66
3
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。 | |||
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。 | |||
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。 | |||
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. | |||
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. | |||
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. | |||
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]. | |||
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]. | |||
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. | |||
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。 |
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。 |