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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2368944-44-7
- 分子式: C48H48Cl2N6O5
- 分子量:859.84
-
保管条件:
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]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
MoreEukaryotic Release Factor (eRF) アイソフォーム固有の製品をすべて表示
MoreCaspase アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
|
MDM2 23 nM (DC50) |
eRF3a/GSPT1 |
Cereblon |
Caspase 3 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SUP-B15 | IC50 |
0.0002 μM
|
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.
|
40440791 |
| NALM-6 | IC50 |
0.0002 μM
|
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.
|
40440791 |
| OCI-AML-3 | IC50 |
3.644 μM
|
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.
|
40440791 |
| SU-DHL-4 | IC50 |
>10 μM
|
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.
|
40440791 |
| MCF7 | IC50 |
>10 μM
|
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.
|
40440791 |
| MDA-MB-231 | IC50 |
>10 μM
|
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.
|
40440791 |
| LNCaP | IC50 |
>10 μM
|
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.
|
40440791 |
| PC-3 | IC50 |
>10 μM
|
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.
|
40440791 |
| RS4-11 | IC50 |
3.2 nM
|
Antiproliferative activity against human RS4;11 leukemia cells.
Antiproliferative activity against human RS4;11 leukemia cells.
|
38761584 |
| RS4-11 | DC50 |
23 nM
|
MDM2 protein degradation activity in human RS4;11 leukemia cells.
MDM2 protein degradation activity in human RS4;11 leukemia cells.
|
38761584 |
体外実験
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.
-
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)
-
Concentration:multiple concentrations (to generate IC50 values)
-
Incubation Time:72 h
-
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.
-
Cell Line:OCI-AML3 acute myeloid leukemia cell line
-
Concentration:0.01-1.0 μM
-
Incubation Time:20 h
-
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.
-
Cell Line:Kasumi-1 acute myeloid leukemia cell line
-
Concentration:0.01-1.0 μM
-
Incubation Time:20 h
-
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.
-
Cell Line:CCRF-CEM acute lymphoblastic leukemia cell line
-
Concentration:0.01-1.0 μM
-
Incubation Time:20 h
-
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).
化学情報
-
CAS 番号 2368944-44-7
-
分子量 859.84
-
分子式 C48H48Cl2N6O5
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
WB156 関連分類
HY-174266 関連分類
Powered by Bioz