SGK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/SGK.html SGKSerum-glucocorticoid regulated kinase; Serum and glucocorticoid-regulated kinaseSerum- and glucocorticoid-inducible kinases (SGKs) form a novel family of serine/threonine kinases that are activated in responseto a variety of extracellular stimuli. S

2、GK family contains three isoforms: SGK1, SGK2, and SGK3. The mRNA encoding SGK1, thebest-studied member of the SGK family, is rapidly induced in response to a variety of stimuli, including growth factors, steroid andpeptide hormones, cytokines, changes in cell volume, and brain injury.SGKs are relat

3、ed to Akt (also called PKB), a serine/threonine kinase that plays a crucial role in promoting cell survival. The SGKfamily members share similar structure, substrate specificity and function with AKT and signal downstream of thephosphatidylinositol 3-kinase (PI3K) signalling pathway. They regulate a

4、 range of fundamental cellular processes such as cellproliferation and survival, thereby playing an important role in cancer development. In addition, SGKs not only regulate cellproliferation and survival, but also play important roles in cancer development via an AKT-independent signalling pathway.

5、 Theimportance of SGKs in cancer development and the scarcity of potent and selective SGK inhibitors support the urgent need fordiscovery and development of small molecules inhibitors targeting SGK for PIK3CA mutant cancers, and especially those that areresistant to AKT inhibition.www.MedChemE 1 HYP

6、ERLINK https:/www.MedChemE/Targets/SGK.html SGK HYPERLINK https:/www.MedChemE/Targets/SGK.html HYPERLINK https:/www.MedChemE/Targets/SGK.html Inhibitors HYPERLINK https:/www.MedChemE/cki7.html CKI-7 HYPERLINK https:/www.MedChemE/cki7.html HYPERLINK https:/www.MedChemE/cki-7.html CKI-7 HYPERLINK http

7、s:/www.MedChemE/cki-7.html HYPERLINK https:/www.MedChemE/cki-7.html free HYPERLINK https:/www.MedChemE/cki-7.html HYPERLINK https:/www.MedChemE/cki-7.html baseCat. No.: HY-W011109 Cat. No.: HY-133028CKI-7 is a potent and ATP-competitive casein kinase1 (CK1) ICinhibitor with an 50 of 6 M and a Kiof 8

8、.5 M. CKI-7 is a selective Cdc7 kinaseinhibitor. CKI-7 also inhibits SGK, ribosomalS6 kinase-1 (S6K1) and mitogen- andstress-activated protein kinase-1 (MSK1).CKI-7 free base is a potent and ATP-competitivecasein kinase 1 (CK1) inhibitor with an IC of 650M and a K of 8.5 M. CKI-7 free base is aisele

9、ctive Cdc7 kinase inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.31%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/EMD638683.html EMD638683 HYPERLINK https:/www.MedChemE/EMD638683.html HYP

10、ERLINK https:/www.MedChemE/EMD638683-R-Form.html EMD638683 HYPERLINK https:/www.MedChemE/EMD638683-R-Form.html HYPERLINK https:/www.MedChemE/EMD638683-R-Form.html R-FormCat. No.: HY-15193 Cat. No.: HY-15193AEMD638683 is a highly selective SGK1 inhibitor,with an IC value of 3 M.50EMD638683 R-Form is

11、the R-form of EMD638683.EMD638683 is a highly selective SGK1 inhibitorwith IC of 3 M.50Purity: 99.80%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www

12、.MedChemE/EMD638683-S-Form.html EMD638683 HYPERLINK https:/www.MedChemE/EMD638683-S-Form.html HYPERLINK https:/www.MedChemE/EMD638683-S-Form.html S-Form HYPERLINK https:/www.MedChemE/EMD638683-S-Form.html HYPERLINK https:/www.MedChemE/GSK-650394.html GSK HYPERLINK https:/www.MedChemE/GSK-650394.html

13、 HYPERLINK https:/www.MedChemE/GSK-650394.html 650394Cat. No.: HY-15193B Cat. No.: HY-15192EMD638683 S-Form is the S-form of EMD638683.EMD638683 is a highly selective SGK1 inhibitorwith IC of 3 M.50GSK 650394 is a novel SGK inhibitor with IC of5062 nM and 103 nM for SGK1 and SGK2 in the SPAassay res

14、pectively. GSK 650394 also inhibitsinfluenza virus replication.Purity: 99.95%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/hu7691.html Hu7691 HYP

15、ERLINK https:/www.MedChemE/hu7691.html HYPERLINK https:/www.MedChemE/hu7691-free-base.html Hu7691 HYPERLINK https:/www.MedChemE/hu7691-free-base.html HYPERLINK https:/www.MedChemE/hu7691-free-base.html free HYPERLINK https:/www.MedChemE/hu7691-free-base.html HYPERLINK https:/www.MedChemE/hu7691-free

16、-base.html baseCat. No.: HY-132302 Cat. No.: HY-132302AHu7691 is an orally active, selective Aktinhibitor with IC s of 4.0 nM, 97.5 nM, 28 nM for50Akt1, Akt2 and Akt3, respectively. Hu7691 inhibitstumor growth and enables decrease of cutaneoustoxicity in mice.Hu7691 free base is an orally active, se

17、lectiveAkt inhibitor with IC s of 4.0 nM, 97.5 nM, 2850nM for Akt1, Akt2 and Akt3, respectively. Hu7691free base inhibits tumor growth and enablesdecrease of cutaneous toxicity in mice.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedS

18、ize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pf-4950834.html PF-4950834 HYPERLINK https:/www.MedChemE/pf-4950834.html HYPERLINK https:/www.MedChemE/protac-sgk3-degrader-1.html PROTAC HYPERLINK https:/www.MedChemE/protac-sgk3-degrader-1.html HYPERLINK https:/www.MedChemE/protac-sgk3-degrader-1.html

19、SGK3 HYPERLINK https:/www.MedChemE/protac-sgk3-degrader-1.html HYPERLINK https:/www.MedChemE/protac-sgk3-degrader-1.html degrader-1Cat. No.: HY-122011(SGK3-PROTAC1) Cat. No.: HY-125878PF-4950834 is a potent, selective, orallybioavailable, ATP-competitive rho kinase inhibitorwith IC values of 8.35 nM

20、 and 33.12 nM against50ROCK2 and ROCK1, respectively. PF-4950834 inhibitsneutrophil migration.PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potentSKG3 degrader based on von Hippel-Lindau ligand.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.32%Clinical Data: No Development

21、 ReportedSize: 1 mg, 5 mg, 10 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/SGK1-IN-1.html SGK1-IN-1 HYPERLINK https:/www.MedChemE/SGK1-IN-1.html HYPERLINK https:/www.MedChemE/sgk1-in-2.html SGK1-IN-2Cat. No.: HY-18607 Cat. No.: HY-135893SGK1-IN-1 is a highly active and selectiveinhibitor of SGK-1, with an IC of 1 nM.50SGK1-IN-2 (14h) is a selective SGK1 (serum andglucocorticoid regulated kinase 1) inhibitor,with an IC of 5 nM at 10 M ATP concentration.50Purity: 98.76%Cli