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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- CAS No.: 315702-79-5
- 화학식: C14H11N3OS
- 분자량:269.32
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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] |
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.
Chemical Information
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CAS No. 315702-79-5
-
분자량 269.32
-
화학식 C14H11N3OS
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SMILES
OC1=CC=C(NC2=NC(C3=NC=CC=C3)=CS2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)