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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].
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...
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].
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。

化合物

PROTAC CRBN Degrader-1
Cat.No: T18604
Synonym:
Target: Others, PROTACs
Homo-PROTAC cereblon degrader 1
Cat.No: T13721
Synonym:
Target: Others, Ligand for E3 Ligase, PROTACs
TD-165
Cat.No: T18787
Synonym:
Target: Others, Ligand for E3 Ligase, PROTACs
Desmorpholinyl Navitoclax-NH-Me
Cat.No: T39910
Synonym: Desmorpholinyl ABT-263-NH-Me,Desmorpholinyl Navitoclax-NH-Me
Target: BCL
Thalidomide 4-fluoride
Cat.No: T7755
Synonym: E3 ligase Ligand 4,2-(2,6-二氧代-哌啶-3-基)-4-氟基-异吲哚-1,3-二酮
Target: IRAK, Ligand for E3 Ligase
SD-36
Cat.No: T18680
Synonym:
Target: Others, PROTACs
PROTAC KRAS G12C degrader-1
Cat.No: T77926
Synonym:
Target: PROTACs
PROTAC Mcl1 degrader-1
Cat.No: T11975
Synonym:
Target: BCL, PROTACs
PROTAC MLKL Degrader-1
Cat.No: T79831
Synonym:
Target:
Thalidomide-C2-amido-C2-COOH
Cat.No: T18805
Synonym:
Target: Others
K-Ras ligand-Linker Conjugate 3
Cat.No: T18056
Synonym:
Target: Others
K-Ras ligand-Linker Conjugate 2
Cat.No: T18055
Synonym:
Target: Others
PROTAC IDO1 Degrader-1
Cat.No: T37329
Synonym: PROTAC IDO1 Degrader-1
Target: PROTACs
PROTAC CDK9 degrader-2
Cat.No: T17728
Synonym:
Target: Others
CDK9 Antagonist-1
Cat.No: T36744
Synonym: CDK9 Antagonist-1
Target:
K-Ras ligand-Linker Conjugate 1
Cat.No: T18054
Synonym:
Target: Others
K-Ras ligand-Linker Conjugate 5
Cat.No: T18058
Synonym:
Target: Others
K-Ras ligand-Linker Conjugate 6
Cat.No: T18059
Synonym:
Target: Others
K-Ras ligand-Linker Conjugate 4
Cat.No: T18057
Synonym:
Target: Others
LSN3106729 hydrochloride
Cat.No: T36967
Synonym:
Target:
PROTAC HSP90 degrader BP3
Cat.No: T73835
Synonym:
Target: PROTACs
PROTAC BRD2/BRD4 degrader-1
Cat.No: T18598
Synonym:
Target: Others
PROTAC BTK Degrader-5
Cat.No: T79292
Synonym:
Target: BTK
SJ988497
Cat.No: T74994
Synonym:
Target: PROTACs
PROTAC EGFR degrader 7
Cat.No: T74623
Synonym:
Target:
GBD-9
Cat.No: T79139
Synonym:
Target: PROTACs
SR-1114
Cat.No: T81108
Synonym:
Target: PROTACs
PF15
Cat.No: T74259
Synonym:
Target: PROTACs
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