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Cat. No.: HY-174266

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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).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 2368944-44-7
화학식: C₄₈H₄₈Cl₂N₆O₅
분자량:859.84

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (290 KB)

WB156 Chemical Structure

CAS No.: 2368944-44-7

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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^[1]^[2]. (Pink: MDM2 and GSPT1 ligand (HY-157830); Blue: Cereblon ligand (HY-138793); Black: linker).

IC₅₀ & Target

^[2]^[1]

MDM2

23 nM (DC₅₀)

eRF3a/GSPT1

Cereblon

Caspase 3

All PROTACs Isoforms :

All Eukaryotic Release Factor (eRF) Isoforms :

All PARP Isoforms :

All Caspase Isoforms :

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

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.

Cell Viability Assay^[1]

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.

Western Blot Analysis^[1]

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.

Western Blot Analysis^[1]

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.

Western Blot Analysis^[1]

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).

Chemical Information

CAS No. 2368944-44-7
분자량 859.84
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

WB156

All PROTACs Isoforms

All Eukaryotic Release Factor (eRF) Isoforms

All PARP Isoforms

All Caspase Isoforms