1. PROTAC Immunology/Inflammation
  2. BCL6 PROTACs
  3. DZ-837

DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949)[1].

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DZ-837

DZ-837 Chemical Structure

CAS No. : 3105664-95-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Description

DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949)[1].

IC50 & Target

BCL6[1]

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]
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]
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]
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]
Molecular Weight

837.92

Formula

C42H44FN9O7S

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1934 mL 5.9672 mL 11.9343 mL
5 mM 0.2387 mL 1.1934 mL 2.3869 mL
View the 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.

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Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
DZ-837
Cat. No.:
HY-161989
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