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。 | |||
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。 | |||
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。 | |||
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。 | |||
T79133 |
UC-764864
|
E1/E2/E3 Enzyme | Ubiquitination |
UC-764864是一种UBE2N抑制剂,能够抑制其酶活性,并对白血病细胞中的UBE2N依赖性信号传导具有细胞毒性作用。此外,UC-764864还能阻断人AML细胞系中先天免疫和炎症相关底物的泛素化。 | |||
T69977 |
BC-1485
|
||
BC-1485 is a first-in-class inhibitor of Fibrosis-inducing E3 ligase 1 (FIEL1 ), which disrupts FIEL1-directed PIAS4 ubiquitination. | |||
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。 | |||
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]. | |||
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。 | |||
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]. | |||
T17868 |
E3 ligase Ligand 10
|
Others | Others |
E3 ligase Ligand 10 serves as a ligand for E3 ubiquitin ligase and can be conjugated to a protein ligand through a linker, resulting in the formation of PROTACs. These PROTACs act as inducers of ubiquitination-mediated degradation, specifically targeting cancer-promoting proteins[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]. | |||
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]. | |||
T78221 |
TRAF6 peptide TFA
|
E1/E2/E3 Enzyme | Ubiquitination |
TRAF6 peptide TFA是一种抑制TRAF6-p62相互作用的特异性分子,可抑制NGF依赖的TrkA泛素化,展现在阿尔茨海默症(AD)、帕金森病、ALS、创伤性脑损伤、癫痫和中风等神经系统疾病研究中的应用潜力。 | |||
T37329 |
PROTAC IDO1 Degrader-1
PROTAC IDO1 Degrader-1 |
PROTACs | PROTAC |
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... | |||
T82610 |
DA-PROTAC
|
PROTACs | PROTAC |
DA-PROTAC是Atox1和CCS铜离子转运蛋白的有效PROTAC降解剂。该化合物能够与Atox1和CCS结合形成复合体,进而与E3连接酶相结合,引起Atox1和CCS的泛素化水平增加,最终通过蛋白酶体途径导致这两种蛋白的降解。DA-PROTAC在三阴性乳腺癌的研究中有应用潜力。 | |||
T36800 |
EN219
|
||
EN219 is a synthetic recruiter of the E3 ubiquitin ligase RNF114.1It binds to cysteine 8 (C8) in the intrinsically disordered region of RNF114 (RNF114-C8; IC50= 470 nM) and inhibits RNF114-induced autoubiquitination and p21 ubiquitination in a cell-free assay when used at a concentration of 50 μM. EN219 (1 μM) also interacts with cysteine residues in the tubulin β1 chain (TUBB1), heat shock protein 60 (Hsp60), also known as Hsp family D member 1 (HspD1), and histone H3.1 (HIST1H3A) in 231MFP hum... | |||
T83667 |
A11 TFA
CPP-EYVQTVKSSKG |
||
A11是一种细胞穿透肽,由HIV-1 Tat蛋白质转导域与对应于脂联素A1 N末端第20至30残基的11氨基酸肽连接而成。它减少脂联素A1与Eph受体酪氨酸激酶A2(EphA2)的结合,并在HK1鼻咽癌(NPC)细胞中增加EphA2的泛素化。A11(10 µM)抑制HK1和5-8F NPC细胞的增殖、迁移和侵袭。在体内,A11减少5-8F和HK1 NPC小鼠异种移植模型中的肿瘤体积。 | |||
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。 |