WB214
WB214 is an MDM2 and GSPT1 degrader with human MDM2 Ki >10 μM. WB214 induces a neo-interaction between MDM2 and the cereblon E3 ligase complex, triggering MDM2 ubiquitination, proteasomal degradation, and bystander p53 degradation, and does not bind MDM2’s p53 binding region. WB214 induces GSPT1 degradation, and exhibits anti-proliferative activity in leukemia cells. WB214 can be used for the research of leukemia.
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- CAS No.: 2640723-72-2
- Formule: C44H43ClF3N5O7
- Masse moléculaire:846.29
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| RS4-11 | IC50 |
1.2 nM
Compound: 11; WB214
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Antiproliferative activity against human RS4-11 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
Antiproliferative activity against human RS4-11 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay
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[PMID: 33862513] |
WB214 (compound 11) (97 nM-10 μM; 72 h) potently inhibits RS4;11 human acute leukemia cell proliferation with an IC50 of 1.2 nM[1].
WB214 (1.2 nM-1 μM; 1-12 h) induces time- and dose-dependent degradation of MDM2 (DC50 = 4.1 nM) and p53 (DC50 = 29 nM) in RS4;11 human acute leukemia cells[1].
WB214 (100 nM; 6 h) mediated degradation of MDM2 and p53 in RS4;11 human acute leukemia cells depends on the CRBN E3 ligase and ubiquitin-proteasome system, with p53 degraded as a bystander due to its association with MDM2[1].
WB214 (97 nM-10 μM; 0.5 h) does not bind to the p53 binding pocket of purified MDM2 protein[1].
WB214 (100 nM) efficiently induces ternary complex formation between MDM2 and CRBN in RS4;11 human acute leukemia cells[1].
WB214 (increasing concentrations; 15 min) potently induces dose-dependent formation of ternary complexes between purified CRBN/DDB1 and MDM2 proteins[1].
WB214 (100 nM; 6 h) causes degradation of MDM2 and p53 that is abolished when co-treated with Lenalidomide (HY-A0003) or MG132 (HY-13259)[1].
WB214 (1.2-nM; 6-12 h) induces dose-dependent degradation of GSPT1 (DC50 = 0.64 nM) in RS4;11 human acute leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11 human acute leukemia cells
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Concentration:1.2 nM; 3.7 nM; 11 nM; 33 nM; 100 nM; 1 μM
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Incubation Time:1 h; 2 h; 4 h; 6 h; 8 h; 12 h
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Result:Induced time-dependent degradation of MDM2 and p53, with detectable degradation observed as early as 4 h post-treatment with 100 nM, and near-complete MDM2 depletion by 8 h.
Exhibited dose-dependent degradation with a DC50 of 4.1 nM for MDM2 and 29 nM for p53 at 12 h.
Resulted in significant depletion of both MDM2 and p53 protein levels when treated at 1 μM for 6 h.
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Cell Line:RS4;11 human acute leukemia cells
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Concentration:100 nM; 100 nM plus 20 μM Lenalidomide; 100 nM plus 5 μM MG132; 100 nM plus 10 μM ligand 1; 100 nM plus 10 μM WB138
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Incubation Time:6 h
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Result:Caused degradation of MDM2 and p53 that was abolished when co-treated with Lenalidomide or MG132.
Induced degradation of MDM2 that was not blocked, and degradation of p53 that was rescued, when co-treated with MDM2 inhibitors ligand 1 or WB138.
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Cell Line:RS4;11 human acute leukemia cells
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Concentration:1.2 nM; 3.7 nM; 11 nM; 33 nM; 100 nM
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Incubation Time:6 h; 12 h
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Result:Induced potent degradation of GSPT1, with dose-dependent degradation observed and a DC50 of 0.64 nM at 12 h.
Resulted in significant depletion of GSPT1 protein levels when treated with 10 nM or 100 nM for 6 h.
Chemical Information
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CAS No. 2640723-72-2
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Masse moléculaire 846.29
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Formule C44H43ClF3N5O7
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SMILES
O=C(C1=C(C(N(CC2=CC(F)=C(C(F)=C2)F)C(CCCCC#CC3=CC=CC4=C3CN(C5C(NC(CC5)=O)=O)C4=O)=O)C(NC(C)(C)C)=O)C6=C(C=C(C=C6)Cl)N1)OCC
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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)
WB214 Related Classifications
HY-182623 Related Classifications
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