Pim-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Pim.html PimPim kinasesThe PIM kinase, also known as serine/threonine kinase plays an important role in cancer biology and is found in three differentisoforms namely PIM-1, PIM-2, and PIM-3. Pim kinases are mainly responsible for cell cycle regulation, antiapop

2、totic activity andthe homing and migration of receptor tyrosine kinases mediated via the JAK/STAT pathway.Pim kinases are over-expressed in various types of tumors and regulate the activation of signaling pathways that are important fortumor cell proliferation, survival and expression of drug efflux

3、 proteins. This makes Pim kinases attractive targets for thedevelopment of anti-cancer chemotherapeutic drugs.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Pim.html Pim HYPERLINK https:/www.MedChemE/Targets/Pim.html HYPERLINK https:/www.MedChemE/Targets/Pim.html Inhibitors HYPERLINK https:/ww

4、w.MedChemE/_1S,3R,5R_-PIM447-dihydrochloride.html (1S,3R,5R)-PIM447 HYPERLINK https:/www.MedChemE/_1S,3R,5R_-PIM447-dihydrochloride.html HYPERLINK https:/www.MedChemE/_1S,3R,5R_-PIM447-dihydrochloride.html dihydrochloride(1S,3R,5R)-LGH447 dihydrochloride) Cat. No.: HY-19322C HYPERLINK https:/www.Med

5、ChemE/_Z_-SMI-4a.html (Z)-SMI-4aCat. No.: HY-16576A(1S,3R,5R)-PIM447 (dihydrochloride) an PIMinhibitor extracted from patent US 20100056576 A1,compound example 72, has IC values of 0.095 M50for Pim1, 0.522 M for Pim2 and 0.369 M for Pim3.(Z)-SMI-4a is a poten, selective, cell-permeableand ATP-compet

6、itive Pim-1 inhibitor with anIC50 of 24 M and a Ki of 0.6 M. (Z)-SMI-4a alsoinhibits Pim-2 (IC of 100 M), and does not50significantly inhibit the other serine/threonine-or tyrosine-kinases.Purity: 98.13%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Re

7、portedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZD1208.html AZD1208 HYPERLINK https:/www.MedChemE/AZD1208.html HYPERLINK https:/www.MedChemE/AZD1208_hydrochloride.html AZD1208 HYPERLINK https:/www.MedChemE/AZD1208_hydrochloride.html HYPERLINK https:/www.MedChemE/AZD1208_hydrochloride.html hydr

8、ochlorideCat. No.: HY-15604 Cat. No.: HY-15604AAZD1208 is an orally bioavailable, highlyselective PIM kinases inhibitor.AZD1208 hydrochloride is an orally bioavailable,highly selective PIM kinases inhibitor.Purity: 99.90%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurit

9、y: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cdk6-pim1-in-1.html CDK6/PIM1-IN-1 HYPERLINK https:/www.MedChemE/cdk6-pim1-in-1.html HYPERLINK https:/www.MedChemE/ck2-erk8-in-1.html CK2/ERK8-IN-1Cat. No.: HY-142696 Cat. No.: HY-135906CDK6/PIM1-IN-1 is a potent and balanced

10、 dualCDK6/PIM1 inhibitor with IC values of 3950and 88 nM, respectively. CDK6/PIM1-IN-1inhibits CDK4 (IC =3.6 nM).50CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Kof 0.25 M) and ERK8 (MAPK15, ERK7) inhibitoriwith IC s of 0.50 M. CK2/ERK8-IN-1 also binds to50PIM1, HIPK2 (homeodomain-interacting prote

11、inkinase 2), and DYRK1A with Ks of 8.65 M, 15.25iM, and 11.9 M, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.82%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ck2-pim1-in-1.html CK2/PIM1-IN-1 HYPE

12、RLINK https:/www.MedChemE/ck2-pim1-in-1.html HYPERLINK https:/www.MedChemE/cx-6258.html CX-6258Cat. No.: HY-135816 Cat. No.: HY-18095CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1,with IC s of 3.787 M and 4.327 M for CK2 and50PIM1, respectively.CX-6258 is a potent and kinase selectivepan-Pim kinases

13、inhibitor, with IC s of 5 nM,5025 nM and 16 nM for Pim-1, Pim-2 and Pim-3,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/cx-6258-hydrochloride.

14、html CX-6258 HYPERLINK https:/www.MedChemE/cx-6258-hydrochloride.html HYPERLINK https:/www.MedChemE/cx-6258-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/cx-6258-hydrochloride.html HYPERLINK https:/www.MedChemE/CX-6258-hydrochloride-hydrate.html CX-6258 HYPERLINK https:/www.MedChemE

15、/CX-6258-hydrochloride-hydrate.html HYPERLINK https:/www.MedChemE/CX-6258-hydrochloride-hydrate.html hydrochloride HYPERLINK https:/www.MedChemE/CX-6258-hydrochloride-hydrate.html HYPERLINK https:/www.MedChemE/CX-6258-hydrochloride-hydrate.html hydrateCat. No.: HY-18095B Cat. No.: HY-18095ACX-6258 h

16、ydrochloride is a potent and kinaseselective pan-Pim kinases inhibitor, with IC s50of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 andPim-3, respectively.CX-6258 hydrochloride hydrate is a potent andkinase selective pan-Pim kinases inhibitor, withIC s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-250and Pim-3,

17、respectively.Purity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 98.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/GDC-0339.html GDC-0339

18、 HYPERLINK https:/www.MedChemE/GDC-0339.html HYPERLINK https:/www.MedChemE/GNE-955.html GNE-955Cat. No.: HY-16976 Cat. No.: HY-101783GDC-0339 is a potent, orally bioavailable and welltolerated pan-Pim kinase inhibitor, with Ks ofi0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 andPim3, respectively. GDC-

19、0339 is discovered as apotential treatment of multiple myeloma.GNE-955 is a potent and orally active pan Pimkinase inhibitor with Ks of 0.018, 0.11, 0.08 nMifor Pim1, Pim2, Pim3, respectively.Purity: 99.77%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data

20、: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Hispidulin.html Hispidulin(Dinatin) Cat. No.: HY-N1950 HYPERLINK https:/www.MedChemE/M-110.html M-110Cat. No.: HY-12830Hispidulin is a natural flavone with a broadspectrum of biological activities. Hispidulin is aPim-1 inhibitor

21、 with an IC of 2.71 M.50Purity: 99.34%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgM-110 is a highly selective, ATP-competitiveinhibitor of PIM kinases with a preference forPIM-3 (IC =47 nM). M-110 inhibits PIM-1 and50PIM-2 with similar IC s of 2.5 M. M-110 inhibits50the

22、 proliferation of prostate cancer cell lineswith IC s of 0.6 to 0.9 M.50Purity: 98.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/mnk-pim-in-1.html MNK/PIM-IN-1Cat. No.: HY-132867 HYPERLINK https:/www.MedChemE/PIM-447-dihydrochloride.html PIM-447

23、 HYPERLINK https:/www.MedChemE/PIM-447-dihydrochloride.html HYPERLINK https:/www.MedChemE/PIM-447-dihydrochloride.html dihydrochloride(LGH447 dihydrochloride) Cat. No.: HY-19322BMNK/PIM-IN-1 represents an innovative dualMNK/PIM inhibitor with a good pharmacokineticprofile.PIM447 dihydrochloride (LGH

24、447 dihydrochloride) isa potent, orally available, and selectivepan-PIM kinase inhibitor, with K values of 6,i18, and 9 pM for PIM1, PIM2, and PIM3,respectively. PIM447 dihydrochloride displays dualantimyeloma and bone-protective effects.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

25、 mgPurity: 99.27%Clinical Data: Phase 1Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/pim-in-1.html PIM-IN-1 HYPERLINK https:/www.MedChemE/pim-in-1.html HYPERLINK https:/www.MedChemE/PIM1-IN-1.html PIM1-IN-1Cat. No.: HY-142656 Cat. No.: HY-111552PIM-IN-1 is a pan-PI

26、M kinase inhibitor (KG-1,EC = 61 nM; pS6, .50 EC50 = 71 nM).PIM1-IN-1 is a potent and highly selectivePIM1/3 inhibitor, with IC s of 7, 5530 and 7050nM for PIM1, PIM2, and PIM3, respectively,inhibits the phosphorylation of BAD, a downstreamtarget of PIM, with an EC of 262 nM.50Purity: 98%Clinical Da

27、ta: No Development ReportedSize: 1 mg, 5 mgPurity: 99.51%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/pim1-in-2.html PIM1-IN-2 HYPERLINK https:/www.MedChemE/pim1-in-2.html HYPERLINK https:/www.MedChemE/Pim1-AKK1-IN-1.html Pim1/AKK1-IN-1C

28、at. No.: HY-108605(LKB1/AAK1 dual inhibitor) Cat. No.: HY-10371PIM1-IN-2 is a potent and ATP competitive Pim-1inhibitor with a K of 91 nM. PIM1-IN-2 targetsithe ATP-binding kinase hinge region not by formingclassical hydrogen bonds.Pim1/AKK1-IN-1 is a potent multi-kinase inhibitorwith K values of 35

29、 nM/53 nM/75 nM/380 nM fordPim1/AKK1/MST2/LKB1 respectively, and alsoinhibits MPSK1 and TNIK.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/PIM447.ht

30、ml PIM447(LGH447) Cat. No.: HY-19322 HYPERLINK https:/www.MedChemE/Quercetagetin.html Quercetagetin(6-Hydroxyquercetin) Cat. No.: HY-N4149PIM447 (LGH447) is a potent, orally available, andselective pan-PIM kinase inhibitor, with Kivalues of 6, 18, and 9 pM for PIM1, PIM2, andPIM3, respectively. PIM4

31、47 displays dualantimyeloma and bone-protective effects. PIM447induces apoptosis.Quercetagetin (6-Hydroxyquercetin) is a flavonoid.Quercetagetin is a moderately potent andselective, cell-permeable pim-1 kinaseinhibitor (IC , 0.34 M). Anti-inflammatory and50anticancer properties.Purity: 98%Clinical D

32、ata: Phase 1Size: 1 mg, 5 mgPurity: 99.24%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/r8-t198wt.html R8-T198wt HYPERLINK https:/www.MedChemE/r8-t198wt.html HYPERLINK https:/www.MedChemE/sel24-b489.html SEL24-B489Cat. No.: HY-P1404 Cat. No.: HY-12

33、0758R8-T198wt is a cell-permeable carboxyl-terminalp27Kip1 peptide exhibits anti-tumor activity byinhibiting Pim-1 kinase.SEL24-B489 is a potent, type I, orally active,dual PIM and FLT3-ITD inhibitor, with Kdvalues of 2 nM for PIM1, 2 nM for PIM2 and 3 nMfor PIM3, respectively.Purity: 98%Clinical Da

34、ta: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/SGI-1776.html SGI-1776Cat. No.: HY-13287 HYPERLINK https:/www.MedChemE/SMI-16a.html SMI-16a(PIM1/2 Kinase Inhibitor VI) Cat. No.: HY-101947SGI-1776 is an inhibit

35、or of Pim kinases, withIC s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and50-3, respectively.SMI-16a is a selective Pim kinase inhibitorwith IC values of 0.15, 0.02 and 48 M for Pim1,50Pim2 and PC3 cells, respectively.Purity: 99.23%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.7

36、0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/TCS-PIM-1-1.html TCS HYPERLINK https:/www.MedChemE/TCS-PIM-1-1.html HYPERLINK https:/www.MedChemE/TCS-PIM-1-1.html PIM-1 HYPERLINK https:/www.MedChemE/TCS-PIM-1-1.html HYPERLINK

37、https:/www.MedChemE/TCS-PIM-1-1.html 1 HYPERLINK https:/www.MedChemE/TCS-PIM-1-1.html HYPERLINK https:/www.MedChemE/TCS-PIM-1-4a.html TCS-PIM-1-4a(SC 204330) Cat. No.: HY-18086 (SMI-4a) Cat. No.: HY-16576TCS PIM-1 1 (SC 204330) is a potent, selective andATP-competitive Pim-1 kianse inhibitor with an

38、IC of 50 nM, displays good selectivity over50Pim-2 and MEK1/MEK2 (IC s 20000 nM).50TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinasesinhibitor that blocks mTORC1 activity viaactivation of AMPK. TCS-PIM-1-4a kills a widerange of both myeloid and lymphoid cell lines(IC values ranging from 0.8 M to 40 M).50Purity: 98.03%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/TP-3654.html TP-3654 HYPERLINK https:/www.MedChemE/TP-3654.html HYPERLINK