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PLK1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Antibiotic (2) Apoptosis (12) Aurora Kinase (1) Autophagy (4) Bcl-2 Family (1) c-Myc (2) CDK (1) DAPK (1) DNA/RNA Synthesis (1) Epigenetic Reader Domain (6) IKK (1) Microtubule/Tubulin (1) Mps1 (1) NEKs (2) Organoid (2) p38 MAPK (1) PARP (1) PI3K (4) PI5P4K (1) PIN1 (1) Polo-like Kinase (PLK) (47) PROTACs (1) RAR/RXR (2) STAT (1)
By Research Areas:	Cancer (54) Cardiovascular Disease (1) Inflammation/Immunology (2) Metabolic Disease (1)
Click Chemistry:	Azide (1) Alkynes (2)

Inhibitors & Agonists

Natural
Products

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15155

MLN0905 4 Publications Verification	Polo-like Kinase (PLK)	Cancer
MLN0905 is a potent, orally active Polo-like kinase 1 (PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC₅₀ value of 2 nM. MLN0905 can be used for the research of cancer .

HY-77195

Poloxime	Polo-like Kinase (PLK)	Cancer
Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive *Plk1* inhibitor, with moderate Plk1 inhibitory activity.

HY-160558

PLK1/BRD4-IN-3	Epigenetic Reader Domain Polo-like Kinase (PLK)	Cancer
PLK1/BRD4-IN-3 (Compound 21) is a selective dual inhibitor for bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). PLK1/BRD4-IN-3 inhibits BRD4-BD1, PLK1 and BRDT-BD1, with IC₅₀s of 0.059, 0.127 and 0.245 μM, respectively .

HY-148974

PLK1-IN-5	Polo-like Kinase (PLK)	Cancer
PLK1-IN-5 is a potent PLK1 inhibitor with an IC50 of < 500 nM. PLK1-IN-5 shows anticancer effects (WO2008113711A1; compound I-4) .

HY-161046

PLK1-IN-8	Polo-like Kinase (PLK)	Cancer
PLK1-IN-8 (compound TE6) is a *PLK1* inhibitor, and inhibits cell proliferation by blocking the cell cycle at G2 phase. PLK1-IN-8 shows anticancer activity in vivo .

HY-156336

PLK1-IN-7	Polo-like Kinase (PLK)	Cancer
PLK1-IN-7 (compound 30e) is a potent *PLK1* inhibitor, with an IC₅₀ of 0.66 nM. PLK1-IN-7 exhibits antiproliferative and antitumor activities .

HY-149100

PLK1-IN-6	Polo-like Kinase (PLK) Epigenetic Reader Domain	Cancer
PLK1-IN-6 is a potent and selective *PLK1* inhibitor, with an IC₅₀ of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells .

HY-139652

PLK1-IN-2	Polo-like Kinase (PLK)	Cancer
PLK1-IN-2 is a *PLK1* kinase inhibitor with an IC₅₀ value of 0.384 μM.

HY-146792

PLK1-IN-4	Polo-like Kinase (PLK)	Cancer
PLK1-IN-4 is a potent and selective *PLK1* inhibitor with IC₅₀ < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .

HY-161521

PLK1-IN-10	Polo-like Kinase (PLK)	Cancer
PLK1-IN-10 (Compound 4Bb) is an orally active *PLK1* PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death .

HY-158031

PLK1/BRD4-IN-5	Apoptosis Polo-like Kinase (PLK) Epigenetic Reader Domain	Cancer
PLK1/BRD4-IN-5 (Compound SC10) is an orally active *PLK1* and BRD4 inhibitor with IC₅₀ values of 0.3  nM and 60.8  nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research .

HY-W276819

PLK1-IN-9	Polo-like Kinase (PLK)	Cancer
PLK1-IN-9 (Compound M2) is an inhibitor for polo-like kinase 1 (PLK1), that inhibits PLK proteins modified with peptides 1010pT, cdc25c and PBIP, with IC₅₀s of 1.6, 0.8 and 1.4 μM, respectively. PLK1-IN-9 inhibits proliferations of cancer cells HeLa, HL60, SNU387/499, HepG2, exhibits cytotoxicity and induces apoptosis. PLK1-IN-9 inhibits tumor growth in HepG2 xenograft mouse model .

HY-13994

Mps1-IN-2	Mps1 Polo-like Kinase (PLK)	Cancer
Mps1-IN-2 is a potent, selective and ATP-competitive dual *Mps1/Plk1* inhibitor, with an IC₅₀ and a K_d of 145 nM and 12 nM for Mps1 and a K_d of 61 nM for Plk1.

HY-160557

PLK1/BRD4-IN-2	Epigenetic Reader Domain	Cancer
PLK1/BRD4-IN-2 (compound 15) is a BI-2536 (HY-50698) analog and dual inhibitor that targets both Polo-like kinase 1 (PLK1) and BRD4bromodomain (BRD4-BD1 IC₅₀=28 nM, PLK1 IC₅₀=40 nM) .

HY-155377

PLK1/p38γ-IN-1	Polo-like Kinase (PLK) p38 MAPK	Cancer
PLK1/p38γ-IN-1(compound 14) is a multitarget inhibitors ofPLK1andp38γ. PLK1/p38γ-IN-1inhibits the growth of human hepatocellular carcinoma and hepatoblastoma cells in vitro .

HY-149085

XS-060	RAR/RXR	Cancer
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting *pRXRα-PLK1* interaction*. XS-060 inhibits* p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome .

HY-15828

Onvansertib 5+ Cited Publications NMS-1286937; NMS-P937	Polo-like Kinase (PLK) Apoptosis	Cancer
NMS-1286937 is a potent, selective and orally available *PLK1* inhibitor, with an IC₅₀ of 2 nM.

HY-143471

WNY0824 PLK1/BRD4-IN-1	Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis Androgen Receptor c-Myc	Cancer
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 .

HY-123702

CAP-53194	Polo-like Kinase (PLK)	Cancer
CAP-53194 is a selective Plk1 inhibitor with potential anticancer activity. CAP-53194 was identified by a high-throughput virtual screening approach using molecular docking, showing 100-fold selectivity for Plk1 over Plk2-4 and other cell cycle kinases. CAP-53194 is able to effectively exploit subtle differences between the binding sites of Plk1 and other Ser/Thr kinases, thereby enhancing their inhibitory effects. CAP-53194 meets the Lipinski compound analog criteria and passes other ADMET filters, indicating good compound compatibility. CAP-53194 belongs to a new class of potential Plk1 inhibitors suitable for subsequent compound development and testing .

HY-160624

CD 10899	Polo-like Kinase (PLK)	Cancer
CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC₅₀: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer .

HY-50877

GSK461364 10+ Cited Publications GSK461364A	Polo-like Kinase (PLK)	Cancer
GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a K_i value of 2.2 nM.

HY-12045

HMN-214 4 Publications Verification IVX-214	Polo-like Kinase (PLK)	Cancer
HMN-214, an orally bioavailable proagent of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.

HY-12134

Poloxin 3 Publications Verification	Polo-like Kinase (PLK)	Cancer
Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC₅₀ of appr 4.8 μM.

HY-15161

Ro3280 4 Publications Verification	Polo-like Kinase (PLK)	Cancer
Ro3280 is a potent, highly selective inhibitor of *PLK1* with an IC₅₀ and a K_d of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.

HY-13647

HMN-176	Polo-like Kinase (PLK)	Cancer
HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization.

HY-108597

TC-S 7005 2 Publications Verification	Polo-like Kinase (PLK)	Cardiovascular Disease Inflammation/Immunology
TC-S 7005 is a Polo-like kinases (Plks) inhibitor with IC₅₀s of 4 nM, 24 nM and 214 nM for Plk2, Plk3, and Plk1, respectively .

HY-N8692

Dihydrobaicalein	Polo-like Kinase (PLK)	Cancer
Dihydrobaicalein is a *PLK1* Inhibitor with an IC₅₀ of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens .

HY-15159

Cyclapolin 9	Polo-like Kinase (PLK)	Cancer
Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 500 nM. Cyclapolin 9 is inactive against other kinases .

HY-102069

3MB-PP1	Polo-like Kinase (PLK) CDK DAPK	Others
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC₅₀=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division .

HY-15158

SBE13 Hydrochloride	Polo-like Kinase (PLK) Autophagy Apoptosis	Cancer
SBE13 Hydrochloride is a potent and selective *Plk1* inhibitor, with an IC₅₀ of 200 pM; SBE13 Hydrochloride poorly inhibits Plk2 (IC₅₀>66 μM) or Plk3 (IC₅₀=875 nM).

HY-15158A

SBE13	Polo-like Kinase (PLK) Autophagy	Cancer
SBE13 is a potent and selective *Plk1* inhibitor, with an IC₅₀ of 200 pM; SBE13 poorly inhibits Plk2 (IC₅₀>66 μM) or Plk3 (IC₅₀=875 nM).

HY-50698

BI 2536 35+ Cited Publications	Polo-like Kinase (PLK) Epigenetic Reader Domain Apoptosis	Cancer
BI 2536 is a dual *PLK1* and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively . BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .

HY-11003

GW843682X 5 Publications Verification GW843682	Polo-like Kinase (PLK)	Cancer
GW843682X is a selective, ATP-competitive inhibitor of *PLK1* and PLK3, with IC₅₀s of 2.2 nM and 9.1 nM, respectively, and is also >100-fold selective against ～30 other kinases.

HY-129265

Poloxin-2	Polo-like Kinase (PLK)	Cancer
Poloxin-2 is a small molecule Plk1 PBD inhibitor that can effectively induce cell mitotic arrest with an EC50 of approximately 15 μM in HeLa cells. Poloxin-2HT was developed by conjugating a hydrophobic tag (HT) to Poloxin-2, a new application of inhibitors targeting protein-protein interactions. Poloxin-2HT significantly enhanced the effects on cell viability and apoptosis by selectively degrading Plk1 protein, and its effect was stronger than that of untagged Poloxin-2. These data validate hydrophobic tags as a new strategy for targeting and disrupting disease-associated proteins.

HY-151986

FOXM1-IN-1	DNA/RNA Synthesis	Cancer
FOXM1-IN-1 is a potent FOXM1 inhibitor with an IC₅₀ value of 2.65 µM. FOXM1-IN-1 shows antiproliferative activity. FOXM1-IN-1 decreases the the expression of FOXM1, PLK1, CDC25B protein .

HY-10197

Wortmannin Maximum Cited Publications 118 Publications Verification SL-2052; KY-12420	Organoid PI3K Polo-like Kinase (PLK) Autophagy Antibiotic	Cancer
Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC₅₀ of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC₅₀s of 5.8 and 48 nM, respectively .

HY-126249

AAPK-25	Aurora Kinase Polo-like Kinase (PLK) Apoptosis	Cancer
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 ^Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with K_d values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with K_d values ranging from 55-456 nM .

HY-147298

Plogosertib 1 Publications Verification CYC140	Polo-like Kinase (PLK)	Cancer
Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive *PLK1* inhibitor (IC₅₀: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers .

HY-139188

CC260	PI5P4K	Metabolic Disease Cancer
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with K_is of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research .

HY-114302

CCB02 1 Publications Verification	Microtubule/Tubulin	Cancer
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC₅₀ of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .

HY-12137

Volasertib 20+ Cited Publications BI 6727	Polo-like Kinase (PLK) Apoptosis	Cancer
Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC₅₀s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .

HY-12037A

Rigosertib 5 Publications Verification ON-01910	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of *PLK1* with an IC₅₀ of 9 nM .

HY-12137A

Volasertib trihydrochloride BI 6727 trihydrochloride	Polo-like Kinase (PLK) Apoptosis	Cancer
Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC₅₀s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .

HY-149086

BPA-B9	RAR/RXR Apoptosis PARP Bcl-2 Family	Cancer
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (K_D=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .

HY-150259

MDEG-541	PROTACs c-Myc	Cancer
MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein .

HY-12037

Rigosertib sodium 5 Publications Verification ON-01910 sodium	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of *PLK1* with an IC₅₀ of 9 nM .

HY-15160

TAK-960 2 Publications Verification	Polo-like Kinase (PLK)	Cancer
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC₅₀ of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .

HY-15160B

TAK-960 dihydrochloride 2 Publications Verification	Polo-like Kinase (PLK)	Cancer
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC₅₀ of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .

HY-15160A

TAK-960 hydrochloride	Polo-like Kinase (PLK)	Cancer
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC₅₀ of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .

HY-10197R

Wortmannin (Standard)	Organoid PI3K Polo-like Kinase (PLK) Autophagy Antibiotic	Cancer
Wortmannin (Standard) is the analytical standard of Wortmannin. This product is intended for research and analytical applications. Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively .

Cat. No.	Product Name		Classification

HY-116423

JH295		Alkynes
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-116423A

JH295 hydrate		Alkynes
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC₅₀ of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-159493

BI2536-PEG2-Halo		Azide
BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC₅₀=23 nM), exhibits selective toxicity against p53 mutant cancer cells .

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PLK1 inhibitor

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