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7-Chloro-9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile, HBX 41108, HBX-41108, HBX41108
C13H3ClN4O
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
O=C(C1=C2C=CC(Cl)=C1)C3=C2N=C(C(C#N)=N3)C#N
InChI
1S/C13H3ClN4O/c14-6-1-2-7-8(3-6)13(19)12-11(7)17-9(4-15)10(5-16)18-12/h1-3H
InChI key
BIGPXXAUSQLTQR-UHFFFAOYSA-N
Biochem/physiol Actions
HBX 41,108 is a catalytic site-targeting, uncompetitive, potent and reversible ubiquitin-specific protease (USP) inhibitor (USP7/HAUSP IC50 = 420 nM) with little potency toward aspartic, serine or other non-USP cysteine proteases. HBX 41,108 exhibits antiproliferation potency in cancer cultures (HCT116 GI50 = 1 μM post 24 h treatment) by preventing USP7-mediated p53 deubiquitination and thereby promoting p53 target genes expression and inducing p53-dependent apoptosis.
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
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Small-molecule inhibitor of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells.
Molecular Cancer Therapeutics, 8, 2286-2295 (2009)
USP7 regulates the proliferation and differentiation of ATDC5 cells through the Sox9-PTHrP-PTH1R axis.
Bone, 143, 115714-115714 (2021)
Frontiers in chemistry, 9, 640105-640105 (2021-03-16)
The potency and selectivity of a small molecule inhibitor are key parameters to assess during the early stages of drug discovery. In particular, it is very informative for characterizing compounds in a relevant cellular context in order to reveal potential
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