Polo-like-Kinase-PLK-Inhibitors-Modulators-生命科学试剂-MedChemExpress

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 againstother members of the PLK family (10 M).(1E)-CFI-400437 dihydrochloride inhibits Aurora A,Aurora B, KDR

8、 and FLT-3 with IC s of 0.37, 0.21,0.48, 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: No

9、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/bi-25

10、36.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 histoneH3 phosphorylation and

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

12、 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 applications.Centrinon

13、e (LCR-263) is a selective and reversibleinhibitor of polo-like kinase 4 (PLK4) with a Kof 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.MedChemE/Centrinon

14、e-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.CFI-400437 is an indolinone-derived

15、,ATP-competitive kinase inhibitor with highselectivity for PLK4 (IC of 0.6 nM).Purity: 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 Cyclapolin HYPERLIN

16、K 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-competitive polo

17、-like kinase 1 (PLK1)inhibitor with an IC of 500 nM. Cyclapolin 9 isinactive against other kinases.GSK461364 is a selective, reversible andATP-competitive Polo-like kinase 1 (PLK1)inhibitor with a K value of 2.2 nM.Purity: 96.13%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgPurity: 99.

18、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-13647GW843682X is

19、 a selective, ATP-competitiveinhibitor of PLK1 and PLK3, with IC s of 2.2 nMand 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 effect ontubulin polymer

20、ization. .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 HYPERLINK https:/ww

21、w.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 sof 2.5 M, 10 M and 61 M; LFM-A13 show

22、s 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.MedChemE/MLN0905.html MLN0905

23、(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 ICof 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 for Mps1Kdand a K of 61

24、nM for Plk1.Purity: 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.MedChemE/on1231320.html HYP

25、ERLINK 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.ON1231320 blocks tumor cell cycle progression inthe G2/M phase in mitosis, causing apoptotic cell

26、death. ON1231320, an arylsulfonylpyrido-pyrimidinone, has antitumor activity.NMS-1286937 is a potent, selective and orallyavailable PLK1 inhibitor, with an IC of 2 nM.Purity: 99.24%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.32%Clinical Data: Phase 2Size:

27、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 with an ICvalue of 0.384 M.PLK1

28、-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 https:/www.MedChemE/plk1-brd4-in-1

29、.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 and109 nM against PLK1 and BRD4, respectively.PLK4-IN-1 (Example A6) is a PLK4 inhibitor, withan IC of 0.1 M.

30、Purity: 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/poloppin.html PoloppinCat. No.: HY-1347

31、75A 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.Poloppin is a potent, cell penetrant inhibitor ofthe mitotic Polo-like kinase (PLK)(IC =26.9 M) and prevents theprotein-protein interaction via the Polo-boxdomai

32、n (PBD) (K = 29.5 M).Purity: 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 HYPERLINK https:/www.MedChemE/Poloxin.html Poloxin

33、Cat. 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, with an IC of appr 4.8 M.Purity: 95.0%Cli

34、nical 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.MedChemE/rigosertib.html HYPERLINK https:/www.M

35、edChemE/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-kinase inhibitorand a selective anti-cancer ag

36、ent, 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 induces apoptosis by inhibition thePI3K/Akt pat

37、hway, 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:/www.MedChemE/Ro3280.html Ro3280 HYPERLINK https

38、:/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 IC Kdwith an and a of 3 nM and 0.09 nM,respectively, and nearly has no effect on PLK2 andPLK3.SBE13 is a potent and selective Plk1 inhi

39、bitor,with an IC of 200 pM; SBE13 poorly inhibits Plk2(IC 66M) or Plk3 (IC =875nM).Purity: 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 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE

40、 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 HYPERLINK https:/www.MedChemE/TAK-960.html TAK-960Cat. No.:

41、 HY-15158 Cat. No.: HY-15160SBE13 Hydrochloride is a potent and selective Plk1inhibitor, with an IC of 200 pM; SBE13Hydrochloride poorly inhibits Plk2(IC 66M) or Plk3 (IC =875nM).TAK-960 is an orally available, selectiveinhibitor of polo-like kinase 1 (PLK1), with anIC of 0.8 nM. TAK-960 also shows

42、inhibitoryactivities against PLK2 and PLK3, with IC s of16.9 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, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/TAK-960_dihydrochlor

43、ide.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.MedChemE/TAK-960-hydrochloride.html TAK-960 HYPERLINK https:/www.MedC

44、hemE/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),with an IC of 0.8 nM. TAK-960 dihydrochloridealso shows inhibit

45、ory activities against PLK2 andPLK3, with IC s of 16.9 and 50.2 nM, respectively.TAK-960 hydrochloride is an orally available,selective inhibitor of polo-like kinase 1 (PLK1),with an IC of 0.8 nM. TAK-960 hydrochloride alsoshows inhibitory activities against PLK2 and PLK3,with IC s of 16.9 and 50.2

46、nM, respectively.Purity: 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 https:/www.MedChemE/tak-960-monohydrochloride.html HYPERLINK https:/www.Me

47、dChemE/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:/www.MedChemE/tc-s-7005.html 7005Cat. No.: HY-15160C Cat. No.: HY-108597

48、TAK-960 monohydrochloride is an orally available,selective inhibitor of polo-like kinase 1 (PLK1),with an IC of 0.8 nM. TAK-960 monohydrochloridealso shows inhibitory activities against PLK2 andPLK3, with IC s of 16.9 and 50.2 nM, respectively.TC-S 7005 is a Polo-like kinases (Plks) inhibitorwith IC s of 4 nM, 24 nM and 214 nM for Plk2,Plk3, and Plk1, respectively.Purit