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PLK1 Human Pre-designed siRNA Set A contains three designed siRNAs for PLK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Plk1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Plk1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Plk1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Plk1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
PLK1-IN-8 (compound TE6) is a PLK1 inhibitor, and inhibits cell proliferation by blocking the cell cycle at G2 phase. PLK1-IN-8 shows anticancer activity in vivo [1].
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 [1].
PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma [1].
PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1 and BRD4 inhibitor with IC50 values of 22 nM and 109 nM against PLK1 and BRD4, respectively. PLK1/BRD4-IN-1 induces cell cycle arrest and apoptosis, downregulates the transcription of several proliferation-related oncogenes, and exhibits favorable in vivo antitumor activity [1].
PLK1/BRD4-IN-5 (Compound SC10) is an orally active PLK1 and BRD4 inhibitor with IC50 values of 0.3 nM and 60.8 nM, respectively. PLK1/BRD4-IN-5 can induce MV4-11 cell block in S phase and apoptosis) in a dose-dependent manner. PLK1/BRD4-IN-5 can be used in cancer research [1].
PLK1/p38γ-IN-1(compound 14) is a multitarget inhibitors ofPLK1andp38γ.PLK1/p38γ-IN-1inhibits the growth of human hepatocellular carcinoma and hepatoblastoma cells in vitro [1].
PROTAC PLK1Degrader-1 (DD-2) is a potent PROTAC PLK1 degrader. PROTAC PLK1Degrader-1 selectively induces PLK1 degradation in cancer cells, including HeLa (DC50=2.5 μM) and nonsmall cell lung cancer (NSCLC), through the N-degron pathway [1].
Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1(PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases [1] .
Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1(Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division [1] .
MLN0905 is a potent, orally active Polo-like kinase 1(PLK1) inhibitor. MLN0905 has inhibitory potency against PLK1 with an IC50 value of 2 nM. MLN0905 can be used for the research of cancer [1] .
FOXM1-IN-1 is a potent FOXM1 inhibitor with an IC50 value of 2.65 µM. FOXM1-IN-1 shows antiproliferative activity. FOXM1-IN-1 decreases the the expression of FOXM1, PLK1, CDC25B protein [1].
CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC50: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer [1].
Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC50 and a Kd of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.
MDEG-541 is a potent MYC-MAX degrader. MDEG-541 is a PROTAC that based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide (HY-14658). MDEG-541 shows antiproliferative activity. MDEG-541 decreases the expression of GSPT1, MYC, GSPT2, PLK1 protein [1].
HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1(plk1), without significant effect on tubulin polymerization.
Dihydrobaicalein is a PLK1 Inhibitor with an IC50 of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens[1].
BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively [1]. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription .
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).
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.
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction[1].
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3 Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM [1].
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 [1] .
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 [1] .
CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1[1].
CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research [1].
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis[1].
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 [1] .
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle [1] . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
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 [1] .
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3K/Akt pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle [1] . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
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 [1].
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 [1].
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1(PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts [1].
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 [1].
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 [1].
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1(PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts [1].
WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 [1].
LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). LC-1-40 selectively inhibits MYCN-induced tumor growth in mouse models. LC-1-40 also induces nucleotide damage and apoptosis in MYCN-associated tumors. LC-1-40 can be used in cancer research [1]. (Red: NUDT1 binder; Blue: CRBN ligand; Black: Linker).
Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors [1].
Dihydrobaicalein is a PLK1 Inhibitor with an IC50 of 6.3 μM. Dihydrobaicalein also inhibits VRK2 and PLK2. Dihydrobaicalein is a natural product that can be isolated from Scutellaria scandens[1].
PLK1 is a serine/threonine protein kinase that centrally coordinates key functions during the M phase of the cell cycle. It regulates centrosome maturation, spindle assembly, cohesin removal, inactivates APC/C inhibitors, and controls mitotic exit and cytokinesis. PLK1 Protein, Human (sf9, His) is the recombinant human-derived PLK1 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of PLK1 Protein, Human (sf9, His) is 603 a.a., with molecular weight of ~66 kDa.
PLK1 Protein, the subject of the paragraph, is not mentioned in the provided text. If you would like a summary involving PLK1, please provide the relevant paragraph or information about PLK1. PLK1 Protein, Mouse (sf9, His) is the recombinant mouse-derived PLK1 protein, expressed by Sf9 insect cells, with N-His labeled tag. The total length of PLK1 Protein, Mouse (sf9, His) is 603 a.a., with molecular weight of ~65 kDa.
Phospho-PLK1 (Thr210) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 68 kDa, targeting to Phospho-PLK1(T210). It can be used for WB,ICC/IF,FC assays with tag free, in the background of Human.
PLK1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 68 kDa, targeting to PLK1. It can be used for WB, ICC/IF, IP assays with tag free, in the background of Human, Rat.
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint [1]. JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint [1]. JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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