2140289-17-2
Chemical Structure
BETd-246
- CAS No.: 2140289-17-2
- Formula:C48H55N11O10
- Molecular Weight:946.02
IUPAC Name: 4-((3-cyclopropyl-1-ethyl-1H-pyrazol-5-yl)amino)-7-(3,5-dimethylisoxazol-4-yl)-N-(3-(2-(2-(3-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)propoxy)ethoxy)ethoxy)propyl)-6-methoxy-9H-pyrimido[4,5-b]indole-2-carboxamide
InChIKey: XEJMFVWHCPNMRS-UHFFFAOYSA-N
SMILES: O=C(C1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1)NCCCOCCOCCOCCCNC7=CC=CC(C(N8C(CC9)C(NC9=O)=O)=O)=C7C8=O
Biological Activity: BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BETd-246 | 98.34% | BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia. | ||||||||||||||||||||
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Similarity Score 0.82
HY-103633PROTAC BET Degrader-1 -
Similarity Score 0.78
HY-101519BETd-260 -
Similarity Score 0.77
HY-114228PROTAC BET degrader-2 -
Similarity Score 0.66
HY-114229PROTAC BET degrader-3 -
Similarity Score 0.60
HY-112429HJB97 -
Similarity Score 0.59
HY-181084PROTAC BCL6/GSPT1 Degrader-1 -
Similarity Score 0.58
HY-W591307P13I -
Similarity Score 0.58
HY-130645iRucaparib-TP3 -
Similarity Score 0.58
HY-107451PROTAC BET-binding moiety 1 -
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References
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[1]. Bai L, et al. Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer. Cancer Res. 2017 May 1;77(9):2476-2487.
[Content Brief] - [2]. Ge H, et al. The BET degrader BETd-246 demonstrated significant anti-tumor efficacy in T-cell acute lymphoblastic leukemia by inhibiting TRAT1. Experimental cell research. 2025 Dec 01;453(2):114791. [Content Brief]
