plk3

Onvansertib (NMS-1286937) is a PLK1 inhibitor (IC50=2 nM) with high selectivity and oral activity. Onvansertib has antitumor activity and inhibits tumor growth.

BI2536 is an effective Plk1 inhibitor (IC50: 0.83 nM). It has 4- and 11-fold greater selectivity than Plk2 and Plk3.

SBE13 Hydrochloride (SBE 13 HCl) is an effective and specific PLK1 inhibitor (IC50: 0.2 nM); no inhibition om Aurora A kinase, Plk2 3.

T521 is a selective inhibitor of the PBD of Plk1 and shows no inhibitory effect on Plk2 and Plk3.

Plogosertib (CYC140) is an orally active, selective, potent, and ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.Plogosertib exhibits antiproliferative and anticancer activity and can be used for the study of solid and hematologic tumors. and hematologic tumors.

Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8 48 nM) that blocks autophagy.

AAPK-25 is a potent and selective Aurora PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A -B -C with Kd values ranging from 23-289 nM.

LFM-A13(IC50=2.5 μM), a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.

Volasertib (BI 6727) (BI-6727) is a potent inhibitor of PLK1 (IC50: 0.87 nM), inducing mitotic arrest and apoptosis. It also inhibits PLK2 PLK3 (IC50s: 5 56 nM).

GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM).

TC-S 7005 is an effective inhibitor of Polo-like kinases (IC50s: 214 nM, 4 nM and 24 nM for Plk1, Plk2, and Plk3).

Rigosertib sodium (ON-01910), a non-ATP-competitive inhibitor of PLK1(IC50=9 nM), exhibits 30-fold higher specificity activity over Plk2 and no effect on Plk3.

TAK-960 monohydrochloride is an orally available compound that selectively inhibits polo-like kinase 1 (PLK1) with an IC₅₀ of 0.8 nM. It also demonstrates inhibitory activity against PLK2 (IC₅₀ of 16.9 nM) and PLK3 (IC₅₀ of 50.2 nM), and effectively suppresses the proliferation of various cancer cell lines, exhibiting significant efficacy against multiple tumor xenografts.

PLK1-IN-6, a potent and selective inhibitor of PLK1, demonstrates significant anti-proliferative activities against cancer cells with an IC50 value of 0.45 nM [1].

ON1231320 (GBO-006) is a Polo-like kinase 2 (PLK2) inhibitor.

PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM).

TAK-960 hydrochloride is a potent, selective, orally active inhibitor of polo-like kinase 1 (PLK1) (IC50: 0.8 nM). TAK-960 hydrochloride inhibits the proliferation of a variety of tumour cell lines and significantly treats a variety of tumour xenografts.

TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.

WRIGHTIADIONE exhibits inhibitory effects on TrkA and PLK3 and acts as a foundational compound for the development of Trk inhibitors. The structure of WRIGHTIADIONE includes a unique tetracyclic isoflavone moiety, which contributes to its wide spectrum of biological activities.

ON-01910 is a non-ATP-competitive PLK1 inhibitor(IC50 of 9 nM, in a cell-free assay). It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Rigosertib inhibits PI3K Akt pathway and activates oxidative stress signals. Rigosertib induces apoptosis in various cancer cells.It is a synthetic benzyl styryl sulfone analogue with potential antineoplastic activity.

Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor targeting the polo-box domain (IC50: appr 4.8 μM).

Poloxipan is a potent and pan-specific PLK1 inhibitor. In vitro, Poloxipan has IC50 3.2 uM (Plk1); 1.7 uM (Plk2); and 3 uM (Plk3). Poloxipan showed minor inhibition over FHA dommain of Chk2, S2 domian of STAT1, STAT5b, Lck, etc.

TAK-960 dihydrochloride is an orally administered, selective polo-like kinase 1 (PLK1) inhibitor with a potent IC50 of 0.8 nM. It also targets PLK2 and PLK3 with IC50 values of 16.9 and 50.2 nM, respectively. This compound effectively inhibits the proliferation of a broad range of cancer cell lines and demonstrates substantial efficacy against various tumor xenografts.

YLT-11 is a potent, selective, and orally active inhibitor of polo-like kinase 4 (PLK4), with dissociation constant (Kd) values of >10000 nM for PLK1, 653 nM for PLK2, >10000 nM for PLK3, and 5.2 nM for PLK4. It demonstrates antiproliferative effects, induces apoptosis, and causes cell cycle arrest at the G2 M phase, highlighting its anticancer activity.