PLK

Cat. No.

A30559

CAS No.

3063893-60-4

PLK1/BRD4-IN-5

PLK1/BRD4-IN-5 is a potent inhibitor targeting both PLK1 and BRD4, exhibiting IC50 values of 0.3 nM and 60.8 nM, respectively. This compound effectively induces cell cycle arrest in the S phase and promotes apoptosis in MV4-11 cells in a dose-dependent manner. PLK1/BRD4-IN-5 is a valuable tool for cancer research, facilitating studies on mechanisms of tumorigenesis and therapeutic responses.

Cat. No.

A31067

CAS No.

946161-17-7

Volasertib trihydrochloride

Synonyms: BI 6727 trihydrochloride

Volasertib trihydrochloride is a potent, ATP-competitive inhibitor of Polo-like kinase 1 (PLK1) with an IC50 of 0.87 nM. This compound also exhibits inhibitory activity against PLK2 and PLK3 with IC50s of 5 nM and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis in cancer cells, demonstrating significant antitumor efficacy across various cancer models. It is a valuable tool for research focused on cell division and the development of cancer therapeutics.

Cat. No.

A31732

CAS No.

3038489-48-1

PLK1-IN-13

PLK1-IN-13 is a selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 0.27 nM, exhibiting oral bioavailability. It also demonstrates inhibitory activity against PLK2 and PLK3, with IC50 values of 12.72 nM and 4.12 nM, respectively. PLK1-IN-13 effectively induces G2 phase cell cycle arrest, promotes apoptosis, and down-regulates the c-MYC oncogene, which is associated with tumor proliferation. This compound is particularly relevant for research on acute myeloid leukemia (AML) and other cancer models.

Cat. No.

A31756

CAS No.

3068529-37-0

PLK1-IN-15

PLK1-IN-15 is a potent inhibitor of Polo-like Kinase 1 (PLK1) with an IC50 of 38.5 nM. It demonstrates significant antiproliferative effects in various cancer cell lines, including HepG2, Huh7, H1299, and A549, with IC50 values of 2.03, 2.08, 4.79, and 17.11 μM, respectively. PLK1-IN-15 is known to induce cell cycle arrest at the G2/M phase and trigger apoptosis, underscoring its potential as an effective agent in cancer research and therapeutic development.

Cat. No.

A32222

CAS No.

2412707-81-2

WNY0824

Synonyms: PLK1/BRD4-IN-1

WNY0824 is a dual inhibitor targeting Polo-like kinase 1 (PLK1) and the Bromodomain and Extra-Terminal (BET) protein family. It demonstrates potent inhibitory activity, with IC50 values of 22 nmol/L for PLK1 and varying efficacy against BRD2, BRD3, BRD4, and BRDT. WNY0824 induces cell cycle arrest and apoptosis by disrupting AR- and MYC-mediated transcriptional processes, making it valuable for research in cancer biology. Furthermore, it has shown effectiveness in inhibiting tumor growth in Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential in overcoming treatment resistance.

Cat. No.

A32512

CAS No.

3016297-55-2

CZS-241

CZS-241 is a selective Polo-like Kinase 4 (PLK4) inhibitor, exhibiting an IC50 of 2.6 nM. In addition to its primary activity, CZS-241 also inhibits TRKA with an IC50 of 2.74 μM. This compound induces apoptosis and effectively arrests the cell cycle at the S/G2 phase. CZS-241 demonstrates potent antiproliferative effects against leukemia cell lines while maintaining safety profiles in normal cell lines, making it a valuable tool for cancer research.

Cat. No.

A32944

CAS No.

3068378-51-5

PLK1-IN-16

PLK1-IN-16 is a potent and selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 value of 0.25 nM. This compound is primarily utilized in cancer research due to its ability to induce G2 phase cell cycle arrest and promote apoptosis, displaying significant antiproliferative activity against various tumor cell lines. Additionally, PLK1-IN-16 has been shown to exhibit stability under simulated gastric acid conditions and presents manageable CYP 450 inhibition. Its applications extend to the study of triple-negative breast cancer (TNBC), breast cancer, and leukemia.

Cat. No.

A33010

CAS No.

1338799-83-9

Ocifisertib hydrochloride

Synonyms: CFI-400945 hydrochloride

Ocifisertib hydrochloride is a potent inhibitor of Polo-like kinase 4 (PLK4) with a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity by inhibiting the growth of various cancer cell lines, inducing cell cycle arrest at the G2/M phase, and promoting apoptosis. Research applications include evaluating its antitumor efficacy in preclinical models, making it a valuable reagent for studying mechanisms of cancer progression and potential therapeutic strategies.

Cat. No.

A36613

CAS No.

1239513-63-3

Poloxipan

Poloxipan is a pan-specific inhibitor targeting polo-like kinases (PLKs), specifically interfering with the Polo-box domain at the C-terminus. It demonstrates IC50 values of 3.2 μM, 1.7 μM, and 3.0 μM against PLK-1, PLK-2, and PLK-3, respectively. Additionally, Poloxipan inhibits various phospho-tyrosine binding domains, including the forkhead-associated domain of CHK-2 and the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1). This compound is valuable for applications in cancer research, particularly in studies involving PLK pathways and associated cellular processes.

Cat. No.

A39634

CAS No.

29115-34-2

MCC1019

MCC1019 is a selective inhibitor of the Polo-like kinase 1 (PLK1) phosphopeptide-binding domain (PBD), exhibiting an IC50 of 16.4 μmol/L. This compound effectively inactivates the AKT signaling pathway in cancer cells, leading to the induction of apoptosis, necroptosis, and autophagy. MCC1019 demonstrates significant anticancer activity against lung and prostate cancer, making it a valuable tool for cancer research and therapeutic studies.

Cat. No.

A40297

CAS No.

2251709-91-6

PLK1/BRD4-IN-3

PLK1/BRD4-IN-3 is a selective dual inhibitor targeting bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). This compound effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059 µM, 0.127 µM, and 0.245 µM, respectively. PLK1/BRD4-IN-3 can be employed in research applications focused on cancer biology, particularly in studies investigating cell proliferation and transcriptional regulation.

Cat. No.

A40319

CAS No.

2251709-89-2

PLK1/BRD4-IN-2

PLK1/BRD4-IN-2 is a dual inhibitor targeting both Polo-like kinase 1 (PLK1) and the bromodomain of BRD4, with an IC50 of 40 nM and 28 nM, respectively. This compound is valuable for research into cancer therapeutics and epigenetic regulation, demonstrating potential in studies focused on cell proliferation and transcriptional control. Its ability to simultaneously inhibit these key oncogenic pathways positions PLK1/BRD4-IN-2 as a crucial tool for advancing cancer research and drug discovery initiatives.

Cat. No.

A40813

CAS No.

2418614-81-8

PLK1/p38γ-IN-1

PLK1/p38γ-IN-1 is a multitarget inhibitor that selectively targets PLK1 and p38γ kinases. This compound has demonstrated the ability to inhibit cell proliferation in human hepatocellular carcinoma and hepatoblastoma cell lines in vitro. PLK1/p38γ-IN-1 is valuable for research focused on cancer biology and the modulation of cell cycle pathways.

Cat. No.

A44078

CAS No.

421586-94-9

8012–3246

8012-3246 is a selective inhibitor of Polo-like kinase 2 (PLK2) with an IC50 of 774.5 nM. This compound effectively suppresses the phosphorylation of GSK3β, demonstrating its potential role in cellular signaling modulation. Additionally, 8012-3246 exhibits significant anticancer activity, particularly against colorectal cancer, making it a valuable tool for cancer research applications focusing on PLK2-related pathways.

Cat. No.

A54996

CAS No.

13756-49-5

3,4,3'-Tri-O-methylflavellagic acid

3,4,3'-Tri-O-methylflavellagic acid is a flavonoid compound that functions as an inhibitor of polo-like kinase-1 (PLK-1) and αβ-tubulin at the colchicine binding site. This compound disrupts microtubule assembly dynamics and modulates kinase activity, making it valuable for research into cancer cell proliferation and anti-nociceptive properties. Its unique biological activities make it a significant reagent for studies focused on cancer therapies and pain management.

Cat. No.

A55070

CAS No.

1817791-70-0

TTK/PLK1-IN-1

TTK/PLK1-IN-1 is a potent inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), demonstrating IC50 values of 7 nM and 72 nM, respectively. This compound plays a crucial role in regulating the spindle assembly checkpoint (SAC), making it relevant for cancer research. It exhibits promising antitumor activity against triple-negative breast cancer (TNBC), contributing to its potential applications in oncology studies.

Cat. No.

A55088

CAS No.

929095-23-8

GSK461364 analogue 1

GSK461364 analogue 1 is a thiophene-based inhibitor targeting Polo-like kinase 1 (PLK1), exhibiting an IC50 value of 2 nM, along with inhibitory activity against PLK3 (IC50: 630 nM) and Nek2 kinase (IC50: 21 nM). With a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%, this compound is suitable for in vitro studies. GSK461364 analogue 1 is particularly relevant for research into malignancies such as colon, lung, breast, and ovarian cancers.

Cat. No.

A56886

CAS No.

667404-66-2

Y207–5465

Y207–5465 is a potent and highly selective inhibitor of Polo-like kinase 2 (PLK2), exhibiting an IC50 value of 584.3 nM. This compound demonstrates limited anti-cancer activity in human colorectal cancer cell lines HT-29 and HCT-116. It is suitable for use in cancer research, providing insights into the role of PLK2 in tumorigenesis and therapeutic resistance.

Cat. No.

A56887

CAS No.

1616420-30-4

Ocifisertib fumarate

Synonyms: CFI-400945 fumarate

Ocifisertib fumarate is a potent and selective inhibitor of Polo-like kinase 4 (PLK4), exhibiting a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity in the modulation of cell cycle progression and centrosome duplication. Ocifisertib fumarate is primarily utilized in research focused on cancer biology, particularly in studies assessing the role of PLK4 in tumorigenesis and potential therapeutic interventions targeting this kinase.

Cat. No.

A56889

CAS No.

1137212-79-3

Plogosertib

Synonyms: CYC140

Plogosertib is a selective and potent ATP-competitive inhibitor of the polo-like kinase 1 (PLK1) with an IC50 of 3 nM. This compound exhibits significant anti-proliferative activity, making it a valuable agent in cancer research. Plogosertib is applicable in studies involving various malignancies, including esophageal, gastric, leukemia, non-small cell lung cancer, ovarian, and squamous cell cancers.

Cat. No.

A56890

CAS No.

2980682-00-4

RP-1664

RP-1664 is a selective and orally active inhibitor of Polo-like kinase 4 (PLK4) with an IC50 of 3 nM. This compound exhibits remarkable selectivity toward PLK4 compared to related kinases such as AURKA, AURKB, and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells, resulting in the accumulation of PLK4 and p21 proteins. Its anti-tumor activity has been demonstrated in models of breast cancer and neuroblastoma, particularly in TRIM37-high-expressing cellular contexts.

Cat. No.

A56891

CAS No.

2923999-01-1

PLK4-IN-4

PLK4-IN-4 is a potent inhibitor of polo-like kinase 4 (PLK4), demonstrating an IC50 value of 7.9 nM. This compound effectively disrupts PLK4 activity, a critical regulator of centriole duplication, making it a valuable tool for cancer research. PLK4-IN-4 is suitable for studies investigating the role of PLK4 in tumorigenesis and may aid in the development of targeted cancer therapies.

Cat. No.

A56893

CAS No.

1247001-12-2

PLK4-IN-1

PLK4-IN-1 is a selective inhibitor of PLK4, exhibiting an IC50 of less than or equal to 0.1 μM. This compound plays a critical role in cell cycle regulation through the inhibition of polo-like kinase 4 activity. Its application is significant in research focusing on cell proliferation, cancer therapeutics, and understanding mitotic processes.

Cat. No.

A56894

CAS No.

40533-25-3

Cyclapolin 9

Cyclapolin 9 is a selective ATP-competitive inhibitor of polo-like kinase 1 (PLK1) with an IC50 of 500 nM. This compound demonstrates potent inhibition specifically against PLK1, making it a valuable tool for studying cell cycle regulation and cancer biology. Its selectivity and efficacy support research applications focused on tumorigenesis and targeted cancer therapies.

Cat. No.

A56895

CAS No.

35683-17-1

Dihydrobaicalein

Dihydrobaicalein is a selective PLK1 inhibitor, exhibiting an IC50 of 6.3 μM. This compound also demonstrates inhibitory activity against VRK2 and PLK2, making it a valuable tool in cancer research. Derived from the natural source Scutellaria scandens, dihydrobaicalein is utilized in studies exploring cell cycle regulation and mitotic processes. Its ability to modulate specific kinases positions it as a significant candidate for further investigation in therapeutic applications.