dBET1
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C38H37ClN8O7S
- MW: 785.27
Description
dBET1 is a potent and selective BRD4 protein degrader. The molecule, dubbed “degronimid”, is harnessed by combining two specific high affinity protein ligands, (+)-JQ1 (Axon 1989) for BRD4 and Thalidomide (Axon 3324) for E3 ubiquitin ligase cereblon (CRBN), tethered by a linker. Fully exploiting the cells’ own protein-degrading machinery, the molecule drags the ubiquitin ligase complex into the tagged protein, leading to a fast, sustainable, CRBN-dependent and ligand-guided BRD4 degradation. It is so selective that only three proteins, BRD2, 3, 4, of >7000 within the cell, were affected. dBET1 demonstrated powerful anti-leukemia activities both in cell and in animal model, with few noticeable side effects.
More Information
| Parent CAS No. | 1799711-21-9 |
|---|---|
| Chemical Name | 2-((S,Z)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)-N-(4-(2-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yloxy)acetamido)butyl)acetamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C(NC(C[C@@H]1N=C(C2C=CC(Cl)=CC=2)C2C(C)=C(C)SC=2N2C(C)=NN=C12)=O)CCCNC(=O)COC1C=CC=C2C(=O)N(C3CCC(=O)NC3=O)C(=O)C=12 |&1:4,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C38H37ClN8O7S/c1-19-20(2)55-38-31(19)33(22-9-11-23(39)12-10-22)42-25(34-45-44-21(3)46(34)38)17-29(49)40-15-4-5-16-41-30(50)18-54-27-8-6-7-24-32(27)37(53)47(36(24)52)26-13-14-28(48)43-35(26)51/h6-12,25-26H,4-5,13-18H2,1-3H3,(H,40,49)(H,41,50)(H,43,48,51)/t25-,26?/m0/s1 |
| InChiKey | LKEGXJXRNBALBV-PMCHYTPCSA-N |
| CID | 91799313 |
| Short Description | BET degrader |
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