3105664-95-4
Chemical Structure
DZ-837
- CAS No.: 3105664-95-4
- Formula:C42H44FN9O7S
- Molecular Weight:837.92
InChIKey: LLKJUUPYYLCBPC-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(C2=CCCC2)S1)NC3=CC=C(NC4=NC(N5CCN(CCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)CC5)=NC=C4F)C=C3OC
Biological Activity: DZ-837 is a BCL6 PROTAC degrader with a DC50 of 557.7 nM. DZ-837 induces BCL6 ubiquitination and degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. DZ-837 activates CDKN1A and CDKN1B, the downstream genes of BCL6. DZ-837 upregulates p21 and p27 proteins. DZ-837 inhibits tumor growth in a diffuse large B-cell lymphoma xenograft mouse model. DZ-837 exerts synergistic antiproliferative effects when combined with Ibrutinib (HY-10997). DZ-837 can be used in studies related to diffuse large B-cell lymphoma[1][2][3].
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DZ-837 | 95.48% | DZ-837 is a BCL6 PROTAC degrader with a DC50 of 557.7 nM. DZ-837 induces BCL6 ubiquitination and degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. DZ-837 activates CDKN1A and CDKN1B, the downstream genes of BCL6. DZ-837 upregulates p21 and p27 proteins. DZ-837 inhibits tumor growth in a diffuse large B-cell lymphoma xenograft mouse model. DZ-837 exerts synergistic antiproliferative effects when combined with Ibrutinib (HY-10997). DZ-837 can be used in studies related to diffuse large B-cell lymphoma. | ||||||||||||||||||||
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- [1]. Mi D, et al. Discovery of novel BCL6-Targeting PROTACs with effective antitumor activities against DLBCL in vitro and in vivo. European journal of medicinal chemistry. 2024 Nov 05;277:116789. [Content Brief]
- [2]. Kraaijeveld R, et al. BCL6 inhibition: a promising approach to prevent germinal center-driven allo-immune responses. Frontiers in immunology. 2025;16:1667185. [Content Brief]
- [3]. Yu X, et al. Discovery of a Selective and Potent BCL6 PROTAC with Efficacious Antiproliferative Activity for the Treatment of Diffuse Large B-Cell Lymphoma. Journal of medicinal chemistry. 2025 Oct 09;68(19):20180-20206. [Content Brief]
Keywords