An inhibitor of USP8
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DUB-IN-1

Item No. 41737

Technical Information
Formal Name
9-[(phenylmethoxy) imino]-9H-indeno[1,2-b] pyrazine-2,3-dicarbonitrile
CAS Number
924296-18-4
Synonyms
  • Deubiquitinase-IN-1
  • Deubiquitinase Inhibitor 1
  • DUB Inhibitor 1
  • DUBs-IN-1
  • DUBs Inhibitor 1
Molecular Formula
C20H11N5O
Formula Weight
Purity
≥95%
Formulation
A solid
DMSO: Soluble: ≥10 mg/ml
SMILES
N#CC(N=C12)=C(C#N)N=C2C3=C(C=CC=C3)C1=NOCC4=CC=CC=C4
InChi Code
InChI=1S/C20H11N5O/c21-10-16-17(11-22)24-20-18(23-16)14-8-4-5-9-15(14)19(20)25-26-12-13-6-2-1-3-7-13/h1-9H,12H2
InChi Key
GKOWDIBLCDZJHF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    DUB-IN-1 is an inhibitor of ubiquitin-specific protease 8 (USP8; IC50 = 0.85 µM).1 It is selective for USP8 over USP7 (IC50 = >100 µM). It inhibits the proliferation of LN-229, U87MG, and T98G glioblastoma cells when used at concentrations ranging from 200 to 800 nM.2 DUB-IN-1 (500 and 800 nM) reduces the migration and stemness of LN-229 and T98G cells and sensitizes both to ionizing radiation. It also reduces the viability of a variety of esophageal squamous cell carcinoma (ESCC) cells (IC50s = 1.58-2.14 µM) and induces apoptosis, autophagy, and cell cycle arrest at the G2/M phase in KYSE-450 and KYSE-30 ESCC cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Colombo, M., Vallese, S., Peretto, I., et alSynthesis and biological evaluation of 9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile analogues as potential inhibitors of deubiquitinating enzymes. ChemMedChem 5(4), 552-558 (2010).

    2. Long, Y., Hu, Z., Yang, D., et alPharmacological inhibition of the ubiquitin-specific protease 8 effectively suppresses glioblastoma cell growth. Open Life Sci. 18(1), 20220562 (2023).

    3. Sha, B., Sun, Y., Zhao, S., et alUSP8 inhibitor-induced DNA damage activates cell cycle arrest, apoptosis, and autophagy in esophageal squamous cell carcinoma. Cell Biol. Toxicol. 39(5), 2011-2032 (2023).