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Cat. No.: HY-153519

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WWL0245

WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC₅₀ (<1 nM) than BRD2/3 and PLK1 ( DC₅₀>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4.

For research use only. We do not sell to patients.

CAS No.: 2869057-11-2
Formula: C₄₅H₅₁N₁₁O₈
Molecular Weight:873.96

Storage:

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

Data Sheet (274 KB)

WWL0245 Chemical Structure

CAS No.: 2869057-11-2

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

BRD4

1 nM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	0.053 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
DU-145	IC₅₀	10 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-negative human castration resistant DU-145 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-negative human castration resistant DU-145 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
LNCaP	IC₅₀	0.021 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-positive harmone sensitive human LNCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-positive harmone sensitive human LNCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
MV4-11	IC₅₀	0.003 μM Compound: 12a; WWL0245	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
PC-3	IC₅₀	2.435 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-negative human castration resistant PC-3 cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-negative human castration resistant PC-3 cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]
VCaP	IC₅₀	0.016 μM Compound: 12a; WWL0245	Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability measured after 4 days by MTT assay	[PMID: 34700270]

In Vitro

WWL0245 (0-1 μM; 96h) suppresses the proliferation of AR-positive prostate cancer cells with IC₅₀ values range from 0.0159 μM -10 μM. It shows greater antiproliferative activity to AR-positive cell lines VCaP, LNCaP, 22Rv1 with IC₅₀ values of 0.016 μM, 0.021 μM, 0.053 μM, respectively^[1].
WWL0245 (1 μM; 24 hours) results in the downregulation of BRD4 and c-Myc in a time-dependent manner in LNCaP, 22Rv1, VCaP cell lines and results in the decrease of BRD4 level and c-Myc level in a concentration-dependent manner in 22Rv1 and VCaP cell with DC50 of sub-nanomolar. But WWL0245 could also downregulate BRD4 level in DU145 cells but has negligible effects in c-Myc level^[1].
WWL0245 (100 nM-1 μM; 24 hours) suppresses the transcription of AR-regulated genes (PSA, TMPRSS2, ERG, FKBP5, BMPR1B) at various degrees^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

HL60, SU-DHL-6, RS4;11, JURKAT, A2780, MDA-MB-468, BT549, LNCaP, 22Rv1, and VCaP cells
Concentration:

0 μM -10 μM
Incubation Time:

96 h
Result:

Inhibited HL60, SU-DHL-6, RS4;11, JURKAT, A2780, MDA-MB-468, BT549, LNCaP, 22Rv1, and VCaP growth with IC₅₀ values of 0.0961, 0.0734, 0.0247, 0.5018, 0.0153, 0.2460, and 0.1732 μM, respcetively[1].

Western Blot Analysis^[1]

Cell Line:

Prostate cancer cell lines: LNCaP, 22Rv1, VCaP, DU145
Concentration:

1 nM, 10 nM, 100 nM, 1000 nM, 10000 nM
Incubation Time:

1 hour, 2 hours, 4 hours,12 hours, 24 hours,48 hours
Result:

Resulted in the downregulation of BRD4 and c-Myc in a time/concentration-dependent manner in 22Rv1 and VCaP cells.

RT-PCR^[1]

Cell Line:

Prostate cancer: VCaP cell
Concentration:

100 nM-1 μM
Incubation Time:

24 h
Result:

Suppressed the expression of AR-regulated genes in prostate cancer.

Chemical Information

CAS No. 2869057-11-2
Molecular Weight 873.96
Formula C₄₅H₅₁N₁₁O₈
SMILES

CC[C@@H](N(C1=N2)CC3CCCCC3)C4=NN=C(C)N4C1=CN=C2NC5=C(C=C(C=C5)C(NC6CCN(CC6)C(COC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8=O)=O)=CC=C7)=O)=O)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Rong Hu, et al. Identification of a selective BRD4 PROTAC with potent antiproliferative effects in AR-positive prostate cancer based on a dual BET/PLK1 inhibitor. Eur J Med Chem. 2022 Jan 5;227:113922. [Content Brief]

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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.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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WWL0245

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Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

WWL0245 Related Classifications

HY-153519 Related Classifications