UBD1031
UBD1031 (SGC-UBD1031) is a selective USP16/HDAC6-UBD antagonist with a human USP16-UBD IC50 of 10.6 μM, KD value of 48 nM, and a human HDAC6-UBD KD of 16 nM. UBD1031 disrupts ISG15 C-terminus interactions with USP16-UBD and HDAC6-UBD, and exhibits cooperative inhibition of full-length USP16 deubiquitinase activity via USP16-UBD binding. UBD1031 can be used in research on cancer, autoimmune diseases, and Down syndrome.
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- Formule: C21H18ClF2N3O4
- Masse moléculaire:449.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
UBD1031 potently binds purified USP16-UBD (residues 25-185) with an SPR-determined KD of 48 nM[1].
UBD1031 potently binds purified HDAC6-UBD (residues 1109-1215) with an SPR-determined KD of 16 nM[1].
UBD1031 (0.01 nM-10 μM) inhibits the deubiquitinase activity of purified full-length USP16 (USP161-823) with an IC50 of 10.6 μM, reaching up to 60% inhibition at maximal tested concentrations[1].
UBD1031 is at least 100-fold selective for USP16-UBD and HDAC6-UBD over seven other tested purified UBD-containing proteins (USP3, USP5, USP13, USP33, USP49, USP51, BRAP)[1].
UBD1031 (0.1-10 μM; 4 h) disrupts the interaction between USP16 and ISG15 in HEK293T cells with an IC50 of 1.7 μM[1].
UBD1031 (0.1-10 μM; 4 h) disrupts the interaction between HDAC6 and ISG15 in HEK293T cells with an IC50 of 1.5 μM[1].
UBD1031 (30 μM; 5 day) shows no detectable toxicity to HEK293T or HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T and HCT116 cells
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Concentration:30 μM
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Incubation Time:5 day
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Result:No reduction in cell confluency was observed relative to DMSO-treated controls in either cell line.
Chemical Information
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Masse moléculaire 449.84
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Formule C21H18ClF2N3O4
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SMILES
OC(CCC1=NC2=C(C(N1CC(N[C@@H](C)C3=C(C=CC=C3F)F)=O)=O)C=CC=C2Cl)=O
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Synonyms
SGC-UBD1031
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UBD1031 Related Classifications
HY-172193 Related Classifications
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