有效的 VHL (Von Hippel-Lindau, the E3 ligase) 的抑制剂，可稳定 HIF-α。VH298 可阻断VHL:HIF-α的相互作用，在等温滴定热分析 (ITC) 中的Kd值为90 nM、在竞争性荧光偏振测定中的Kd值为80 nM。VH-298可用于PROTAC技术。
S2225	TAME TAME是一种APC抑制剂。	Cancer Cell Int, 2020, 19;20:58	Knockdown of p21 or inhibiting APC/C by TAME sensitized NSCLC cells to 5-FU. Cells were treated with 5-FU. 2 days after treatment, surviving cells were stained with cystal violet. Representive microscopic fields were shown. The blue stained cells were counted and shown in histogram at the right side.
S2781	RITA (NSC 652287) RITA (NSC 652287)诱导DNA-蛋白质和DNA-DNA交联，检测不到DNA单链断裂，通过靶向作用于p53，也抑制MDM2-p53相互作用。	Cancer Cell, 2019, 35(2):191-203 Br J Cancer, 2018, 119(4):450-461 Radiol Oncol, 2016, 50(2):168-74	To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
S8000	Tenovin-1 Tenovin-1防止MDM2介导的p53的降解，涉及泛素化途径，通过抑制SirT1和SirT2的蛋白脱乙酰活性。	J Transl Med, 2019, 17(1):76 Int J Mol Med, 2019, 44(3):1091-1105	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
S2754	AT406 (SM-406) AT-406是一种有效的，拟Smac的IAP(通过E3泛素连接酶起作用的凋亡蛋白抑制剂)拮抗剂，与XIAP-BIR3， cIAP1-BIR3和cIAP2-BIR3结合，K_i为66.4 nM， 1.9 nM和5.1 nM，比作用于Smac AVPI肽亲和力高50到100倍。Phase 1。	Nature, 2020, 577(7788):109-114 Cell Death Dis, 2020, 22;11(5):391 Apoptosis, 2020, 21	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
S5315	PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.	Genome Res, 2019, 29(10):1659-1672
S8760	Iberdomide(CC220) Iberdomide (CC-220)是一种新型口服免疫调节化合物，靶向cereblon（cereblon是CRL4CRBN E3泛素连接酶复合体的一部分），IC50为60 nM。
S7892	Avadomide(CC-122) CC-122，一种新型的多效性修饰剂化合物，在弥漫性大B细胞淋巴瘤（DLBCL）中具有抗肿瘤、免疫调节活性。其分子靶标为cereblon (CRBN)，CRBN是E3泛素化连接酶复合体CRL4^CRBN的底物受体。	Blood Adv, 2019, 3(14):2105-2117
S2678	NSC 207895 NSC 207895抑制MDMX，IC50为2.5 μM，促进p53稳定/激活和DNA损伤，也调节MDM2（E3连接酶）。	Genes Dev, 2020, 34(7-8):526-543 Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).
S1061	Nutlin-3 Nutlin-3是一种有效的，选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂，无细胞试验中IC50为90 nM；可稳定p53缺陷细胞中的p73。	Clin Cancer Res, 2020, 26(1):122-134 Cell Rep, 2020, 30(2):497-509 Eur J Cancer, 2020, 126:93-103	Ubiquitination of p53 in vivo by BIRC6 in the presence of Nutlin-3. Cells were treated with Nutlin-3 (20 uM, 24 h) before harvest. Cell lysates were immunoprecipitated with anti-p53 antibody and immunoblotted by anti-ubiquitin antibody.
S1172	JNJ-26854165 (Serdemetan) JNJ-26854165 (Serdemetan)是一种HDM2泛素连接酶拮抗剂，作用于p53野生型细胞，诱导早期凋亡，在缺乏功能性p53的细胞中，抑制细胞增殖而延迟细胞凋亡。	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40
S8888^New	GMB-475 GMB-475 是一种靶向蛋白水解的嵌合体(PROTAC)，它以变构方式靶向 BCR-ABL1 蛋白并募集 the E3 ligase Von Hippel-Lindau (VHL)，从而导致泛素化并随后降解致癌融合蛋白。
S6794^New	Thalidomide-O-COOH (Cereblon ligand 3) Thalidomide-O-COOH (Cereblon ligand 3) 是基于Thalidomide的 Cereblon (CRBN) 配体，可用于募集CRBN蛋白。Thalidomide-O-COOH (Cereblon ligand 3) 可以通过连接器与蛋白质的配体连接以形成 PROTACs (Proteolysis Targeting Chimera)。

目录号	产品描述	文献引用	实验数据
S1029	Lenalidomide (CC-5013) Lenalidomide (CC-5013)是一种TNF-α分泌抑制剂，在PBMCs中IC50为13 nM。Lenalidomide (CC-5013) 是 ubiquitin E3 ligase cereblon (CRBN) 的配体，它通过CRBN-CRL4泛素连接酶引起两个淋巴样转录因子IKZF1和IKZF3的选择性泛素化和降解。	Nat Cell Biol,2020, 22(5):526-533 Mol Cell,2020, 5;77(5):1092-1106 e9 Nat Commun,2020, 17;11(1):359	Effect of lenalidomide treatment (50 mg/kg/day, p.o. for 3 days) on expression of tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), Fas, Fas ligand (FasL), and cleaved caspase-3 in myocardium from lean and ob/ob mice. (a) Representative gel blots of TNF-α, IL-6, Fas, FasL, cleaved caspase-3 and α-Tubulin (as loading control) using specific antibodies. (b) TNF-α.
S1567	Pomalidomide Pomalidomide抑制LPS诱导的TNF-α释放，在PBMCs中IC50为13 nM。Pomalidomide 可以在PROTAC中用作靶向 E3 ligase 和抑制 E3 ligase protein cereblon (CRBN)。Pomalidomide可促进凋亡和细胞周期阻滞。	Leukemia,2020, 1 Cell Chem Biol,2020, 18 pii: S2451-9456(20)30117-3 Cell Chem Biol,2020, 14;S2451-9456(20)30145-8	OPM2 cells stably expressing either NT or CRBN shRNA were seeded and incubated with pomalidomide at the indicated concentration, followed by MTT assay at day 3 after adding drugs. Each experimental condition was performed in triplicate and repeated at least once.
S1193	Thalidomide 沙利度胺作为一种镇静药，免疫调节剂，也用于研究治疗许多癌症的症状。沙利度胺抑制E3泛素连接酶（一种CRBN-DDB1-Cul4A复合物）。	Cell Chem Biol,2020, 14;S2451-9456(20)30145-8 Cancer Cell Int,2020, 19;20:58 Leukemia,2019, 10.1038/s41375-019-0525-6	(E) MM.1S cells were treated with Thal(Thalidomide) or Pom for 48 hours. In each case, western blot was carried out using cell lysates and the indicated Abs.
S8449^New	VH298 VH298 是一种有效的 VHL (Von Hippel-Lindau, the E3 ligase) 的抑制剂，可稳定 HIF-α。VH298 可阻断VHL:HIF-α的相互作用，在等温滴定热分析 (ITC) 中的Kd值为90 nM、在竞争性荧光偏振测定中的Kd值为80 nM。VH-298可用于PROTAC技术。
S2225	TAME TAME是一种APC抑制剂。	Cancer Cell Int,2020, 19;20:58	Knockdown of p21 or inhibiting APC/C by TAME sensitized NSCLC cells to 5-FU. Cells were treated with 5-FU. 2 days after treatment, surviving cells were stained with cystal violet. Representive microscopic fields were shown. The blue stained cells were counted and shown in histogram at the right side.
S2781	RITA (NSC 652287) RITA (NSC 652287)诱导DNA-蛋白质和DNA-DNA交联，检测不到DNA单链断裂，通过靶向作用于p53，也抑制MDM2-p53相互作用。	Cancer Cell,2019, 35(2):191-203 Br J Cancer,2018, 119(4):450-461 Radiol Oncol,2016, 50(2):168-74	To determine the number of viable cells, cells were serum starved for 8 hours and treated with 25 nM RITA and stimulated with 1ug/mL SDF1α for 48 hours in serum-free media. After 48 hours, cells were harvested and counted by trypan blue exclusion, using standard methods.
S8000	Tenovin-1 Tenovin-1防止MDM2介导的p53的降解，涉及泛素化途径，通过抑制SirT1和SirT2的蛋白脱乙酰活性。	J Transl Med,2019, 17(1):76 Int J Mol Med,2019, 44(3):1091-1105	The SIRT1 inhibitor (tenovin-1) partially blocked the protective effect of γ-man in L02 cells. The effect of tenovin-1 on expression and acetylation level of PGC-1α (B) in L02 cells treated with or without γ-man.
S2754	AT406 (SM-406) AT-406是一种有效的，拟Smac的IAP(通过E3泛素连接酶起作用的凋亡蛋白抑制剂)拮抗剂，与XIAP-BIR3， cIAP1-BIR3和cIAP2-BIR3结合，K_i为66.4 nM， 1.9 nM和5.1 nM，比作用于Smac AVPI肽亲和力高50到100倍。Phase 1。	Nature,2020, 577(7788):109-114 Cell Death Dis,2020, 22;11(5):391 Apoptosis,2020, 21	G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting.
S5315	PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.	Genome Res,2019, 29(10):1659-1672
S8760	Iberdomide(CC220) Iberdomide (CC-220)是一种新型口服免疫调节化合物，靶向cereblon（cereblon是CRL4CRBN E3泛素连接酶复合体的一部分），IC50为60 nM。
S7892	Avadomide(CC-122) CC-122，一种新型的多效性修饰剂化合物，在弥漫性大B细胞淋巴瘤（DLBCL）中具有抗肿瘤、免疫调节活性。其分子靶标为cereblon (CRBN)，CRBN是E3泛素化连接酶复合体CRL4^CRBN的底物受体。	Blood Adv,2019, 3(14):2105-2117

目录号	产品描述	文献引用	实验数据
S2678	NSC 207895 NSC 207895抑制MDMX，IC50为2.5 μM，促进p53稳定/激活和DNA损伤，也调节MDM2（E3连接酶）。	Genes Dev, 2020, 34(7-8):526-543 Oncol Lett, 2018, 15(2):1673-1679 Stem Cell Reports, 2016, 7(6):1140-1151	Median overall survival of mice (n = 5 mice in vehicle and PYR-41; n = 4 mice in NSC group) inoculated with IOWA-1T xenografts were increased to 43 ± 0.5 and 39 ± 2 days with PYR-41 (PYR) and NSC-207895 (NSC), respectively, compared with a vehicle-treated control group 33 ± 1 days (*p < 0.05).

目录号

产品描述

文献引用

实验数据

S2678

NSC 207895

NSC 207895抑制MDMX，IC50为2.5 μM，促进p53稳定/激活和DNA损伤，也调节MDM2（E3连接酶）。

Genes Dev, 2020, 34(7-8):526-543

Oncol Lett, 2018, 15(2):1673-1679

Stem Cell Reports, 2016, 7(6):1140-1151

目录号	产品描述	文献引用	实验数据
S1061	Nutlin-3 Nutlin-3是一种有效的，选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂，无细胞试验中IC50为90 nM；可稳定p53缺陷细胞中的p73。	Clin Cancer Res, 2020, 26(1):122-134 Cell Rep, 2020, 30(2):497-509 Eur J Cancer, 2020, 126:93-103	Ubiquitination of p53 in vivo by BIRC6 in the presence of Nutlin-3. Cells were treated with Nutlin-3 (20 uM, 24 h) before harvest. Cell lysates were immunoprecipitated with anti-p53 antibody and immunoblotted by anti-ubiquitin antibody.
S1172	JNJ-26854165 (Serdemetan) JNJ-26854165 (Serdemetan)是一种HDM2泛素连接酶拮抗剂，作用于p53野生型细胞，诱导早期凋亡，在缺乏功能性p53的细胞中，抑制细胞增殖而延迟细胞凋亡。	Cell, 2019, 36(2):179-193 Cancer Cell, 2019, 36(2):179-193 BMC Pharmacol Toxicol, 2017, 18(1):40

目录号

产品描述

文献引用

实验数据

S1061

Nutlin-3

Nutlin-3是一种有效的，选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂，无细胞试验中IC50为90 nM；可稳定p53缺陷细胞中的p73。

Clin Cancer Res, 2020, 26(1):122-134

Cell Rep, 2020, 30(2):497-509

Eur J Cancer, 2020, 126:93-103

S1172

JNJ-26854165 (Serdemetan)

JNJ-26854165 (Serdemetan)是一种HDM2泛素连接酶拮抗剂，作用于p53野生型细胞，诱导早期凋亡，在缺乏功能性p53的细胞中，抑制细胞增殖而延迟细胞凋亡。

Cell, 2019, 36(2):179-193

Cancer Cell, 2019, 36(2):179-193

BMC Pharmacol Toxicol, 2017, 18(1):40

目录号	产品描述	文献引用	实验数据
S8888^New	GMB-475 GMB-475 是一种靶向蛋白水解的嵌合体(PROTAC)，它以变构方式靶向 BCR-ABL1 蛋白并募集 the E3 ligase Von Hippel-Lindau (VHL)，从而导致泛素化并随后降解致癌融合蛋白。
S6794^New	Thalidomide-O-COOH (Cereblon ligand 3) Thalidomide-O-COOH (Cereblon ligand 3) 是基于Thalidomide的 Cereblon (CRBN) 配体，可用于募集CRBN蛋白。Thalidomide-O-COOH (Cereblon ligand 3) 可以通过连接器与蛋白质的配体连接以形成 PROTACs (Proteolysis Targeting Chimera)。

目录号

产品描述

文献引用

实验数据

S8888^New

GMB-475

GMB-475 是一种靶向蛋白水解的嵌合体(PROTAC)，它以变构方式靶向 BCR-ABL1 蛋白并募集 the E3 ligase Von Hippel-Lindau (VHL)，从而导致泛素化并随后降解致癌融合蛋白。

S6794^New

Thalidomide-O-COOH (Cereblon ligand 3)

Thalidomide-O-COOH (Cereblon ligand 3) 是基于Thalidomide的 Cereblon (CRBN) 配体，可用于募集CRBN蛋白。Thalidomide-O-COOH (Cereblon ligand 3) 可以通过连接器与蛋白质的配体连接以形成 PROTACs (Proteolysis Targeting Chimera)。

研究领域

产品类型

E3 Ligase

信号通路图

研究领域

抑制剂选择性比较

E3 Ligase 产品