PLK4 Inhibitor

Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a K_i of 0.16 nM.

CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a K_i and an IC₅₀ of 0.26 nM and 2.8 nM, respectively.

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.

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

CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a K_i and an IC₅₀ of 0.26 nM and 2.8 nM, respectively.

RP-1664 is a selective and orally active PLK4 inhibitor with an IC₅₀ of 3 nM. RP-1664 demonstrates exquisite selectivity over related kinases, including AURKA/B and PLK1. RP-1664 disrupts centriole biogenesis in cancer cells and leads an accumulation of PLK4 and p21 protein. RP-1664 demonstrates increased sensitivity in TRIM37-high-expressing cells or tumors. RP-1664 exhibits anti-tumor activity in breast cancer and neuroblastoma research^[1][2].

PLK4-IN-4 (compound 22) is a potent PLK4 inhibitor with an IC₅₀ value of 7.9 nM. PLK4-IN-4 has the potential for the research of cancer.

(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC₅₀= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC₅₀s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity.

CZS-241 is an orally active and selective inhibitor of Polo-like Kinase (PLK) 4 (IC₅₀=2.6 nM). CZS-241 inhibits TRKA with an IC₅₀ value of 2.74 μM. CZS-241 induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines.

Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a K_i and an IC₅₀ of 0.26 nM and 2.8 nM. Ocifisertib hydrochloride inhibits growth of various cancer cells, arrests cell cycles at G2/M phase, and induces apoptosis. Ocifisertib hydrochloride exhibits antitumor efficacy in mouse model.

CZL-S092 is a PLK4 inhibitor with an IC₅₀ value of 0.9 nM and excellent selectivity over other PLK4 family members (PLK1, PLK2, and PLK3). CZL-S092 exhibits anti-neuroblastoma activity in vitro (IMR-32 cells, IC₅₀ = 1.143 μM). CZL-S092 inhibits cell migration and halts the cell cycle and induces apoptosis. CZL-S092 can be used in studies of various cancers including neuroblastoma cancer.

PLK4-IN-6 (compound C05) is an PLK4 inhibitor (IC₅₀ < 0.1 nM). PLK4-IN-6 has anti proliferative activity against various tumor cells, such as IMR-32 (IC₅₀ = 0.948 μM), MCF-7 (IC₅₀ = 0.979 μM), H460 (IC₅₀ = 1.679 μM) cells. PLK4-IN-6 can significantly induce cell apoptosis and block the cell cycle. PLK4-IN-6 can be used for research on various types of cancer.

PLK4-IN-7 is a selective and orally active PLK4 inhibitor with an IC₅₀ value of 7.9 nM. PLK4-IN-7 exhibits potent antitumor activity and favorable metabolic stability. PLK4-IN-7 can be used for the research of tumors such as neuroblastoma.

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.

PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a spiro cyclopropyl indolinone compound and PLK4 inhibitor with inhibitory activity against Aurora A and Aurora B kinases .PLK4-IN-1 can be used for the research of cancer .