DZ-837
Based on 1 Customer Validation
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.
(Pink: BCL6 ligand (HY-161990); Blue: Cereblon ligand (HY-103596); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 95.48%
- CAS 番号: 3105664-95-4
- 分子式: C42H44FN9O7S
- 分子量:837.92
-
保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
|
Cereblon |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| DOHH-2 | IC50 |
56.2 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human DOHH-2 cells assessed as inhibition in cell growth measured after 6 days by MTS assay
Antiproliferative activity against BCL6-dependent human DOHH-2 cells assessed as inhibition in cell growth measured after 6 days by MTS assay
|
[PMID: 39208743] |
| HEK-293T | IC50 |
>10000 nM
Compound: 3d; DZ-837
|
Cytotoxicity against HEK293T cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Cytotoxicity against HEK293T cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| OCI-Ly1 | IC50 |
1370 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human OCI-Ly1 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Antiproliferative activity against BCL6-dependent human OCI-Ly1 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| SUD4 | IC50 |
399 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human SU-DHL-4 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Antiproliferative activity against BCL6-dependent human SU-DHL-4 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| SU-DHL-6 | IC50 |
450.9 nM
Compound: 3d; DZ-837
|
Antiproliferative activity against BCL6-dependent human SU-DHL-6 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Antiproliferative activity against BCL6-dependent human SU-DHL-6 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
| WI-38 VA13 | IC50 |
>10000 nM
Compound: 3d; DZ-837
|
Cytotoxicity against human WI-38 VA13 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
Cytotoxicity against human WI-38 VA13 cells assessed as inhibition in cell growth measured after 6 days by MTT assay
|
[PMID: 39208743] |
DZ-837 (20 nM-10 μM; 48 h) potently degrades BCL6 protein in SU-DHL-4 diffuse large B-cell lymphoma (DLBCL) cells, with a DC50 of 676.1 nM and a maximum degradation rate of 93.0%[1].
DZ-837 (20 nM-10 μM; 48 h) potently degrades BCL6 protein in DOHH2 diffuse large B-cell lymphoma (DLBCL) cells, with a DC50 of 557.7 nM and a maximum degradation rate of 93.7%[1].
DZ-837 (10 μM; 48 h) reactivates BCL6 downstream genes CDKN1A and CDKN1B in SU-DHL-4 diffuse large B-cell lymphoma (DLBCL) cells without altering the mRNA level of BCL6[1].
DZ-837 (0.1-10 μM; 48 h, 12-72 h) induces sustained reduction of BCL6 protein and upregulates p21 and p27 proteins in a time- and concentration-dependent manner in SU-DHL-4 diffuse large B-cell lymphoma (DLBCL) cells[1].
DZ-837 exhibits synergistic antiproliferative effects with Ibrutinib (HY-10997) in DLBCL cells[1].
DZ-837 induces BCL6 degradation with a DC50 of approximately 600 nM, and potently inhibits the proliferation of various diffuse large B-cell lymphoma cell lines[3].
DZ-837 (0.1-10 μM; 72 h) induces dose-dependent G1 phase arrest in SU-DHL-4 diffuse large B-cell lymphoma (DLBCL) cells, with 93.3% of cells arrested in the G1 phase after treatment with 10 μM for 72 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:DOHH2 diffuse large B-cell lymphoma (DLBCL) cells
-
Concentration:20-10000 nM
-
Incubation Time:48 h
-
Result:Induced dose-dependent BCL6 degradation with a DC50 of 557.7 nM and a maximum degradation (D_max) of 93.7% after 48 hours of treatment.
-
Cell Line:SU-DHL-4 DLBCL cells
-
Concentration:10 μM
-
Incubation Time:48 h
-
Result:Did not alter BCL6 mRNA levels, but significantly upregulated mRNA levels of BCL6-repressed target genes CDKN1A (p21) and CDKN1B (p27) by approximately 3-fold and 2-fold, respectively.
-
Cell Line:SU-DHL-4 DLBCL cells
-
Concentration:0.1-10 μM
-
Incubation Time:72 h
-
Result:Induced dose-dependent G1 phase arrest: compared to 61.4% of cells in G1 phase in the control group, 86.7% and 93.3% of cells were in G1 phase after treatment with 1 μM and 10 μM DZ-837, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:nu/nu (female, 6 weeks old, subcutaneous xenograft of SU-DHL-4 cells)[1]
-
Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
-
Administration:i.p.
-
Result:Achieved tumor growth inhibition (TGI) of 22.2% at 10 mg/kg, 47.4% (P < 0.05) at 20 mg/kg, and 71.8% (P < 0.01) at 40 mg/kg.
Caused no significant mouse body weight loss during treatment.
Downregulated BCL6 protein levels and significantly increased p21 and p27 protein levels in tumor tissue from the 40 mg/kg group on average.
化学情報
-
CAS 番号 3105664-95-4
-
性状 Solid
-
分子量 837.92
-
分子式 C42H44FN9O7S
-
Color Light yellow to yellow
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 25 mg/mL (29.84 mM; ultrasonic and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
取扱説明書 (2659 KB)
参考文献
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1934 mL | 5.9672 mL | 11.9343 mL | 29.8358 mL |
| 5 mM | 0.2387 mL | 1.1934 mL | 2.3869 mL | 5.9672 mL | |
| 10 mM | 0.1193 mL | 0.5967 mL | 1.1934 mL | 2.9836 mL | |
| 15 mM | 0.0796 mL | 0.3978 mL | 0.7956 mL | 1.9891 mL | |
| 20 mM | 0.0597 mL | 0.2984 mL | 0.5967 mL | 1.4918 mL | |
| 25 mM | 0.0477 mL | 0.2387 mL | 0.4774 mL | 1.1934 mL |
DZ-837 関連分類
HY-161989 関連分類
Powered by Bioz