1. Cell Cycle/DNA Damage Epigenetics
  2. Deubiquitinase HDAC
  3. 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.

For research use only. We do not sell to patients.

UBD1031

UBD1031 Chemical Structure

Size Price Stock Quantity
5 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 8 - 10 weeks
10 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 8 - 10 weeks
25 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 8 - 10 weeks
50 mg Get quote 8 - 10 weeks 7 - 9 weeks 9 - 11 weeks 8 - 10 weeks
100 mg   Get quote  
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T and HCT116 cells
Concentration: 30 μM
Incubation Time: 5 day
Result: No reduction in cell confluency was observed relative to DMSO-treated controls in either cell line.
Molecular Weight

449.84

Formula

C21H18ClF2N3O4

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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UBD1031
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HY-172193
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