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
1 mL x 10 mM in DMSO 180 In Stock
5MG 187 In Stock
10MG 275 In Stock
25MG 453 In Stock
50MG 591 In Stock
100MG 820 In Stock
200MG 1097 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    PBRM1-BD2-IN-5
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    PBRM1-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.
  • In Vitro
    PBRM1-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.
  • In Vivo
    ——
  • Synonyms
    ——
  • Pathway
    Chromatin/Epigenetic
  • Target
    Epigenetic Reader Domain
  • Recptor
    Epigenetic Reader Domain
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2819989-61-0
  • Formula Weight
    272.73
  • Molecular Formula
    C15H13ClN2O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (366.66 mM; Ultrasonic )
  • SMILES
    O=C1C=2C(NC(N1)C3=CC(C)=CC=C3)=CC=CC2Cl
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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