Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T18604 |
PROTAC CRBN Degrader-1
|
Others; PROTACs | Others; PROTAC |
PROTAC CRBN Degrader-1 is a chemical compound consisting of a cereblon (CRBN) ligand binding group, a linker, and a von Hippel-Landau (VHL) binding group. It functions as a cereblon (CRBN) degrader[1]. | |||
T13721 |
Homo-PROTAC cereblon degrader 1
|
Others; Ligand for E3 Ligase; 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。 | |||
T18787 |
TD-165
|
Others; Ligand for E3 Ligase; PROTACs | Others; PROTAC |
TD-165 是一种基于 PROTAC 技术的 CRBN 降解剂。它包括一个 CRBN 配体结合基团,一个 linker 和一个 VHL 结合基团。 | |||
T39910 |
Desmorpholinyl Navitoclax-NH-Me
Desmorpholinyl ABT-263-NH-Me,Desmorpholinyl Navitoclax-NH-Me |
BCL | Apoptosis |
Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2]. | |||
T7755 |
Thalidomide 4-fluoride
E3 ligase Ligand 4,2-(2,6-二氧代-哌啶-3-基)-4-氟基-异吲哚-1,3-二酮 |
IRAK; Ligand for E3 Ligase | Immunology/Inflammation; NF-κB; PROTAC |
Thalidomide 4-fluoride (E3 ligase Ligand 4) 是一种基于 Thalidomide 的 Cereblon 配体,可用于募集 CRBN 蛋白。它能够利用 linker 与 IRAK4 靶蛋白配体连接,得到 PROTAC IRAK4 degrader-1。 | |||
T18680 |
SD-36
|
Others; PROTACs | Others; PROTAC |
SD-36, a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), exhibits high specificity for STAT3 over other STAT members. It effectively targets both wild-type and mutated STAT3 proteins in cells, inhibiting their transcriptional activity (IC50=10 nM). The compound, consisting of the STAT3 inhibitor SI-109, a linker, and a CRBN ligand Lenalidomide analog for E3 ubiquitin ligase[1], demonstrates significant anti-tumor effects and achieves complete, long-lasting tumor regression in mouse mod... | |||
T77926 |
PROTAC KRAS G12C degrader-1
|
PROTACs | PROTAC |
PROTACKRAS G12C degrader-1是基于Cereblon的KRASG12C PROTAC降解剂,能诱导CRBN/KRASG12C二聚化,并在报告细胞中降解GFP-KRASG12C。 | |||
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. | |||
T79831 |
PROTAC MLKL Degrader-1
|
||
PROTACMLKL Degrader-1 (Compound 36) 为MLKL的PROTAC靶向降解剂,具有超过90%的Dmax效率。该化合物构成包含了修饰后的CRBN配体、linker 及 Lenalidomide 接头片段,能有效消除TSZ坏死模型中的细胞死亡。 | |||
T18805 | Thalidomide-C2-amido-C2-COOH | Others | Others |
Thalidomide-C2-amido-C2-COOH is a compound that includes a CRBN ligand for the E3 ubiquitin ligase, as well as a linker. It is utilized in the development of PROTAC CDK2/9 Degrader-1[1]. | |||
T18056 |
K-Ras ligand-Linker Conjugate 3
|
Others | Others |
K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound that consists of a ligand for K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential in the synthesis of PROTAC K-Ras Degrader-1, a potent PROTAC K-Ras degrader that demonstrates a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T18055 |
K-Ras ligand-Linker Conjugate 2
|
Others | Others |
K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker. This compound is capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC K-Ras Degrader-1, which is a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T17728 |
PROTAC CDK9 degrader-2
|
Others | Others |
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. | |||
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... | |||
T36744 |
CDK9 Antagonist-1
CDK9 Antagonist-1 |
||
CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381. | |||
T18054 |
K-Ras ligand-Linker Conjugate 1
|
Others | Others |
K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1]. | |||
T18058 |
K-Ras ligand-Linker Conjugate 5
|
Others | Others |
K-Ras ligand-Linker Conjugate 5 is a chemical compound that combines a ligand for the K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The K-Ras ligand-Linker Conjugate 5 plays a crucial role in the synthesis of PROTAC K-Ras Degrader-1, a highly potent K-Ras degrader. In SW1573 cells, this degrader exhibits an impressive degradation efficacy of ≥70% [1]. | |||
T18059 |
K-Ras ligand-Linker Conjugate 6
|
Others | Others |
K-Ras ligand-Linker Conjugate 6 is a chemical compound that combines a ligand for K-Ras recruiting moiety and a PROTAC linker. This compound can recruit E3 ligases, including VHL, CRBN, MDM2, and IAP. K-Ras ligand-Linker Conjugate 6 is particularly useful in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1]. | |||
T18057 |
K-Ras ligand-Linker Conjugate 4
|
Others | Others |
K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1]. | |||
T36967 |
LSN3106729 hydrochloride
|
||
LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods o... | |||
T73835 |
PROTAC HSP90 degrader BP3
|
PROTACs | PROTAC |
PROTACHSP90 degrader BP3 以 CRBN 依赖性方式有效且选择性地降解 HSP90。PROTACHSP90 degrader BP3对 MCF-7 细胞中的 HSP90蛋白有一定的降解作用 (DC50=0.99 µM)。PROTACHSP90 degrader BP3 抑制乳腺癌细胞的生长。 | |||
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]. | |||
T79292 |
PROTAC BTK Degrader-5
|
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
PROTACBTK Degrader-5 (compound 3e) 是一种BTK选择性降解剂,其在JeKo-1细胞中的DC50为7.0 nM。该化合物对CRBN新基态显示出无脱靶活性,且对淋巴瘤细胞表现出抗增殖效果,适用于恶性淋巴瘤的研究1。 | |||
T74994 |
SJ988497
|
PROTACs | PROTAC |
SJ988497是一种PROTACJAK2降解剂,有效地抑制CRLF2重排(CRLF2r)细胞增殖并降解CRBN新底物GSPT1。该化合物由Ruxolitinib衍生物、连接子以及CRBN配体Pomalidomide构成,可作为急性淋巴细胞白血病(ALL)研究用途。 | |||
T74623 |
PROTAC EGFR degrader 7
|
||
PROTACEGFRdegrader 7 (compound 13b) 是一种有效的、选择性 CRBN 招募的 PROTACEGFRL858R/T790M 降解剂,其 DC50为 13.2 nM。PROTACEGFRdegrader 7 抑制 NCI-H1975 细胞增殖,IC50为 46.82 nM。PROTACEGFRdegrader 7 显著诱导 NCI-H1975 细胞凋亡 (apoptosis) 和 G2/M 期阻滞。PROTACEGFRdegrader 7 具有抗肿瘤活性,可用于非小细胞肺癌 (NSCLC) 研究。 | |||
T79139 |
GBD-9
|
PROTACs | PROTAC |
GBD-9,一种双机制降解剂,有效通过E3 连接酶cereblon(CRBN)招募来降解BTK与GSPT1。作为PROTAC分子,GBD-9诱导BTK降解,同时亦作为分子胶(molecular glue)针对GSPT1。该化合物能有效抑制癌细胞生长。 | |||
T81108 |
SR-1114
|
PROTACs | PROTAC |
SR-1114 是一种创新的PROTACENL降解剂,能够在MV4;11、MOLM-13和OCI/AML-2细胞中迅速降解ENL,其DC50值分别为150 nM 、311 nM 和1.65 μM。 | |||
T74259 | PF15 | PROTACs | PROTAC |
PF15是一种将FLT3 kinase配体与CRBN配体结合的PROTAC,它是FLT3-ITD的高选择性降解剂,显示出76.7 nM的DC50。该化合物能有效抑制FLT3-ITD阳性细胞增殖,并降低FLT3和STAT5的磷酸化水平。在小鼠模型中,PF15也能够抑制肿瘤生长,对白血病研究具有潜在应用价值。 |