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Cat. No.: HY-180886

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ZD-1-186

ZD-1-186 is a non-degradative, covalent-dependent molecular glue that targets BCL6 and BRD9. ZD-1-186 inhibits the transcriptional output of MYC, relieves the repression of canonical BCL6 target loci (including CDKN1A (p21)), and mediates the selective recruitment of BRD9 to BCL6. ZD-1-186 can be used for research on diffuse large B-cell lymphoma.

For research use only. We do not sell to patients.

Formula: C₃₅H₃₇ClFN₉O₅S
Molecular Weight:750.24

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

ZD-1-186 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

BRD4

All Epigenetic Reader Domain Isoforms :

In Vitro

Anti-cancerCell Cycle RegulationOthers

Anti-cancer

Cell Cycle Regulation

ZD-1-186 (50 μM; 24 h) potently inhibits MYC mRNA and protein levels, and induces the protein level of CDKN1A (p21) in HT diffuse large B-cell lymphoma cells, with minimal effects on cell viability at the tested concentration^[1].
ZD-1-186 (50 μM; 24 h) inhibits MYC protein levels and induces increased CDKN1A (p21) and BIM protein levels in SU-DHL-4 diffuse large B-cell lymphoma cells^[1].
The MYC inhibition and CDKN1A (p21) induction mediated by ZD-1-186 (50 μM; 24 h) are attenuated in a dose-dependent manner by pharmacological inhibition of BRD9 with BI-9564 in HT diffuse large B-cell lymphoma cells^[1].
The inhibitory effect of ZD-1-186 (50 μM; 24 h) on MYC in HT diffuse large B-cell lymphoma cells is attenuated by BRD9 knockout, whereas BRD9 knockout alone does not reduce MYC levels^[1].
ZD-1-186 (50 μM; 24 h) simultaneously relieves the repression of the canonical BCL6 inhibitory site and suppresses MYC-driven transcriptional programs in HT diffuse large B-cell lymphoma cells^[1].

Others

ZD-1-186 (50 μM; 24 h) induces selective proximity binding between BCL6 and BRD9 in HEK293T cells^[1].
ZD-1-186 covalently binds to the C288 residue of BRD9, and competitively inhibits the labeling of BRD9 by cysteine-reactive probes in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

Molecular Weight 750.24
Formula C₃₅H₃₇ClFN₉O₅S
SMILES

CNC(COC1=CC2=C(N(C)C1=O)C=CC(NC3=C(C=NC(N4CCN(C(/C=C/C(NC5=CC=C(C(F)=C5)N6CCSCC6)=O)=O)CC4)=N3)Cl)=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 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)
Handling Instructions (2659 KB)

References

[1]. Duong T N, et al. Discovery of non-degradative covalent molecular glues for transcriptional reprogramming[J]. bioRxiv, 2025.

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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.

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Biological Activity
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- In Vitro
Chemical Information
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References

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ZD-1-186

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Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ZD-1-186 Related Classifications

HY-180886 Related Classifications

Bioz

Keywords

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