MAP4K-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/MAP4K.html MAP4KMAPK Kinase Kinase KinaseMAP kinase kinase kinase kinases (MAP4Ks) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4Ksincluding MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K5/KHS, and MAP4K6/MINK have been repo

2、rted toinduce JNK activation through activating the MAP3K-MAP2K cascade. MAP4Ks play important roles in the regulation of cellapoptosis, cell survival, cell autophagy, and cell migration. Several studies reported that MAP4Ks are involved in the regulation ofimmune-cell responses through JNK-independ

3、ent pathways.MAP4K1/HPK1 and MAP4K4/HGK play negative roles in T-cell activation and inflammatory responses. In contrast, MAP4K3/GLKplays a positive role in T-cell activation and autoimmune responses. Moreover, MAP4K1 downregulation and MAP4K3overexpression in T cells are involved in human autoimmun

4、e diseases such as psoriatic arthritis, rheumatoid arthritis (RA),adult-onset Stills disease, and SLE.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/MAP4K.html MAP4K HYPERLINK https:/www.MedChemE/Targets/MAP4K.html HYPERLINK https:/www.MedChemE/Targets/MAP4K.html Inhibitors HYPERLINK https:/ww

5、w.MedChemE/DMX-5804.html DMX-5804 HYPERLINK https:/www.MedChemE/DMX-5804.html HYPERLINK https:/www.MedChemE/GNE_220.html GNE HYPERLINK https:/www.MedChemE/GNE_220.html HYPERLINK https:/www.MedChemE/GNE_220.html 220Cat. No.: HY-111754 Cat. No.: HY-U00428DMX-5804 is a potent, orally active and selecti

6、veMAP4K4 ICinhibitor, with an 50 of 3 nM, a pIC50of 8.55 for human MAP4K4, less potent onMINK1/MAP4K6 (pIC , 8.18), and TNIK/MAP4K750(pIC , 7.96).50GNE-220 is a potent and selective inhibitor ofMAP4K4 with an IC of 7 nM.50Purity: 99.63%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

7、 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/GNE_220_Hydrochloride.html GNE HYPERLINK https:/www.MedChemE/GNE_220_Hydrochloride.html HYPERLINK https:/www.MedChemE/GNE_220_Hydrochloride.html 220 HYPERLINK https:/www.MedChemE/GNE_220

8、_Hydrochloride.html HYPERLINK https:/www.MedChemE/GNE_220_Hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/GNE_220_Hydrochloride.html HYPERLINK https:/www.MedChemE/gne-1858.html GNE-1858Cat. No.: HY-U00428A Cat. No.: HY-135892GNE 220 (hydrochloride) is a potent and selectiveinhibitor o

9、f MAP4K4, with an IC of 7 nM.50GNE-1858 is a potent and ATP-competitivehematopoietic progenitor kinase-1 (HPK1)inhibitor, with IC s of 1.9 nM, 1.9 nM, and 4.550nM for wild-type and the active mimetic mutantsHPK1-TSEE and HPK1-SA, respectively.Purity: 98.33%Clinical Data: No Development ReportedSize:

10、 5 mg, 10 mg, 25 mgPurity: 99.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GNE-495.html GNE-495 HYPERLINK https:/www.MedChemE/GNE-495.html HYPERLINK https:/www.MedChemE/hpk1-in-10.html HPK1-IN-10Cat. No.: HY-100343 Cat. No.: HY-14

11、5036GNE-495 is a potent and selective MAP4K4inhibitor with an IC of 3.7 nM.50HPK1-IN-10 is potent inhibitor of HPK1. HPK1 is aserine/threonine protein kinase cloned fromhematopoietic progenitor cells and belongs to theMAP4K family of mammalian Ste-20-related proteinkinases.Purity: 99.68%Clinical Dat

12、a: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hpk1-in-11.html HPK1-IN-11 HYPERLINK https:/www.MedChemE/hpk1-in-11.html HYPERLINK https:/www.MedChemE/hpk1-in-12.html HPK1-IN-12Cat. No.: H

13、Y-145037 Cat. No.: HY-145038HPK1-IN-11 is potent inhibitor of HPK1. HPK1 is aserine/threonine protein kinase cloned fromhematopoietic progenitor cells and belongs to theMAP4K family of mammalian Ste-20-related proteinkinases.HPK1-IN-12 is potent inhibitor of HPK1. HPK1 is aserine/threonine protein k

14、inase cloned fromhematopoietic progenitor cells and belongs to theMAP4K family of mammalian Ste-20-related proteinkinases.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/hpk1-in-13.html H

15、PK1-IN-13 HYPERLINK https:/www.MedChemE/hpk1-in-13.html HYPERLINK https:/www.MedChemE/hpk1-in-14.html HPK1-IN-14Cat. No.: HY-145039 Cat. No.: HY-145040HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is aserine/threonine protein kinase cloned fromhematopoietic progenitor cells and belongs to theMAP4K fa

16、mily of mammalian Ste-20-related proteinkinases.HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is aserine/threonine protein kinase cloned fromhematopoietic progenitor cells and belongs to theMAP4K family of mammalian Ste-20-related proteinkinases.Purity: 98%Clinical Data: No Development ReportedSize:

17、1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/hpk1-in-15.html HPK1-IN-15 HYPERLINK https:/www.MedChemE/hpk1-in-15.html HYPERLINK https:/www.MedChemE/hpk1-in-16.html HPK1-IN-16Cat. No

18、.: HY-145041 Cat. No.: HY-145042HPK1-IN-15 is a potent and selective inhibitor ofHPK1. Hematopoietic progenitor kinase 1 (HPKl)originally cloned from hematopoietic progenitorcells is a member of MAP kinase kinase kinasekinases (MAP4Ks) family.HPK1-IN-16 is a potent and selective inhibitor ofHPK1. He

19、matopoietic progenitor kinase 1 (HPKl)originally cloned from hematopoietic progenitorcells is a member of MAP kinase kinase kinasekinases (MAP4Ks) family.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https

20、:/www.MedChemE/hpk1-in-17.html HPK1-IN-17 HYPERLINK https:/www.MedChemE/hpk1-in-17.html HYPERLINK https:/www.MedChemE/hpk1-in-18.html HPK1-IN-18Cat. No.: HY-145044 Cat. No.: HY-145045HPK1-IN-17 is a potent and selective inhibitor ofHPK1. Hematopoietic progenitor kinase 1 (HPKl)originally cloned from

21、 hematopoietic progenitorcells is a member of MAP kinase kinase kinasekinases (MAP4Ks) family.HPK1-IN-18 is a potent and selective inhibitor ofHPK1. Hematopoietic progenitor kinase 1 (HPKl)originally cloned from hematopoietic progenitorcells is a member of MAP kinase kinase kinasekinases (MAP4Ks) fa

22、mily.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/hpk1-in-19.html HPK1-IN-19 HYPERLINK https:/www.MedChemE/hpk1-in-19.html HYPERLINK https:/www.MedChemE/hpk1-in-20.html HPK1-IN-20Cat.

23、No.: HY-145107 Cat. No.: HY-145109HPK1-IN-19 is a hematopoietic progenitor kinase1 (HPK1) inhibitor extracted from patentWO2018102366A1 compound I-47.HPK1-IN-19 is a hematopoietic progenitor kinase1 (HPK1) inhibitor extracted from patentWO2020235902A1 compound 106.Purity: 98%Clinical Data: No Develo

24、pment ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hpk1-in-21.html HPK1-IN-21 HYPERLINK https:/www.MedChemE/hpk1-in-21.html HYPERLINK https:/www.MedChemE/hpk1-in-24.html HPK1-IN-24Cat. No.: HY-144073 Cat. No.: HY-144091HPK1-I

25、N-21 is a potent inhibitor of HPK1 kinaseinhibitor (Ki=0.8 nM), HPK1-IN-21 also has orallyactive.HPK1-IN-24 (example 51) is a hematopoieticprogenitor kinase 1 (HPK1) inhibitor with a K ofi100 nM. HPK1-IN-24 has the potentialfor cancer research.Purity: 98%Clinical Data: No Development ReportedSize: 1

26、 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/hpk1-in-25.html HPK1-IN-25 HYPERLINK https:/www.MedChemE/hpk1-in-25.html HYPERLINK https:/www.MedChemE/hpk1-in-26.html HPK1-IN-26Cat. No.: HY-144092 Cat. No.: HY-144093HPK1-IN-25 (example 94) is

27、a hematopoieticprogenitor kinase 1 (HPK1) inhibitor with aenzymatic activity IC of 129 nM.50HPK1-IN-25 has the potential forcancer research.HPK1-IN-26 is a HPK1 and GLK inhibitor extractedfrom patent WO2021254118A1 compound 1. HPK1-IN-26can be used for the research of animal pathogeninfection.Purity

28、: 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/hpk1-in-27.html HPK1-IN-27 HYPERLINK https:/www.MedChemE/hpk1-in-27.html HYPERLINK https:/www.MedChemE/hpk1-in-28.html HPK1-IN-28Ca

29、t. No.: HY-143868 Cat. No.: HY-143869HPK1-IN-27 is a potent inhibitor of HPK1. MAP4K1is also known as hematopoietic progenitor kinase 1(HPK1). MAP4K1 is a serine/threonine kinase andmember of the germinal center kinase family.HPK1-IN-28 is a potent inhibitor of HPK1.Hematopoietic progenitor kinase 1

30、 (HPK1) is anegative regulator of the activation response ofdendritic cells (DCs), T cells and B cells.HPK1-IN-28 enhances the bodys anti-tumorimmunity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/

31、www.MedChemE/hpk1-in-29.html HPK1-IN-29 HYPERLINK https:/www.MedChemE/hpk1-in-29.html HYPERLINK https:/www.MedChemE/hpk1-in-3.html HPK1-IN-3Cat. No.: HY-143870 Cat. No.: HY-138568HPK1-IN-29 is a potent inhibitor of HPK1.Hematopoietic progenitor kinase 1 (HPK1) is anegative regulator of the activatio

32、n response ofdendritic cells (DCs), T cells and B cells.HPK1-IN-29 enhances the bodys anti-tumorimmunity.HPK1-IN-3 is a potent and selectiveATP-competitive hematopoietic progenitor kinase1 (HPK1; MAP4K1) inhibitor with an IC of 0.2550nM. HPK1-IN-3 has IL-2 cellular potency with anEC of 108 nM in hum

33、an peripheral blood50mononuclear cells (PBMCs).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.53%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/hpk1-in-30.html HPK1-IN-30 HYPERLINK https:/www.MedChemE/hpk1-in-3

34、0.html HYPERLINK https:/www.MedChemE/hpk1-in-4.html HPK1-IN-4Cat. No.: HY-143871 Cat. No.: HY-138569HPK1-IN-30 is a potent inhibitor of HPK1. MAP4K1is also known as hematopoietic progenitor kinase 1(HPK1). MAP4K1 is a serine/threonine kinase andmember of the germinal center kinase family.HPK1-IN-4 (

35、comp 22) is a HPK1 (MAPK41)inhibitor (IC of 0.061 nM) as preclinical50immunotherapy tool compound.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.09%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/hpk1-in-7.html

36、HPK1-IN-7 HYPERLINK https:/www.MedChemE/hpk1-in-7.html HYPERLINK https:/www.MedChemE/hpk1-in-8.html HPK1-IN-8Cat. No.: HY-138742 Cat. No.: HY-132926HPK1-IN-7 is a potent, orally active HPK1(hematopoietic progenitor kinase 1, MAP4K1)inhibitor (IC =2.6 nM) with excellent family and50kinome selectivity

37、. HPK1-IN-7 shows selectivityagainst IRAK4 (59 nM) and GLK (140 nM).HPK1-IN-8 is an allosteric, inactiveconformation-selective inhibitor of full-lengthHPK1.Purity: 99.61%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize

38、: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/hpk1-in-9.html HPK1-IN-9 HYPERLINK https:/www.MedChemE/hpk1-in-9.html HYPERLINK https:/www.MedChemE/ky-05009.html KY-05009Cat. No.: HY-145035 Cat. No.: HY-124745HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is aserine/threonine protein

39、kinase cloned fromhematopoietic progenitor cells and belongs to theMAP4K family of mammalian Ste-20-related proteinkinases.KY-05009 is an ATP-competitive Traf2- andNck-interacting kinase (TNIK) inhibitor with a Kiof 100 nM. KY-05009 pharmacologically inhibitsTGF-1-induced epithelial-to-mesenchymaltr

40、ansition (EMT) in human lung adenocarcinomacells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 25 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/map4k4-i

41、n-3.html MAP4K4-IN-3 HYPERLINK https:/www.MedChemE/map4k4-in-3.html HYPERLINK https:/www.MedChemE/NCB-0846.html NCB-0846Cat. No.: HY-125012 Cat. No.: HY-100830MAP4K4-IN-3 (Compound 17) is a potent andselective MAP4K4 inhibitor with an IC of 14.950nM in kinase assay, an IC of 470 nM in cell50assay. A

42、ntidiabetic agent.NCB-0846 is an orally available TNIK inhibitor withan IC of 21nM.50Purity: 99.13%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.36%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/NG25.html NG25 HYPERLINK https:/www.MedChemE/NG25.html HYPERLINK https:/www.MedChemE/PF-06260933.html PF-06260933Cat. No.: HY-1543