WNY0824 (Synonyms: PLK1/BRD4-IN-1)

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WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC₅₀ values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models.

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WNY0824 Chemical Structure

CAS No. : 2412707-81-2

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PLK1 PLK2 PLK3 PLK4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[2]

PLK1

22 nM (IC₅₀)

BRD2

402.5 nM (IC₅₀)

BRD3

150.7 nM (IC₅₀)

BRD4

103.9 nM (IC₅₀)

BRDT

311.9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	2.82 μM Compound: 9b	Cytotoxicity against human A-375 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A-375 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32088495]
CWR22R	IC₅₀	0.58 μM Compound: WNY0824	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	1.465 μM Compound: WNY0824	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]
HT-29	IC₅₀	2.51 μM Compound: 9b	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32088495]
LNCaP	IC₅₀	0.14 μM Compound: 9b	Cytotoxicity against human LNCaP cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human LNCaP cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32088495]
LNCaP	IC₅₀	1.451 μM Compound: WNY0824	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	0.13 μM Compound: WNY0824	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]
MV4-11	IC₅₀	0.13 μM Compound: 9b	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32088495]
PC-3	IC₅₀	1.403 μM Compound: WNY0824	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]
SK-OV-3	IC₅₀	1.1 μM Compound: 9b	Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human SK-OV-3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32088495]
VCaP	IC₅₀	0.628 μM Compound: WNY0824	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

Cell Viability Assay^[1]

Cell Line:	MV4-11, LnCap, HT-29, A375, SKOV-3
Concentration:	Cells were maintained in RPMI 1640 or DMEM medium supplemented with 10% FBS (v/v) in 5% CO₂, except for MV4-11 cells, which were cultured in IMDM medium.
Incubation Time:	72 h
Result:	Showed broad-spectrum antiproliferative activities with IC₅₀ values of 0.13, 0.14, 1.10, 2.82 and 2.51 µM against MV4-11, LnCap, SKOV-3, A375 and HT29 cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:	MV4-11
Concentration:	0.1, 0.3, 1, 3, 9 µM
Incubation Time:	24 h
Result:	Induced obvious G2/M arrest in a concentration-dependent manner

Apoptosis Analysis^[1]

Cell Line:	MV4-11
Concentration:	0.1, 0.3, 1, 3, 9 µM
Incubation Time:	48 h
Result:	Significantly increased the number of Annexin V/PI-positive MV4-11 cells in a concentration-dependent manner.

RT-PCR^[1]

Cell Line:	MV4-11
Concentration:	0.1, 0.3, 1, 3, 9 µM
Incubation Time:	24 h
Result:	Reduced the transcription of c-MYC and MYCN as well as BCL-2, in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:	MV4-11
Concentration:	0.1, 0.3, 1, 3, 9 µM
Incubation Time:	48 h
Result:	Decreased the expression of c-Myc and Bcl-2 in a concentration dependent-manner and upregulated cleaved caspase-3 and cleaved PARP.

In Vivo

Animal Model:	Five weeks old male NOD-SCID mice^[1].
Dosage:	60 mg/kg/d
Administration:	Oral gavage, 18 days; tumor xenograft models were established by subcutaneously injecting 100 µL of 1×10⁸ cell/mL MV4-11 cell suspension into NOD-SCID mice.
Result:	Resulted in a significant decrease in average tumor size, with 66% tumor growth inhibition, and didn’t obviously affect the body weight of mice.

Molecular Weight

573.73

Formula

C₃₁H₄₃N₉O₂

CAS No.

2412707-81-2

SMILES

O=C(NC1CCN(C)CC1)C2=CC=C(NC(N=C3N(CC4CCCCC4)[C@@H]5CC)=NC=C3N6C5=NN=C6C)C(OC)=C2

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

Handling Instructions (2659 KB)

References

[1]. Ning-Yu Wang, et al. Design, synthesis, and biological evaluation of 4,5-dihydro-[1,2,4]triazolo[4,3-f]pteridine derivatives as novel dual-PLK1/BRD4 inhibitors. Eur J Med Chem. 2020 Apr 1;191:112152. [Content Brief]

[2]. Ying Xu, et al. "Novel dual BET and PLK1 inhibitor WNY0824 exerts potent antitumor effects in CRPC by inhibiting transcription factor function and inducing mitotic abnormality." Molecular Cancer Therapeutics 19.6 (2020): 1221-1231. [Content Brief]

WNY0824 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:

WNY08242412707-81-2PLK1/BRD4-IN-1WNY 0824WNY-0824Polo-like Kinase (PLK)Epigenetic Reader DomainApoptosisAndrogen Receptorc-MycMycMV4-11NOD-SCIDkinase inhibitorsInhibitorinhibitorinhibit

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