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PBRM1-BD2-IN-5
CAS No. 2819989-61-0
PBRM1-BD2-IN-5( —— )
Catalog No. M35352 CAS No. 2819989-61-0
PBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 134 | Get Quote |
|
| 5MG | 188 | Get Quote |
|
| 10MG | 301 | Get Quote |
|
| 25MG | 439 | Get Quote |
|
| 50MG | 585 | Get Quote |
|
| 100MG | 794 | Get Quote |
|
| 500MG | 1593 | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NamePBRM1-BD2-IN-5
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NoteResearch use only, not for human use.
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Brief DescriptionPBRM1-BD2-IN-5 is a potent inhibitor of the PBRM1 Bromodomain, with dissociation constant (Kd) values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5 respectively, and an inhibitory concentration 50 (IC50) value of 0.26 μM for PBRM1-BD2.
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DescriptionPBRM1-BD2-IN-5 is a potent PBRM1 Bromodomain inhibitor with Kd values of 1.5 μM and 3.9 μM for PBRM1-BD2 and PBRM1-BD5, respectively, and an IC50 value of 0.26 μM for PBRM1-BD2. PBRM1-BD2-IN-5 reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptide. PBRM1-BD2-IN-5 can be used to research anticancer.
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In VitroPBRM1-BD2-IN-5 (compound 16) (0-10 μM; 5 days) inhibits PBRM1-expressed LNCaP cells, and reduces the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.Cell Viability Assay Cell Line:LNCaP cells expressing lentiviral shPBRM1 Concentration:0, 0.1, 1 and 10 μM Incubation Time:5 days Result:Exhibited a more significant effect on LNCaP viability in cells with native PBRM1 levels than in cells with PBRM1 knockdown.Reduced the binding of full-length PBRM1 within the PBAF complex in cell lysates to acetylated histone peptides.
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In Vivo——
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Synonyms——
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PathwayChromatin/Epigenetic
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TargetEpigenetic Reader Domain
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RecptorEpigenetic Reader Domain
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Research Area——
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Indication——
Chemical Information
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CAS Number2819989-61-0
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Formula Weight272.73
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Molecular FormulaC15H13ClN2O
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (366.66 mM; Ultrasonic )
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SMILESO=C1C=2C(NC(N1)C3=CC(C)=CC=C3)=CC=CC2Cl
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Shishodia S, et al. Selective and Cell-Active PBRM1 Bromodomain Inhibitors Discovered through NMR Fragment Screening. J Med Chem. 2022 Oct 13.?
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