PLK3 Inhibitor

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.

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.

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.

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC₅₀ of 0.31 μM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity.

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.

GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC₅₀ of 2 nM and a PLK3 IC₅₀ of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC₅₀: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian 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.

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.

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.

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.

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).

LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC₅₀s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.

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.

LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC₅₀s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research

PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC₅₀: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC₅₀: 12.72 nM) and PLK3 (IC₅₀: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML).

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.

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.

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).

YLT-11 is a potent, selective and orally active PLK4 inhibitor with K_d values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity.

PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC₅₀ of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC₅₀: >10000 nM) and PLK3 (IC₅₀: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research.