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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C35H37ClFN9O5S
- Molecular Weight:750.24
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
BRD4 |
In Vitro
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].
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
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Molecular Weight 750.24
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Formel C35H37ClFN9O5S
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)