1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. CS-1-69

CS-1-69 is an MBD2 ligand analog that does not bind to individual NuRD components MBD2 or HDAC1, but binds robustly to the assembled NuRD complex (MBD2, HDAC1, and MT1A) in a dose-responsive manner. CS-1-69 attenuates Transcriptional Repression via Active Chemical Epigenetic Reprogrammin (TRACER)-mediated strogen receptor (ER) inhibitory activity.

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CS-1-69

CS-1-69 Chemical Structure

CAS No. : 315702-79-5

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Description

CS-1-69 is an MBD2 ligand analog that does not bind to individual NuRD components MBD2 or HDAC1, but binds robustly to the assembled NuRD complex (MBD2, HDAC1, and MT1A) in a dose-responsive manner. CS-1-69 attenuates Transcriptional Repression via Active Chemical Epigenetic Reprogrammin (TRACER)-mediated strogen receptor (ER) inhibitory activity[1].

Cellular Effect
Cell Line Type Value Description References
HeLa EC50
<1.2 μM
Compound: 21
Inhibition of VCP in human HeLa cells assessed as stabilization of ubiquitin-tagged luciferase after 24 hrs by reporter gene assay
Inhibition of VCP in human HeLa cells assessed as stabilization of ubiquitin-tagged luciferase after 24 hrs by reporter gene assay
[PMID: 20137940]
RCC4 GI50
36 μM
Compound: 79
Growth inhibition of VHL-null human RCC4 cells after 4 days by XTT assay
Growth inhibition of VHL-null human RCC4 cells after 4 days by XTT assay
[PMID: 19994864]
In Vitro

CS-1-69 (0-150 μM; 1 h) binds specifically to the assembled NuRD complex of purified MBD2, HDAC1, and MT1A proteins in a dose-responsive manner, with no binding to isolated MBD2 or HDAC1[1].
CS-1-69 (25 μM; 24 h) blocks CS-1-103-mediated inhibition of ER transcriptional activity in T47D breast cancer cells, confirming CS-1-103 acts via recruitment of MBD2[1].

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

Molecular Weight

269.32

Formula

C14H11N3OS

CAS No.
SMILES

OC1=CC=C(NC2=NC(C3=NC=CC=C3)=CS2)C=C1

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Purity & Documentation
References
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    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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CS-1-69
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HY-128562
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