PLK

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

PLK Products

Catalog No. Information Product Use Citations Product Validations
S1109

BI 2536

BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.

S2235

Volasertib (BI 6727)

Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.

S2758

Wortmannin (KY 12420)

Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.

S1362

Rigosertib (ON-01910)

Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with 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. Phase 3.

S2193

GSK461364

GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3. Phase 1.

S7837New

Centrinone (LCR-263)

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

S1485

HMN-214

HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.

S2898

MLN0905

MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.

S7248

Ro3280

RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

S5807

HMN-176

HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. HMN-176 effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure.

S7255

Onvansertib (NMS-P937)

Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.

S7552

CFI-400945

CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM.

S7720

SBE 13 HCl

SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3.

Catalog No. Information Product Use Citations Product Validations
S1109

BI 2536

BI-2536 is a potent Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. BI-2536 inhibits Bromodomain 4 (BRD4) with Kd of 37 nM and potently suppresses c-Myc expression. BI-2536 induces apoptosis and attenuates autophagy. Phase 2.

S2235

Volasertib (BI 6727)

Volasertib (BI 6727) is a highly potent Plk1 inhibitor with IC50 of 0.87 nM in a cell-free assay. It shows 6- and 65-fold greater selectivity against Plk2 and Plk3. Volasertib induces cell cycle arrest and apoptosis in various cancer cells. Phase 3.

S2758

Wortmannin (KY 12420)

Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.

S1362

Rigosertib (ON-01910)

Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with 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. Phase 3.

S2193

GSK461364

GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3. Phase 1.

S7837New

Centrinone (LCR-263)

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

S1485

HMN-214

HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.

S2898

MLN0905

MLN0905 is a potent inhibitor of PLK1 with IC50 of 2 nM.

S7248

Ro3280

RO3280 (Ro5203280) is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

S5807

HMN-176

HMN-176 is an active metabolite of HMN-214, which has a potent antitumor activity in mouse xenograft models. HMN-176 effectively inhibits PLK-1 by interference with its normal subcellular spatial distribution at centrosomes and along the cytoskeletal structure.

S7255

Onvansertib (NMS-P937)

Onvansertib (NMS-P937, PCM-075, NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Onvansertib (NMS-P937) potently causes a mitotic cell-cycle arrest followed by apoptosis in cancer cell lines and inhibits tumor growth. Phase 1.

S7552

CFI-400945

CFI-400945 is an orally active, potent and selective polo-like kinase 4(PLK4) inhibitor with Ki value of 0.26 nM.

S7720

SBE 13 HCl

SBE 13 HCl is a potent and selective PLK1 inhibitor with IC50 of 200 pM, >4000-fold selectivity over Aurora A kinase, Plk2 and Plk3.

Tags: PLK inhibition | PLK activation | PLK1 cancer | PLK1 phosphorylation | PLK1 pathway | PLK1 activation | PLK1 signaling | PLK1 kinase assay | PLK pathway | PLK inhibitors cancer | PLK1 inhibitor development | PLK inhibitor review