Lenalidomide-Br

  Cat. No.:  DC39709   Featured
Chemical Structure
2093387-36-9
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Field of application
Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs.
Cas No.: 2093387-36-9
Chemical Name: 3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione
Synonyms: SY263571;3-(4-Bromo-1-oxoisoindolin-2-yl)piperidine-2,6-dione;Lenalidomide-Br
SMILES: BrC1=C([H])C([H])=C([H])C2C(N(C([H])([H])C=21)C1([H])C(N([H])C(C([H])([H])C1([H])[H])=O)=O)=O
Formula: C13H11BrN2O3
M.Wt: 323.142042398453
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17. [2]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
Description: Lenalidomide-Br (Compound 41) is the Lenalidomide-based ligand. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].
References: [1]. Bai L, et al. A Potent and Selective Small-Molecule Degrader of STAT3 Achieves Complete Tumor Regression In Vivo. Cancer Cell. 2019 Nov 11;36(5):498-511.e17. [2]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
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Cat. No. Product name Field of application
DC39709 Lenalidomide-Br Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs.
DC72103 CC-99282 CC-99282 (Golcadomide) is an orally active cereblon (CRBN) E3 ligase modulator (CELMoD). Ikaros and Aiolos are degraded potently and specifically by CC-99282, which co-opts CRBN.
DC42464 CRBN modulator-1 CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
DC28693 CC-90009 CC-90009 is a cereblon modulator. CC-90009 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3), which are transcriptional repressors in T-cells. This reduces the levels of these transcription factors, and modulates the activity of the immune system, which may include the activation of T-lymphocytes. .
DC11579 VH032 VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM..
DC11565 E3 Ligase Ligand 2 E3 ligase Ligand 2 is a Ligand for E3 Ligase used in PROTAC technology.
DC11588 CC-885 CC-885 (CC 885, CC885) is a novel E3 ligase cereblon (CRBN) modulator with potent anti-tumour activity mediated through the degradation of GSPT1.
DC11578 VHL Ligand 3 A VHL ligand for PROTAC..
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