XM-U-14
XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)).
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- CAS No.: 3098519-83-3
- Formule: C58H69N11O7S
- Masse moléculaire:1064.30
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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USP7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| REH | IC50 |
8.3 nM
Compound: 14h; XM-U-14
|
Antiproliferative activity against human REH cells with wild type p53 assessed as cell viability measured after 3 days by PMS-MTS assay
Antiproliferative activity against human REH cells with wild type p53 assessed as cell viability measured after 3 days by PMS-MTS assay
|
[PMID: 39028938] |
| RS4-11 | IC50 |
>20000 nM
Compound: 14h; XM-U-14
|
Antiproliferative activity against human RS4-11 cells with shp53 assessed as cell viability measured after 7 days by PMS-MTS assay
Antiproliferative activity against human RS4-11 cells with shp53 assessed as cell viability measured after 7 days by PMS-MTS assay
|
[PMID: 39028938] |
| RS4-11 | IC50 |
0.5 nM
Compound: 14h; XM-U-14
|
Antiproliferative activity against human RS4-11 cells with wild type p53 assessed as cell viability measured after 3 days by PMS-MTS assay
Antiproliferative activity against human RS4-11 cells with wild type p53 assessed as cell viability measured after 3 days by PMS-MTS assay
|
[PMID: 39028938] |
Chemical Information
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CAS No. 3098519-83-3
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Masse moléculaire 1064.30
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Formule C58H69N11O7S
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SMILES
CC1=C(SC=N1)C2=CC=C(C=C2)[C@H](C)NC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)C)C4=CC(N5CCN(CC5)CC6=CC=C(C=C6)C7=C(C8=NN7C)N=CN(C8=O)CC9(CCN(CC9)C(C[C@@H](C)C%10=CC=CC=C%10)=O)O)=NO4)=O)=O
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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)