plk4

Ocifisertib (CFI-400945 free base) is a potent, selective and orally active inhibitor of polo-like kinase 4 (PLK4; Ki value 0.26 nM; IC50 value 2.8 nM).

PLK4-IN-4 (compound 22), a potent inhibitor of PLK4, exhibits an IC50 value of 7.9 nM, suggesting its potential use in cancer research [1].

Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor with a Ki of 0.59 nM.

CFI-400437 is an ATP-competitive PLK4 inhibitor (IC50: 0.6 nM) and is an indolequinone derivative.

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

FMF-06-098-1 is a multitargeted depressant that promotes the degradation of various kinases including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].

CZS-241 is an orally active, selective Polo-like Kinase (PLK) 4 inhibitor with an IC 50 of 2.6 nM that also inhibits TRKA at an IC 50 of 2.74 μM. It induces apoptosis and causes cell cycle arrest at the S G2 phase, demonstrating potent antiproliferative effectiveness against leukemia cell lines while maintaining safety towards normal cell lines.

NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1 CDK1 levels, leading to G2 M cell cycle arrest and initiating apoptosis through caspase-9 caspase-3 cleavage.

Centrinone (LCR-263) (LCR-263) is a reversible inhibitor of polo-like kinase 4 (PLK4; Ki:0.16 nM).

DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in research on diseases or disorders caused by aberrant kinase activity [1].

Mps1-IN-2 is a potent, selective, and ATP-competitive inhibitor of both Mps1 and Plk1.

XMD8-92 is an effective and specific BMK1 ERK5 inhibitor (Kd: 80 nM).

SP27, a selective PROTAC, degrades PLK4 with a DC50 of 19.5 nM and may be utilized in breast cancer research [1].

CFI-400945 is an orally active, potent, and selective inhibitor of polo-like kinase 4.

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.

MPI-0479605 is an ATP competitive and selective inhibitor.

Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib. It is an orally bioavailable PLK4 inhibitor with a Ki of 0.26 nM and an IC50 of 2.8 nM. This compound inhibits the growth of multiple cancer cell types, causes cell cycle arrest at the G2 M phase, and induces apoptosis. In mouse models, Ocifisertib hydrochloride exhibits antitumor activity.

(1E)-CFI-400437 dihydrochloride (CFI-400437 dihydrochloride) is a selective and potent polo-like kinase 4 (PLK4) inhibitor.