Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T82745 |
Cereblon inhibitor 1
|
Others | Others |
Cereblon inhibitor1,一种异吲哚啉衍生的分子,作为cereblon E3 泛素连接酶的调节剂,展现了在癌症研究中的应用潜力。 | |||
T13721 |
Homo-PROTAC cereblon degrader 1
|
Others; PROTACs | Others; PROTAC |
Homo-PROTAC cereblon degrader 1 (compound 15a) 是一种高效 cereblon 降解剂,对 IKZF1 和 IKZF3 的影响很小。 | |||
T10765 |
Eragidomide
CC-90009,Cereblon modulator 1 |
Apoptosis; Ligand for E3 Ligase; Molecular Glues | Apoptosis; PROTAC |
Cereblon modulator 1 是一种 GSPT1 选择性cereblon (CRBN)E3 连接酶调节剂,以分子胶的方式作用。它通过 CRL4CRBN选择性靶向 GSPT1 进行泛素化和蛋白酶体降解。 | |||
T17325 |
Pomalidomide-PEG4-C-COOH
Cereblon Ligand -Linker Conjugates 1,E3 Ligase Ligand-Linker Conjugates 1 |
Others; E3 Ligase Ligand-Linker Conjugate | Others; PROTAC |
Pomalidomide-PEG4-C-COOH (E3 Ligase Ligand-Linker Conjugates 1) 包含基于 Pomalidomide 的 cereblon 配体和 4 个单元 PEG linker,是一种合成的 E3 连接酶配体-linker 偶联物。 | |||
T36243 |
PROTAC RIPK degrader-6
|
PROTACs | PROTAC |
PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker to a cereblon binder[1]. | |||
T11975 |
PROTAC Mcl1 degrader-1
|
BCL; PROTACs | Apoptosis; PROTAC |
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. | |||
T84904 |
Thalidomide-Piperazine 5-fluoride hydrochloride
UUN-14238,Pomalidomide 5'-fluoro-6'-piperazine,UUN14238,UUN 14238 |
Others | Others |
Thalidomide-Piperazine 5-fluoride hydrochloride,作为Thalidomide衍生物,是一种cereblon(CRBN)抑制剂,用作E3 泛素连接酶的配体(Ligands for E3 Ligase),适用于PROTACs合成。 | |||
T18641 |
SirReal1-O-propargyl
PROTAC Sirt2-binding moiety 1 |
Others | Others |
SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2[1]. | |||
T16667 |
PROTAC Sirt2 Degrader-1
|
Sirtuin; PROTACs | Chromatin/Epigenetic; DNA Damage/DNA Repair; PROTAC |
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1]. | |||
T18601 |
Desmethyl-QCA276
PROTAC BRD4-binding moiety 4 |
Others | Others |
Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1]. | |||
T84709 |
PRO-6E
|
Others | Others |
PRO-6E是一种基于Cereblon配体的口服活性PROTAC,能在1 μM浓度下使MKN-45细胞中MET的降解率达到81.9%。该化合物有效地在体内外抑制肿瘤生长,并能诱导细胞凋亡(apoptosis)及细胞周期阻滞(结构备注:(Blue:Cereblon配体, Black: linker;Pink: ALK/c-Met抑制剂Crizotinib)。 | |||
T18598 |
PROTAC BRD2/BRD4 degrader-1
|
Others | Others |
PROTAC BRD2/BRD4 degrader-1 (compound 15) serves as a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination of BRD4 and BRD2 compared to BRD3. Its efficacy in suppressing solid tumors manifest with minimal cytotoxic effects. This compound comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN)/cullin 4A[1]. | |||
T73909 |
Abemaciclib metabolite M18
LSN3106729 |
Ligands for Target Protein for PROTAC | PROTAC |
Abemaciclibmetabolite M18 (LSN3106729) 是一种CDK抑制剂,具有抗肿瘤活性。作为Abemaciclib的代谢物,Abemaciclibmetabolite M18 能与CRBN配体结合,用于设计PROTAC CDK4/6降解剂。 | |||
T79230 |
JET-209
|
PROTACs | PROTAC |
JET-209为高效PROTAC CBP/p300降解剂,DC50分别为CBP和p300的0.05 nM与0.2 nM。该化合物融合了Lenalidomide (cereblon配体)、连接子以及GNE-207 (溴结构域抑制剂)。JET-209主要应用于癌症研究领域。 | |||
T83857 |
Soluble Epoxide Hydrolase PROTAC 1a
sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a |
Others | Others |
Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术,通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解,特异性抑制sEH的水解酶活性(IC50 = 0.8 nM),相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解,并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接,表明能减少ER应激。 | |||
T83889 |
C-02
|
Others | Others |
C-02是一种由巨噬细胞抑制剂Lonidamine和Cereblon配体Thalidomide组成的蛋白酶体靶向嵌合体(PROTAC)。在20 µM浓度下使用时,可诱导786-O和PANC-1细胞中的Hexokinase 2降解。C-02对786-O、4T1、PANC-1、HGC-27和MCF-7癌细胞具有细胞毒性(IC50分别为34.07、5.08、31.53、6.11和21.65 µM)。同时,20 µM浓度下减少4T1细胞的细胞外酸化率(ECAR)和氧气消耗率(OCR),表明其抑制糖酵解和引起线粒体损伤。在体内,C-02(50 mg/kg)能减少4T1小鼠乳腺癌模型的肿瘤体积,并诱导肿瘤内细胞因子积累和细胞焦亡。 |