Polo-like Kinase (PLK) Inhibitor

PLK3 Human Pre-designed siRNA Set A contains three designed siRNAs for PLK3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

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

ZK-Thiazolidinone is an ATP-competitive Polo-like kinase 1 (Plk1) inhibitor with an IC₅₀ of 19 nM. ZK-Thiazolidinone inhibits tumor cell proliferation, induces cell cycle arrest and typical mitotic defects. ZK-Thiazolidinone impairs the recruitment of γ-tubulin and Aurora A kinase to centrosomes, resulting in failure of bipolar spindle maintenance and sister chromatid arm cohesion.\nZK-Thiazolidinone is applicable for cancer research.

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.

PLK4-IN-5 (compound 5f) is a PLK4 (IC₅₀ = 0.8 nM) inhibitor. PLK4-IN-5 can inhibit MCF-7 cell clone formation, induce cell cycle arrest (S/G2 phase), and apoptosis. PLK4-IN-5 has anti proliferative activity against MCF-7 cells (IC₅₀ = 0.48 μM). PLK4-IN-5 can be used in the research of cancer such as breast cancer.

(S)-BI 2536 is the enantiomer of BI 2536 (HY-50698). (S)-BI 2536 acts as an inhibitor of the BRD4 bromodomain and PLK1 kinase, with a K_i value of 54 nM against BRD4 and a K_i value of 0.42 nM against PLK1 kinase. (S)-BI 2536 exhibits anticancer activity against acute myeloid leukemia. (S)-BI 2536 can be used for the research of acute myeloid leukemia.

PLK3-IN-1 is a selective Polo-like kinase 3 (PLK3) inhibitor with a human PLK3 IC₅₀ of 5 nM. PLK3-IN-1 can be used for cancer research.

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.

Plk3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Plk3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

MLN0905 (Standard) is the analytical standard of MLN0905. This product is intended for research and analytical applications. 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.

Poloxipan is a pan-specific polo-like kinase (PLK) inhibitor that can inhibit a non-catalytic region at the C-terminus called the Polo-box domain (PBD) found in kinases. The IC₅₀ values for Poloxipan against the PBDs of PLK-1/2/3 are 3.2 μM, 1.7 μM, and 3.0 μM, respectively. Poloxipan also inhibits other phospho-tyrosine binding domains, such as the forkhead-associated (FHA) domain of CHK-2, the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1), and the phospho-tyrosine binding domains of STAT1/3/5 and lymphocyte-specific protein tyrosine kinase's SH2 domain. Poloxipan can be used in cancer research.

3MB-PP1 (Standard) is the analytical standard of 3MB-PP1 (HY-102069). This product is intended for research and analytical applications. 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.

PLK1-IN-16 is a selective polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 0.25 nM. PLK1-IN-16 exhibits lower inhibitory potency against PLK2 and PLK3, induces G2 phase cell cycle arrest, induces apoptosis, and exhibits antiproliferative activity against tumor cells. PLK1-IN-16 can be stable under simulated gastric acid environmental conditions, and acceptable CYP 450 inhibition. PLK1-IN-16 can be used for the study of triple-negative breast cancer (TNBC), breast cancer, leukemia.

PLK1-IN-17 is a potent PLK1 inhibitor with an IC₅₀ of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.

PLHSpT is an inhibitor of the Polo-box domain (PBD) of Polo-like kinase 1 (Plk1), with an IC₅₀ of 36 μM. It binds to the PB1-PB2 cleft of the Plk1 PBD to block its interaction with phosphoprotein substrates, thereby inducing mitotic arrest and apoptosis in tumor cells. PLHSpT exerts antiglioma effects when delivered via liposomes, and it is applicable to research on glioblastoma multiforme and other human cancers.

GW843682X (Standard) is the analytical standard of GW843682X (HY-11003). This product is intended for research and analytical applications. 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 K_inases.

IIP0943 is a selective inhibitor of PLK1 (polo-like kinase 1), with an IC₅₀ of 5.1 nM for PLK1. In addition, IIP0943 exhibits antiproliferative activity against HCT116 cells, with an IC₅₀ of 0.22 µM. These results suggest that IIP0943 holds promise for research in the field of cancer therapeutics.

Wrightiadione is a selective natural tetracyclic isoflavone kinase inhibitor with inhibitory activity against TrkA and PLK3. The IC₅₀ values of Wrightiadione against TrkA and PLK3 are 55.8 μM and 9.0 μM, respectively. Wrightiadione is found in the dried bark of Wrightia tomentosa. Wrightiadione can be used in studies of leukemia, kinase inhibition and cancer-related signaling pathways.

BDE30671203 is a highly selective PLK1 inhibitor (IC₅₀ = 2.163 nM). BDE30671203 induces G2/M phase arrest and Apoptosis. BDE30671203 downregulates key cell cycle regulators (CDC20, CDK1) and the anti-apoptotic gene Bcl-2. BDE30671203 exhibits anticancer activity against non-small cell lung cancer, large cell lung cancer, and liver 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.