2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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.

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WWL0245 Chemical Structure

WWL0245 Chemical Structure

CAS No. : 2869057-11-2

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WWL0245 Related Antibodies

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Description

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[1].

IC50 & Target[1]

BRD4

1 nM (IC50)

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.

WWL0245 Related Antibodies

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.
Molecular Weight

873.96

Formula

C45H51N11O8
CAS No.
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
References
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WWL0245 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WWL02452869057-11-2WWL 0245WWL-0245Epigenetic Reader DomainBRD4PROTACAR-positiveprostate cancerInhibitorinhibitorinhibit

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