E3 Ligase
E3 Ligase 产品
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。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。 |
![]() ![]()
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. |
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S1567 |
PomalidomidePomalidomide (CC-4047)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。 |
![]() ![]() 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.
|
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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)。 |
![]() ![]() (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.
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S8449New |
VH298VH298 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。 |
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S8979New |
THAL-SNS-032THAL-SNS-032 是一种选择性的 Cyclin-dependent kinase 9 (CDK9) 的降解剂PROTAC,包含一个与CDK结合的SNS-032配体、一个thalidomide衍生物和 E3 ubiquitin ligase Cereblon (CRBN)相结合。 |
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S9605New |
ApcinApcin (APC inhibitor) 是一种有丝分裂的 anaphase-promoting complex/cyclosome (APC/C) 的E3连接酶活性的抑制剂,其可与Cdc20结合并竞争性地抑制含D-box底物的泛素化。 |
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S0095New |
VL285VL285 是一种有效的 VHL ligand 对应的IC50值为0.34 μM,可降解HaloTag7融合蛋白。HaloPROTAC3 衍生自 VL285。 |
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S0097New |
(S,R,S)-AHPC (MDK7526)(S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1)是一种 VH032-based VHL ligand,可用于募集 von Hippel-Lindau (VHL)蛋白。(S,R,S)-AHPC 可能对 androgen receptor 的靶向降解有用。(S,R,S)-AHPC 可以通过接头与蛋白质的配体例如BCR-ABL1连接,以形成PROTAC例如GMB-475。GMB-475 可在 Ba/F3 细胞中诱导BCR-ABL1降解,IC50值为1.11 μM。 |
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S2225 |
TAMETAME是一种APC抑制剂。 |
![]() ![]() 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.
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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。 |
![]() ![]() 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.
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S2754 |
AT406 (SM-406)AT406 (SM-406, ARRY-334543, Debio1143) 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,Ki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。 |
![]() ![]() G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting. |
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S5315 |
PRT4165PRT4165 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. |
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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。Iberdomide (CC-220) 可诱导凋亡并具有抗肿瘤和免疫刺激的活性。 |
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S7892 |
Avadomide (CC-122)Avadomide (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CRL4CRBN的底物受体。 |
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S8652 |
Skp2 inhibitor C1 (SKPin C1)Skp2 inhibitor C1 (SKPin C1)是一种高选择性的Skp2-mediated p27 degradation小分子抑制剂。 |
||
S2678 |
NSC 207895NSC 207895 (XI-006) 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)。 |
![]() ![]() 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).
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S1061 |
Nutlin-3Nutlin-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。 |
![]() ![]() 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.
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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。 |
![]() ![]() |
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S8975New |
CC-92480CC-92480 是一种新型蛋白降解剂,是一种 cereblon E3 ligase 调节剂(CELMoD),并具有抗骨髓瘤活性。 |
||
S8888New |
GMB-475GMB-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。 |
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S6794New |
Thalidomide-O-COOH (Cereblon ligand 3)Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase 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。Lenalidomide 可促进 cleaved caspase-3 的表达、抑制 VEGF 的表达并诱导凋亡。 |
![]() ![]()
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 |
PomalidomidePomalidomide (CC-4047)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。 |
![]() ![]() 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)。 |
![]() ![]() (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.
|
|
S8449New |
VH298VH298 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。 |
||
S8979New |
THAL-SNS-032THAL-SNS-032 是一种选择性的 Cyclin-dependent kinase 9 (CDK9) 的降解剂PROTAC,包含一个与CDK结合的SNS-032配体、一个thalidomide衍生物和 E3 ubiquitin ligase Cereblon (CRBN)相结合。 |
||
S9605New |
ApcinApcin (APC inhibitor) 是一种有丝分裂的 anaphase-promoting complex/cyclosome (APC/C) 的E3连接酶活性的抑制剂,其可与Cdc20结合并竞争性地抑制含D-box底物的泛素化。 |
||
S0095New |
VL285VL285 是一种有效的 VHL ligand 对应的IC50值为0.34 μM,可降解HaloTag7融合蛋白。HaloPROTAC3 衍生自 VL285。 |
||
S0097New |
(S,R,S)-AHPC (MDK7526)(S,R,S)-AHPC (MDK7526, VH032-NH2, VHL ligand 1)是一种 VH032-based VHL ligand,可用于募集 von Hippel-Lindau (VHL)蛋白。(S,R,S)-AHPC 可能对 androgen receptor 的靶向降解有用。(S,R,S)-AHPC 可以通过接头与蛋白质的配体例如BCR-ABL1连接,以形成PROTAC例如GMB-475。GMB-475 可在 Ba/F3 细胞中诱导BCR-ABL1降解,IC50值为1.11 μM。 |
||
S2225 |
TAMETAME是一种APC抑制剂。 |
![]() ![]() 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。 |
![]() ![]() 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.
|
|
S2754 |
AT406 (SM-406)AT406 (SM-406, ARRY-334543, Debio1143) 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,Ki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。 |
![]() ![]() G, cells treated with the SM406 (1 μmol/L) for 48 hours were subjected to Western blotting. |
|
S5315 |
PRT4165PRT4165 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. |
||
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。Iberdomide (CC-220) 可诱导凋亡并具有抗肿瘤和免疫刺激的活性。 |
||
S7892 |
Avadomide (CC-122)Avadomide (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CRL4CRBN的底物受体。 |
||
S8652 |
Skp2 inhibitor C1 (SKPin C1)Skp2 inhibitor C1 (SKPin C1)是一种高选择性的Skp2-mediated p27 degradation小分子抑制剂。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S2678 |
NSC 207895NSC 207895 (XI-006) 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)。 |
![]() ![]() 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 |
---|---|---|---|
S1061 |
Nutlin-3Nutlin-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。 |
![]() ![]() 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。 |
![]() ![]() |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8975New |
CC-92480CC-92480 是一种新型蛋白降解剂,是一种 cereblon E3 ligase 调节剂(CELMoD),并具有抗骨髓瘤活性。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S8888New |
GMB-475GMB-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。 |
||
S6794New |
Thalidomide-O-COOH (Cereblon ligand 3)Thalidomide-O-COOH (Cereblon ligand 3, E3 ligase 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)。 |