2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs Deubiquitinase Apoptosis MDM-2/p53
  4. U7D-1

U7D-1 

Cat. No.: HY-148369 Purity: 99.65%
COA Handling Instructions

U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells.

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

U7D-1 Chemical Structure

U7D-1 Chemical Structure

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1 mg USD 231 In-stock
5 mg USD 509 In-stock
10 mg USD 814 In-stock
25 mg USD 1630 In-stock
50 mg USD 2610 In-stock
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Based on 1 publication(s) in Google Scholar

U7D-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells[1].

IC50 & Target

DC50: 33 nM (USP7 in RS4;11 cells)[1]
In Vitro

U7D-1 (0-1 μM, 0-24 h) induced USP7 degradation in RS4;11 cell, reducing the USP7 protein level by 83.2% at 1 μM[1].
U7D-1 (0-20 μM, 3 days) shows anti-proliferative activity in p53 wild-type cell lines, and maintains potent cell growth inhibition in p53 mutant cancer cells[1].
U7D-1 (1 μM, 0-24 h) upregulates the level of p53 and p21 proteins in a time-dependent manner, and induces cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner[1].
U7D-1 (1 μM, 24 h) up-regulates the expression of apoptotic related genes and down-regulates the expression of E2F related genes in Jeko-1 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

U7D-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: RS4;11 cells
Concentration: 0, 5, 20, 50, 100, and 500 nM
Incubation Time: 24 h
Result: Induced USP7 degradation in RS4;11 cell in a dose dependent manner, with a DC50 (half-maximal degradation) value of 33 nM.

Cell Proliferation Assay[1]

Cell Line: p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines); p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM)
Concentration: 0-20 μM
Incubation Time: 3 days
Result: Showed antiproliferative activity in p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines), and p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM), with IC50 values for 3 days of 79.4, 227.0, 830.3, 1367.2, 4948.0, 1034.9, 1175.3, 1860.6, 6077.6, 9078.0, and 10675.0, respectively. Had an antiproliferative activity with an IC50 value of 53.5 nM in Jeko-1 cells for 7 days but exhibited a 13-fold loss in antiproliferative activity with an IC50 value of 727 nM in Jeko-1 CRBN KO cells.

Western Blot Analysis[1]

Cell Line: RS4;11 cells, Jeko-1 and Mino cell
Concentration: 1 μM
Incubation Time: 0, 2, 4, 6, 8, 10, 12, 20, 24, 36, 48, 60, and 72 h
Result: USP7 degradation in RS4;11 cells induced by U7D-1 started after 4 h of exposure and more effective degradation was observed after 8 h of exposure. Up-regulated the level of p53 and p21 proteins in RS4;11 cells in a time-dependent manner. Had no effect on the level of p53 protein in p53-mutant cell lines. Induced cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner.
Molecular Weight

940.14

Appearance

Solid

Formula

C53H65N9O7
SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCCCCCCNCC4=CC=C(C5=C(C6=NN5C)N=CN(CC7(O)CCN(C(C[C@H](C8=CC=CC=C8)C)=O)CC7)C6=O)C=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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U7D-1 Related Classifications

Help & FAQs
  • 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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Keywords:

U7D-1PROTACsDeubiquitinaseApoptosisMDM-2/p53DUBsRS4;11OCI-ly10MV4;11RehMOLT4 cellJeko-1 cellsMinoRPMI-8226JurkatSU-DHL-6CCRF-CEMp53 mutant cancer cellsantiproliferativeJeko-1 CRBN KO cellsInhibitorinhibitorinhibit

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