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PLK4 inhibitor

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18682
    Centrinone
    Maximum Cited Publications
    32 Publications Verification

    LCR-263

    		 Polo-like Kinase (PLK) Cancer
    Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
    Centrinone
  • HY-12300
    Ocifisertib
    4 Publications Verification

    CFI-400945 free base

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    CFI-400945 free base is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.
    Ocifisertib
  • HY-14443
    XMD8-92
    10+ Cited Publications

    		 Epigenetic Reader Domain ERK TNK1 CaMK Cancer
    XMD8-92 is a potent ERK5 (BMK1)/BRD4 inhibitor with Kds of 80 and 190 nM, respectively. XMD8-92 inhibits DCAMKL2, PLK4 and TNK1 with Kds of 190, 600 and 890 nM, respectively. Anti-cancer activity .
    XMD8-92
  • HY-18683
    Centrinone-B
    5+ Cited Publications

    LCR-323

    		 Polo-like Kinase (PLK) Cancer
    Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.
    Centrinone-B
  • HY-172737
    RP-1664

    		Polo-like Kinase (PLK) Cancer
    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].
    RP-1664
  • HY-134775
    PLK4-IN-1

    		Polo-like Kinase (PLK) Cancer
    PLK4-IN-1 (Example A6) is a PLK4 inhibitor, with an IC50 of ≤ 0.1 μM .
    PLK4-IN-1
  • HY-12300B
    Ocifisertib fumarate
    4 Publications Verification

    CFI-400945 fumarate

    		 Polo-like Kinase (PLK) Cancer
    CFI-400945 fumarate is a potent, selective and orally bioavailable PLK4 inhibitor with a Ki and an IC50 of 0.26 nM and 2.8 nM, respectively.
    Ocifisertib fumarate
  • HY-128493
    PLK4-IN-4

    		Polo-like Kinase (PLK) Cancer
    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 .
    PLK4-IN-4
  • HY-15800A
    CZC-25146

    		TNK1 LRRK2 Neurological Disease Inflammation/Immunology
    CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases .
    CZC-25146
  • HY-132135
    (1E)-CFI-400437 dihydrochloride

    		Polo-like Kinase (PLK) 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 .
    (1E)-CFI-400437 dihydrochloride
  • HY-149912
    CZS-241

    		Polo-like Kinase (PLK) Trk Receptor Apoptosis Cancer
    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 .
    CZS-241
  • HY-176734
    CZL-S092

    		Polo-like Kinase (PLK) Cancer
    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 .
    CZL-S092
  • HY-179149
    PLK4-IN-6

    		Polo-like Kinase (PLK) Apoptosis 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-6
  • HY-115589
    YLT-11

    		Polo-like Kinase (PLK) Apoptosis Cancer
    YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd 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 .
    YLT-11
  • HY-134775A
    PLK4-IN-3

    		Polo-like Kinase (PLK) Cancer
    PLK4-IN-3 is a less active absolute stereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4 inhibitor, with an IC50 of 0.65 μM .
    PLK4-IN-3
  • HY-120279A
    CFI-400437

    		Polo-like Kinase (PLK) Cancer
    CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM) .
    CFI-400437
  • HY-12300A
    Ocifisertib hydrochloride

    CFI-400945 hydrochloride

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    Ocifisertib hydrochloride (CFI-400945 hydrochloride) is the hydrochloride salt form of Ocifisertib (HY-12300). Ocifisertib hydrochloride is an orally active PLK4 inhibitor with a Ki 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 .
    Ocifisertib hydrochloride
  • HY-149912A
    CZS-241 hydrochloride

    		Polo-like Kinase (PLK) Trk Receptor Apoptosis Cancer
    CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 (PLK4) (IC50=2.6 nM). CZS-241 hydrochloride inhibits TRKA with an IC50 value of 2.74 μM. CZS-241 hydrochloride induces apoptosis and arrests cell cycle at S/G2 phase. CZS-241 hydrochloride shows highly potent antiproliferative activity against leukemia cell lines, and exhibits safety against normal cell lines .
    CZS-241 hydrochloride
  • HY-15800
    CZC-25146 hydrochloride

    		TNK1 LRRK2 Neurological Disease Inflammation/Immunology
    CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases .
    CZC-25146 hydrochloride
  • HY-180111
    PLK4-IN-7

    		Polo-like Kinase (PLK) Neurological Disease 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 .
    PLK4-IN-7
  • HY-116190
    CFI-401870

    		Mps1 DNA/RNA Synthesis Cancer
    CFI-401870 is an orally active threonine tyrosine kinase (TTK (Mps1)) inhibitor with an IC50 of 3.1 nM. CFI-401870 exhibits IC50s against PLK4, KDR, AURKA and other kinases such as AURKB/INCENP were all greater than 1 μM.CFI-401870 inhibits the growth of various cancer cells, causing chromosome lag, an increase in aneuploidy and cell cycle arrest. CFI-401870 can be used for the study of cancers such as colon cancer .
    CFI-401870
  • HY-179103
    PLK4-IN-5

    		Polo-like Kinase (PLK) Apoptosis Cancer
    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 .
    PLK4-IN-5
  • HY-162895
    NL13

    		Polo-like Kinase (PLK) Akt CDK Caspase Apoptosis Cancer
    NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC50 value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC50 values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth .
    NL13

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