An inhibitor of PRC1 ubiquitin ligases
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PRT4165

Item No. 19093

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(3-pyridinylmethylene)-1H-indene-1,3(2H)-dione
CAS Number
31083-55-3
Synonyms
  • NSC 600157
Molecular Formula
C15H9NO2
Formula Weight
235.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 2 mg/mlEthanol: 1 mg/ml
λmax
245, 264, 330 nm
SMILES
O=C(C1=CC=CC=C1C/2=O)C2=C\C3=CC=CN=C3
InChi Code
InChI=1S/C15H9NO2/c17-14-11-5-1-2-6-12(11)15(18)13(14)8-10-4-3-7-16-9-10/h1-9H
InChi Key
OMHZFEWYVFWVLI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $63

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    10 mg

    $94

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    25 mg

    $195

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    Product Description

    PRT4165 is an inhibitor of the ubiquitin ligase activity of PRC1.1,2 It blocks BMI1/RING1A self-ubiquitination (IC50 = 3.9 µM), as well as polyubiquitination of topoisomerase 2α in cells.1 PRT4165 inhibits ubiquitination of H2A by either RNF2 or RING1. Through these actions, PRT4165 prevents the accumulation of detectable ubiquitin at DNA double-strand breaks, the retention of response proteins around breaks, and the repair of breaks.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Alchanati, I., Teicher, C., Cohen, G., et al. The E3 ubiquitin-ligase Bmi1/Ring1A controls the proteasomal degradation of Top2α cleavage complex - a potentially new drug target. PLoS One 4(12), (2009).

    2. Ismail, I.H., McDonald, D., Strickfaden, H., et al. A small molecule inhibitor of polycomb repressive complex 1 inhibits ubiquitin signaling at DNA double-strand breaks. The Journal of Biological Chemisty 288(37), 26944-26954 (2013).