Referencia número: HY-161989

DZ-837

Name: DZ-837
Brand: MedChemExpress
SKU: HY-161989
Price: 520.00 USD
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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).

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Pureza: 95.48%
No. CAS: 3105664-95-4
Fòrmula: C₄₂H₄₄FN₉O₇S
Peso molecular:837.92

Almacenamiento:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

DZ-837 Chemical Structure

No. CAS: 3105664-95-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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]. (Pink: BCL6 ligand (HY-161990); Blue: Cereblon ligand (HY-103596); Black: linker).

IC₅₀ & Target

^[1]

Cereblon

Ver todos los productos específicos de isoformas PROTACs :

Ver todos los productos específicos de isoformas PAK :

Cellular Effect

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]

In Vitro

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.

Western Blot Analysis^[1]

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.

Real Time qPCR^[1]

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 Cycle Analysis^[1]

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.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	AUC_0-∞	MRT_0-t
Rat^[1]	10 mg/kg	i.p.	3823 ng/mL	2.67 h	2.59 h	33814 ng·h/mL	33892 ng·h/mL	5.30 h
Rat^[1]	20 mg/kg	p.o.	703 ng/mL	1.00 h	1.06 h	2288 ng·h/mL	2328 ng·h/mL	2.48 h

In Vivo

DZ-837 (10-40 mg/kg; i.p.) dose-dependently inhibits SU-DHL-4 xenograft tumor growth in nude mice, reaching a maximum TGI of 71.8% at 40 mg/kg once daily, with no observed body weight loss and evidence of on-target BCL6 degradation and downstream target activation in tumor tissue^[1].

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.

Chemical Information

No. CAS 3105664-95-4
Appearance Solid
Peso molecular 837.92
Fòrmula 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
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1934 mL

5.9672 mL

11.9343 mL

5 mM

0.2387 mL

1.1934 mL

2.3869 mL

10 mM

0.1193 mL

0.5967 mL

1.1934 mL

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.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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DZ-837

Ver todos los productos específicos de isoformas PROTACs

Ver todos los productos específicos de isoformas PAK