Polo-like-Kinase-PLK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html Polo-like HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html Kinase HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html HYPERLINK https:/w

2、ww.MedChemE/Targets/Polo-like Kinase (PLK).html (PLK)Polo-like Kinases (PLKs) are a group of highly conserved serine/threonine protein kinases that play a key role in processes such ascell division and checkpoint regulation of mitosis. In mammals, five PLKs (PLK 1-5) encompass diverse roles in centr

3、osomedynamics, spindle formation, intra S-phase and G2/M checkpoints, and DNA damage response.PLKs are characterized by their Polo-box domain, which mediates protein interactions. They are additionally controlled byphosphorylation, proteolysis, and transcription, depending on the biological context.

4、 PLKs are now recognized to link cell divisionto developmental processes and to function in differentiated cells.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html Polo-like HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html HYPERLINK https:/www.MedChemE/

5、Targets/Polo-like Kinase (PLK).html Kinase HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html (PLK) HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinase (PLK).html HYPERLINK https:/www.MedChemE/Targets/Polo-like Kinas

6、e (PLK).html Inhibitors HYPERLINK https:/www.MedChemE/1e-cfi-400437-dihydrochloride.html (1E)-CFI-400437 HYPERLINK https:/www.MedChemE/1e-cfi-400437-dihydrochloride.html HYPERLINK https:/www.MedChemE/1e-cfi-400437-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/1e-cfi-400437-dihyd

7、rochloride.html HYPERLINK https:/www.MedChemE/3mb-pp1.html 3MB-PP1Cat. No.: HY-132135 Cat. No.: HY-102069(1E)-CFI-400437 dihydrochloride is a potent PLK4(IC = 0.6 nM) inhibitor and selective against50other members of the PLK family (10 M).(1E)-CFI-400437 dihydrochloride inhibits Aurora A,Aurora B, K

8、DR and FLT-3 with IC s of 0.37, 0.21,500.48, and 0.18 M, respectively.3MB-PP1, a bulky purine analog, is a Polo-likekinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitoticprogression and cell division arise through targetPlk1 in in cells expressing analog-sensitive Plk1alleles.Purity: 98.89%Clinical Data:

9、 No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/aapk-25.html AAPK-25 HYPERLINK https:/www.MedChemE/aapk-25.html HYPERLINK https:/www.MedChemE/bi-2536.html BI HYPERLINK https:/www.MedChemE/b

10、i-2536.html HYPERLINK https:/www.MedChemE/bi-2536.html 2536Cat. No.: HY-126249 Cat. No.: HY-50698AAPK-25 is a potent and selective Aurora/PLK dualinhibitor with anti-tumor activity, which cancause mitotic delay and arrest cells in aprometaphase, reflecting by the biomarker histoneH3Ser10 phosphoryla

11、tion and followed by a surgein apoptosis.BI 2536 is a dual PLK1 and BRD4 inhibitor withIC s of 0.83 and 25 nM, respectively. BI-253650suppresses IFNB (encoding IFN-) genetranscription.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.95%Clinical Data: Phase 2Size: 10 mM 1 m

12、L, 5 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bto-1.html BTO-1Cat. No.: HY-112395 HYPERLINK https:/www.MedChemE/Centrinone.html Centrinone(LCR-263) Cat. No.: HY-18682BTO-1 is a Polo-like kinase (Plk) inhibitor. BTO-1is primarily used for phosphorylation anddephosphorylation application

13、s.Centrinone (LCR-263) is a selective and reversibleinhibitor of polo-like kinase 4 (PLK4) with a Kiof 0.16 nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.57%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChe

14、mE/Centrinone-B.html Centrinone-B HYPERLINK https:/www.MedChemE/Centrinone-B.html HYPERLINK https:/www.MedChemE/cfi-400437.html CFI-400437(LCR-323) Cat. No.: HY-18683Cat. No.: HY-120279ACentrinone-B (LCR-323) is a potent and highlyselective PLK4 inhibitor, with a K of 0.59 nM.iCFI-400437 is an indol

15、inone-derived,ATP-competitive kinase inhibitor with highselectivity for PLK4 (IC of 0.6 nM).50Purity: 98.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cyclapolin-9.html Cycl

16、apolin HYPERLINK https:/www.MedChemE/cyclapolin-9.html HYPERLINK https:/www.MedChemE/cyclapolin-9.html 9 HYPERLINK https:/www.MedChemE/cyclapolin-9.html HYPERLINK https:/www.MedChemE/gsk461364.html GSK461364Cat. No.: HY-15159(GSK461364A) Cat. No.: HY-50877Cyclapolin 9 is a potent, selective andATP-c

17、ompetitive polo-like kinase 1 (PLK1)inhibitor with an IC of 500 nM. Cyclapolin 9 is50inactive against other kinases.GSK461364 is a selective, reversible andATP-competitive Polo-like kinase 1 (PLK1)inhibitor with a K value of 2.2 nM.iPurity: 96.13%Clinical Data: No Development ReportedSize: 10 mM 1 m

18、L, 5 mgPurity: 99.82%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/GW843682X.html GW843682X(GW843682) Cat. No.: HY-11003 HYPERLINK https:/www.MedChemE/HMN-176.html HMN-176Cat. No.: HY

19、-13647GW843682X is a selective, ATP-competitiveinhibitor of PLK1 and PLK3, with IC s of 2.2 nM50and 9.1 nM, respectively, and is also 100-foldselective against 30 other kinases.HMN-176 is a stilbene derivative whichinhibits mitosis, interfering with polo-likekinase-1 (plk1), without significant effe

20、ct ontubulin polymerization. .Purity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/HMN-214.html HMN-214(IVX-214) Cat. No.: HY-12045

21、 HYPERLINK https:/www.MedChemE/LFM-A13.html LFM-A13Cat. No.: HY-18009HMN-214, an orally bioavailable prodrug ofHMN-176, is an inhibitor of polo-like kinase-1(plk1), with antitumor activity.LFM-A13 is a potent BTK, JAK2, PLK inhibitor,inhibits recombinant BTK, Plx1 and PLK3 with IC s50of 2.5 M, 10 M

22、and 61 M; LFM-A13 shows noeffects on JAK1 and JAK3, Src family kinase HCK,EGFR and IRK.Purity: 99.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChem

23、E/MLN0905.html MLN0905(PLK1 Inhibitor) Cat. No.: HY-15155 HYPERLINK https:/www.MedChemE/Mps1-IN-2.html Mps1-IN-2Cat. No.: HY-13994MLN0905 is a potent PLK1 inhibitor, with an IC50of 2 nM.Mps1-IN-2 is a potent, selective andATP-competitive dual Mps1/Plk1 inhibitor, withan IC and a of 145 nM and 12 nM

24、for Mps150 Kdand a K of 61 nM for Plk1.dPurity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.15%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/on1231320.html ON1231320 HYPERLINK https:/www

25、.MedChemE/on1231320.html HYPERLINK https:/www.MedChemE/NMS-1286937.html OnvansertibCat. No.: HY-100789(NMS-1286937; NMS-P937) Cat. No.: HY-15828ON1231320 is a highly specific polo like kinase 2(PLK2) inhibitor with an IC of 0.31 M.50ON1231320 blocks tumor cell cycle progression inthe G2/M phase in m

26、itosis, causing apoptotic celldeath. ON1231320, an arylsulfonylpyrido-pyrimidinone, has antitumor activity.NMS-1286937 is a potent, selective and orallyavailable PLK1 inhibitor, with an IC of 2 nM.50Purity: 99.24%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99

27、.32%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/plk1-in-2.html PLK1-IN-2 HYPERLINK https:/www.MedChemE/plk1-in-2.html HYPERLINK https:/www.MedChemE/plk1-in-4.html PLK1-IN-4Cat. No.: HY-139652 Cat. No.: HY-146792PLK1-IN-2 is a PLK1 kinase inhibitor

28、 with an IC50value of 0.384 M.PLK1-IN-4 is a potent and selective PLK1inhibitor with IC 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/plk1-brd4-in-1.html PLK1/BRD4-IN-1 HYPERLINK

29、https:/www.MedChemE/plk1-brd4-in-1.html HYPERLINK https:/www.MedChemE/plk4-in-1.html PLK4-IN-1Cat. No.: HY-143471 Cat. No.: HY-134775PLK1/BRD4-IN-1 (9b) is an orally active dual PLK1and BRD4 inhibitor with IC values of 22 nM and50109 nM against PLK1 and BRD4, respectively.PLK4-IN-1 (Example A6) is a

30、 PLK4 inhibitor, withan IC of 0.1 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/plk4-in-3.html PLK4-IN-3 HYPERLINK https:/www.MedChemE/plk4-in-3.html HYPERLINK https:/www.MedChemE/p

31、oloppin.html PoloppinCat. No.: HY-134775A Cat. No.: HY-124761PLK4-IN-3 is a less active absolutestereochemistry of PLK4-IN-1. PLK4-IN-1 is a PLK4inhibitor, with an IC of 0.65 M.50Poloppin is a potent, cell penetrant inhibitor ofthe mitotic Polo-like kinase (PLK)(IC =26.9 M) and prevents the50protein

32、-protein interaction via the Polo-boxdomain (PBD) (K = 29.5 M).dPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Poloxime.html Poloxime HYPERLINK https:/www.MedChemE/Poloxime.html HYPERLI

33、NK https:/www.MedChemE/Poloxin.html PoloxinCat. No.: HY-77195 Cat. No.: HY-12134Poloxime, a hydrolysis product of poloxin, is anon-ATP-competitive Plk1 inhibitor, with moderatePlk1 inhibitory activity.Poloxin is a non-ATP competitive Polo-like Kinase 1(PLK1) inhibitor that targets the polo-boxdomain

34、, with an IC of appr 4.8 M.50Purity: 95.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 500 mg, 1 gPurity: 98.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/rigosertib.html Rigosertib HYPERLINK https:/www.Me

35、dChemE/rigosertib.html HYPERLINK https:/www.MedChemE/Rigosertib-sodium.html Rigosertib HYPERLINK https:/www.MedChemE/Rigosertib-sodium.html HYPERLINK https:/www.MedChemE/Rigosertib-sodium.html sodium(ON-01910) Cat. No.: HY-12037A (ON-01910 sodium) Cat. No.: HY-12037Rigosertib (ON-01910) is a multi-k

36、inase inhibitorand a selective anti-cancer agent, which inducesapoptosis by inhibition the PI3 kinase/Akt pathway,promots the phosphorylation of histone H2AX andinduces G2/M arrest in cell cycle.Rigosertib sodium (ON-01910 sodium) is amulti-kinase inhibitor and a selective anti-canceragent, which in

37、duces apoptosis by inhibition thePI3K/Akt pathway, promotes the phosphorylation ofhistone H2AX and induces G2/M arrest in cellcycle.Purity: 98.81%Clinical Data: Phase 3Size: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.49%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/ww

38、w.MedChemE/Ro3280.html Ro3280 HYPERLINK https:/www.MedChemE/Ro3280.html HYPERLINK https:/www.MedChemE/SBE13.html SBE13Cat. No.: HY-15161 Cat. No.: HY-15158ARo3280 is a potent, highly selective inhibitor ofPLK1 IC50 Kdwith an and a of 3 nM and 0.09 nM,respectively, and nearly has no effect on PLK2 an

39、dPLK3.SBE13 is a potent and selective Plk1 inhibitor,with an IC of 200 pM; SBE13 poorly inhibits Plk250(IC 66M) or Plk3 (IC =875nM).50 50Purity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Te

40、l: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/SBE13-Hydrochloride.html SBE13 HYPERLINK https:/www.MedChemE/SBE13-Hydrochloride.html HYPERLINK https:/www.MedChemE/SBE13-Hydrochloride.html Hydrochloride HYPERLINK https:/www.MedChemE/SBE13-Hydrochloride.html HYPER

41、LINK https:/www.MedChemE/TAK-960.html TAK-960Cat. No.: HY-15158 Cat. No.: HY-15160SBE13 Hydrochloride is a potent and selective Plk1inhibitor, with an IC of 200 pM; SBE1350Hydrochloride poorly inhibits Plk2(IC 66M) or Plk3 (IC =875nM).50 50TAK-960 is an orally available, selectiveinhibitor of polo-l

42、ike kinase 1 (PLK1), with anIC of 0.8 nM. TAK-960 also shows inhibitory50activities against PLK2 and PLK3, with IC s of5016.9 and 50.2 nM, respectively.Purity: 98.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 95.44%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg,

43、 50 mg, 100 mg HYPERLINK https:/www.MedChemE/TAK-960_dihydrochloride.html TAK-960 HYPERLINK https:/www.MedChemE/TAK-960_dihydrochloride.html HYPERLINK https:/www.MedChemE/TAK-960_dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/TAK-960_dihydrochloride.html HYPERLINK https:/www.MedC

44、hemE/TAK-960-hydrochloride.html TAK-960 HYPERLINK https:/www.MedChemE/TAK-960-hydrochloride.html HYPERLINK https:/www.MedChemE/TAK-960-hydrochloride.html hydrochlorideCat. No.: HY-15160B Cat. No.: HY-15160ATAK-960 dihydrochloride is an orally available,selective inhibitor of polo-like kinase 1 (PLK1

45、),with an IC of 0.8 nM. TAK-960 dihydrochloride50also shows inhibitory activities against PLK2 andPLK3, with IC s of 16.9 and 50.2 nM, respectively.50TAK-960 hydrochloride is an orally available,selective inhibitor of polo-like kinase 1 (PLK1),with an IC of 0.8 nM. TAK-960 hydrochloride also50shows

46、inhibitory activities against PLK2 and PLK3,with IC s of 16.9 and 50.2 nM, respectively.50Purity: 99.81%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/tak-960-monohydrochloride.html TAK-960 HYPERLINK h

47、ttps:/www.MedChemE/tak-960-monohydrochloride.html HYPERLINK https:/www.MedChemE/tak-960-monohydrochloride.html monohydrochloride HYPERLINK https:/www.MedChemE/tak-960-monohydrochloride.html HYPERLINK https:/www.MedChemE/tc-s-7005.html TC-S HYPERLINK https:/www.MedChemE/tc-s-7005.html HYPERLINK https

48、:/www.MedChemE/tc-s-7005.html 7005Cat. No.: HY-15160C Cat. No.: HY-108597TAK-960 monohydrochloride is an orally available,selective inhibitor of polo-like kinase 1 (PLK1),with an IC of 0.8 nM. TAK-960 monohydrochloride50also shows inhibitory activities against PLK2 andPLK3, with IC s of 16.9 and 50.2 nM, respectively.50TC-S 7005 is a Polo-like kinases (Plks) inhibitorwith IC s of 4 nM, 24 nM and 214 nM for Plk2,50Plk3, and Plk1, respectively.Purity: