E3 Ligase
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S1193 | Thalidomide | <1 mg/mL | 51 mg/mL | 2 mg/mL |
| S2225 | TAME | 69 mg/mL | 69 mg/mL | 3 mg/mL |
| S5315 | PRT4165 | <1 mg/mL | 11 mg/mL | 4 mg/mL |
| S2781 | RITA (NSC 652287) | <1 mg/mL | 58 mg/mL | 8 mg/mL |
| S8000 | Tenovin-1 | <1 mg/mL | 74 mg/mL | <1 mg/mL |
| S2754 | AT406 (SM-406) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7892 | Avadomide(CC-122) | <1 mg/mL | 57 mg/mL | 1 mg/mL |
| S2678 | NSC 207895 | <1 mg/mL | 0.4 mg/mL | <1 mg/mL |
| S1061 | Nutlin-3 | <1 mg/mL | 100 mg/mL | 30 mg/mL |
| S1172 | JNJ-26854165 (Serdemetan) | <1 mg/mL | 66 mg/mL | 2 mg/mL |
- E3 Ligase 抑制剂（10）
- 新E3 Ligase 产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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.
|
|
| 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.
|
|
| S5315New |
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. |
||
| 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.
|
|
| S8000 |
Tenovin-1Tenovin-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。 |
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，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. |
|
| 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CRL4CRBN的底物受体。 |
||
| S2678 |
NSC 207895NSC 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）。 |
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-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。 |
Caspase 3/7 activation in UKF-NB-3 or UKF-NB-3rNutlin10 μM cells treated nutlin-3 (10 μM), VCR (10 ng/ml), DOX (20 ng/ml), or CDDP (1000 ng/ml). |
|
| 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。 |
|
-J-Immunol-20170125.gif)
