WB156
WB156 is a dual MDM2 and GSPT1 PROTAC degrader with a DC50 of 23 nM against MDM2. WB156 induces the degradation of MDM2 and GSPT1 via the ubiquitin-proteasome system. WB156 upregulates the levels of p53 and p21, and triggers Apoptosis through the cleavage of PARP and Caspase-3. WB156 can be used in leukemia-related research.
(Pink: MDM2 and GSPT1 ligand (HY-157830); Blue: Cereblon ligand (HY-138793); Black: linker).
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- CAS No.: 2368944-44-7
- Formule: C48H48Cl2N6O5
- Masse moléculaire:859.84
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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
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Activité biologique
Description
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MDM2 23 nM (DC50) |
eRF3a/GSPT1 |
Cereblon |
Caspase 3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SUP-B15 | IC50 |
0.0002 μM
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Antiproliferative activity against human SUP-B15 leukemia cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human SUP-B15 leukemia cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| NALM-6 | IC50 |
0.0002 μM
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Antiproliferative activity against human NALM-6 leukemia cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human NALM-6 leukemia cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| OCI-AML-3 | IC50 |
3.644 μM
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Antiproliferative activity against human Oci-AML3 leukemia cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human Oci-AML3 leukemia cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| SU-DHL-4 | IC50 |
>10 μM
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Antiproliferative activity against human SU-DHL-4 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human SU-DHL-4 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| MCF7 | IC50 |
>10 μM
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Antiproliferative activity against human MCF-7 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human MCF-7 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| MDA-MB-231 | IC50 |
>10 μM
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Antiproliferative activity against human MDA-MB-231 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human MDA-MB-231 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| LNCaP | IC50 |
>10 μM
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Antiproliferative activity against human LnCaP non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human LnCaP non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| PC-3 | IC50 |
>10 μM
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Antiproliferative activity against human PC3 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
Antiproliferative activity against human PC3 non-leukemia cancer cells assessed as reduction in cell viability incubated for 72 hrs by Alamar Blue assay.
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40440791 |
| RS4-11 | IC50 |
3.2 nM
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Antiproliferative activity against human RS4;11 leukemia cells.
Antiproliferative activity against human RS4;11 leukemia cells.
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38761584 |
| RS4-11 | DC50 |
23 nM
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MDM2 protein degradation activity in human RS4;11 leukemia cells.
MDM2 protein degradation activity in human RS4;11 leukemia cells.
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38761584 |
In Vitro
WB156 (multiple concentrations; 72 h) inhibits proliferation in all tested leukemia cell lines (wild-type and mutant p53) with IC50 values ranging from 0.0002 μM to 3.644 μM, but has no anti-proliferative effect on tested lymphoma, breast, or prostate cancer cell lines[1].
WB156 (100 nM; 3 h, 6 h) induces degradation of MDM2, GSPT1, and GSPT2, and upregulates p53 in MV-4-11 and MOLT-4 leukemia cells[1].
WB156 (0.01-1.0 μM; 20 h) upregulates p53, does not alter MDM2 levels, and degrades GSPT1 in OCI-AML3 cells[1].
WB156 (0.01-1.0 μM; 20 h) degrades both MDM2 and GSPT1 in Kasumi-1 cells[1].
WB156 (0.01-1.0 μM; 20 h) reduces MDM2 levels at 0.1, 1.0 μM, and degrades GSPT1 at 0.01, 0.1, and 1.0 μM in CCRF-CEM cells[1].
WB156 potently inhibits RS4;11 leukemia cell proliferation with an IC50 of 3.2 nM, degrades MDM2 protein with a DC50 of 23 nM, upregulates p53 and p21, and induces apoptosis via PARP and caspase-3 cleavage[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:12 leukemia cell lines (RS4;11, MOLT-4, Jurkat, MV-4-11, MOLM-13, Oci-AML3, Kasumi-1, Kasumi-3, CCRF-CEM, THP-1, SUP-B15, NALM-6), 6 non-leukemia cancer cell lines (SU-DHL-4, MCF-7, MDA-MB-231, LnCaP, PC3, 22rv1)
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Concentration:multiple concentrations (to generate IC50 values)
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Incubation Time:72 h
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Result:Exhibited anti-proliferative activity in all 12 leukemia cell lines, with IC50 values ranging from 0.0002 μM to 3.644 μM.
Showed no anti-proliferative activity (IC50 >10 μM) in all 6 tested non-leukemia cancer cell lines.
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Cell Line:OCI-AML3 acute myeloid leukemia cell line
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Concentration:0.01-1.0 μM
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Incubation Time:20 h
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Result:Did not significantly modulate MDM2 levels at all tested concentrations.
Induced significant upregulation of p53 levels at all tested concentrations.
Significantly reduced GSPT1 levels at all tested concentrations.
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Cell Line:Kasumi-1 acute myeloid leukemia cell line
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Concentration:0.01-1.0 μM
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Incubation Time:20 h
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Result:Induced degradation of MDM2 at all tested concentrations.
Induced degradation of GSPT1 at all tested concentrations, with the strongest degradation observed at 1.0 μM.
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Cell Line:CCRF-CEM acute lymphoblastic leukemia cell line
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Concentration:0.01-1.0 μM
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Incubation Time:20 h
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Result:Induced loss of MDM2 at 0.1 μM and 1.0 μM.
Induced degradation of GSPT1 at all tested concentrations (0.01, 0.1, 1.0 μM).
Chemical Information
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CAS No. 2368944-44-7
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Masse moléculaire 859.84
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Formule C48H48Cl2N6O5
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SMILES
O=C(N1CCN(CC1)CC#CC2=C3C(C(N(C4C(NC(CC4)=O)=O)C3)=O)=CC=C2)N5[C@H](C6=CC=C(C=C6)Cl)[C@H](C7=CC=C(C=C7)Cl)N=C5C8=C(C=C(C=C8)C(C)(C)C)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
[1]. Tandon I, et al. Characterization of a dual degrader of MDM2 and GSPT1. European journal of medicinal chemistry. 2025 Oct 05;295:117793. [Content Brief]
[2]. Li H, et al. An overview of PROTACs targeting MDM2 as a novel approach for cancer therapy. European journal of medicinal chemistry. 2024 Jun 05;272:116506. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WB156 Related Classifications
HY-174266 Related Classifications
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