PBRM1-BD2-IN-1
PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitory activity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer.
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- CAS No.: 1915012-21-3
- Formule: C17H19ClN2O
- Masse moléculaire:302.80
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
Kd: 0.7 μM (PBRM1-BD2), 0.35 μM (PBRM1-BD5), 8.1 μM (SMARCA2B), 5.0 μM (SMARCA4) [1].
IC50: 0.2 μM (PBRM1-BD2)[1].
In Vitro
PBRM1-BD2-IN-1 (0, 0.1, 1, and 10 μM; 5 days) selectively inhibit growth of a PBRM1-dependent prostate cancer cell line[1].
PBRM1-BD2-IN-1 has binding affinity for PBRM1-BD2, PBRM1-BD5, SMARCA2B amd SMARCA4 with Kd values of 0.7 μM, 0.35 μM, 8.1 μM and 5.0 μM, respectively[1].
PBRM1-BD2-IN-1 has inhibitory activity for PBRM1-BD2 with IC50 value of 0.2 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human prostate cell lines LNCaP, PC3, and RWPE-1
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Concentration:0, 0.1, 1, and 10 μM
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Incubation Time:5 days
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Result:Inhibited LNCaP growth at higher concentrations.
Chemical Information
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CAS No. 1915012-21-3
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Masse moléculaire 302.80
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Formule C17H19ClN2O
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SMILES
O=C1N=C(/C(CC2)=C/C(CC)CC)N2C3=C1C(Cl)=CC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PBRM1-BD2-IN-1 Related Classifications
HY-151528 Related Classifications
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