IFNAR-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/IFNAR.html IFNARInterferon-/ receptor; Interferon-alpha/beta receptorThe interferon-/ receptor (IFNAR) is composed of two subunits, IFNAR1 and IFNAR2, encoding transmembrane polypeptides.Type-I IFNs, interferon (IFN-) and interferon (IFN-), act through a shared

2、 receptor complex, IFNAR. Binding of type-I IFN toIFNAR1 will robustly activate Janus activated kinase-signal transducer and activator of transcription (JAK-STAT) signaling pathway.Aberrant activation of the type-I IFN response results in a spectrum of disorders called interferonopathies.Type-I IFN

3、response occurs when IFN-/ binds to their receptor complex, IFNAR. The ligand-receptor complex is phosphorylated,presumably by pre-associated Janus activated kinases (JAKs) namely tyrosine kinase 2 (TYK2) on IFNAR1 and JAK1 on IFNAR2. Thephosphorylated receptors are docking sites for signal transduc

4、ers and activators of transcription (STAT) factors that dimerise andtranslocate to the nucleus. STATs 1, 2, 3, 4, and 5 are activated by type-I IFNs in many cell types. Other kinases (e.g.,mitogen-activated protein kinases) and transcription factors (e.g., nuclear factor-B) can also be activated in

5、response to type-IIFNs. Multiple pathways and IFN-regulated genes are activated by IFNs, many of which remain unknown.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/IFNAR.html IFNAR HYPERLINK https:/www.MedChemE/Targets/IFNAR.html HYPERLINK https:/www.MedChemE/Targets/IFNAR.html Inhibitors, HY

6、PERLINK https:/www.MedChemE/Targets/IFNAR.html HYPERLINK https:/www.MedChemE/Targets/IFNAR.html Agonists, HYPERLINK https:/www.MedChemE/Targets/IFNAR.html HYPERLINK https:/www.MedChemE/Targets/IFNAR.html Activators, HYPERLINK https:/www.MedChemE/Targets/IFNAR.html HYPERLINK https:/www.MedChemE/Targe

7、ts/IFNAR.html Modulators HYPERLINK https:/www.MedChemE/Targets/IFNAR.html HYPERLINK https:/www.MedChemE/Targets/IFNAR.html & HYPERLINK https:/www.MedChemE/Targets/IFNAR.html HYPERLINK https:/www.MedChemE/Targets/IFNAR.html Inducers HYPERLINK https:/www.MedChemE/2-3-cgamp.html 2,3-cGAMP(2-3-cyclic GM

8、P-AMP) Cat. No.: HY-100564 HYPERLINK https:/www.MedChemE/2-3-cgamp-sodium.html 2,3-cGAMP HYPERLINK https:/www.MedChemE/2-3-cgamp-sodium.html HYPERLINK https:/www.MedChemE/2-3-cgamp-sodium.html sodium(2-3-cyclic GMP-AMP sodium) Cat. No.: HY-100564A2,3-cGAMP (2-3-cyclic GMP-AMP) is a endogenouscGAMP i

9、n mammalian cells. 2,3-cGAMP binds toSTING with a high affinity and is a potent inducerof interferon- (IFN). 2,3-cGAMP is produced inmammalian cells in response to DNA in thecytoplasm.2,3-cGAMP sodium (2-3-cyclic GMP-AMP sodium)is a endogenous cGAMP in mammalian cells.2,3-cGAMP sodium binds to STING

10、 with a highaffinity and is a potent inducer of interferon-(IFN). 2,3-cGAMP sodium is produced in mammaliancells in response to DNA in the cytoplasm.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.82%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK

11、https:/www.MedChemE/AX-024.html AX-024 HYPERLINK https:/www.MedChemE/AX-024.html HYPERLINK https:/www.MedChemE/AX-024_hydrochloride.html AX-024 HYPERLINK https:/www.MedChemE/AX-024_hydrochloride.html HYPERLINK https:/www.MedChemE/AX-024_hydrochloride.html hydrochlorideCat. No.: HY-107390 Cat. No.: H

12、Y-107390AAX-024 is an orally available, first-in-classinhibitor of the TCR-Nck interaction thatselectively inhibits TCR-triggered T cellactivation with an IC 1 nM. AX-024 modulates50cell signaling by targeting SH3 domains.AX-024 hydrochloride is an orally available,first-in-class inhibitor of the TC

13、R-Nckinteraction that selectively inhibitsTCR-triggered T cell activation with an IC 150nM. AX-024 hydrochloride modulates cell signalingby targeting SH3 domains.Purity: 98.0%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.12%Clinical Data: Phase 1Size: 10 mM 1 mL

14、, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CCCP.html CCCP HYPERLINK https:/www.MedChemE/CCCP.html (Carbonyl cyanide 3-chlorophenylhydrazone; CarbonylCyanide m-Chlorophenylhydrazone) Cat. No.: HY-100941 HYPERLINK https:/www.MedChemE/cirsilineol.html CirsilineolCat. No.: HY-1193

15、47CCCP is an oxidative phosphorylation (OXPHOS)uncoupler. CCCP induces activation of PINK1leading to Parkin Ser65 phosphorylation.Cirsilineol, a natural flavone compound,selectively inhibits IFN-/STAT1/T-bet signalingin intestinal CD4+ T cells. Cirsilineol haspotent immunosuppressive and anti-tumorp

16、roperties.Purity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg, 500 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CP-28888.html CP-28888 HYPERLINK https:/www.MedChemE/CP-28888.html HYPERLINK https:/www.MedChemE/cridanimod.

17、html Cridanimod(CP 28888-27) Cat. No.: HY-U00008Cat. No.: HY-W011890CP-28888 is an interferon inducer, more potent inmice, but is less active in man and devoid ofantirhinovirus effects.Cridanimod is a potent progesterone receptor (PR)activator mediated through induction of IFN andIFN expression. Cri

18、danimod is a small-moleculeimmunomodulator and interferon inducer.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BMS-986165.html Deucravacitinib HYPERLINK

19、https:/www.MedChemE/BMS-986165.html HYPERLINK https:/www.MedChemE/ginsenoside-f3.html Ginsenoside HYPERLINK https:/www.MedChemE/ginsenoside-f3.html HYPERLINK https:/www.MedChemE/ginsenoside-f3.html F3(BMS-986165) Cat. No.: HY-117287Cat. No.: HY-N0600Deucravacitinib (BMS-986165) is a highlyselective,

20、 orally bioavailable allosteric TYK2inhibitor for the treatment of autoimmunediseases, which selectively binds to TYK2pseudokinase (JH2) domain (IC =1.0 nM) and blocks50receptor-mediated Tyk2 activation byGinsenoside F3, a component of PPTGs (an minorsaponin in the leaves of Panax ginseng), hasimmun

21、oenhancing activity by regulating productionand gene expression of type 1 cytokines (IL-2,IFN-gamma) and type 2 cytokines (IL-4 and IL-10).Purity: 99.79%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mgPurity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1

22、mL, 1 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/gsk2245035.html GSK2245035 HYPERLINK https:/www.MedChemE/gsk2245035.html HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1.html IFN HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1.html HYPERLINK http

23、s:/www.MedChemE/IFN-alpha-IFNAR-IN-1.html alpha-IFNAR-IN-1Cat. No.: HY-118250 Cat. No.: HY-12836GSK2245035 is a highly potent and selectiveintranasal Toll-Like receptor 7 (TLR7) agonistwith preferential Type-1 interferon(IFN)-stimulating properties. GSK2245035 haspEC s of 9.3 and 6.5 for IFN and TFN

24、.50IFN alpha-IFNAR-IN-1 is a nonpeptidic,low-molecular-weight inhibitor of the interactionbetween IFN- and IFNAR; inhibit MVA-induced IFN-responses by BM-pDCs (IC50=2-8 uM).Purity: 99.79%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development Report

25、edSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1-hydrochloride.html IFN HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1-hydrochloride.html HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1-hydrochloride.html alpha-IFNAR-IN-1 HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1

26、-hydrochloride.html HYPERLINK https:/www.MedChemE/IFN-alpha-IFNAR-IN-1-hydrochloride.html hydrochlorideCat. No.: HY-12836A HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html IFN- HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html HYPERLINK https:/www

27、.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html Receptor HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html Recognition HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.

28、html HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html Peptide HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html HYPERLINK https:/www.MedChemE/ifn-alpha-receptor-recognition-peptide-1.html 1(IRRP1) Cat. No.: HY-P1758IFN alpha-IFNAR-IN-1 hydrochlori

29、de is anonpeptidic, low-molecular-weight inhibitor of theinteraction between IFN- and IFNAR; inhibitMVA-induced IFN- responses by BM-pDCs (IC50=2-8uM).IFN- Receptor Recognition Peptide 1 is a peptideof IFN- associated with receptor interactions.Purity: 99.76%Clinical Data: No Development ReportedSiz

30、e: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Interferon_receptor_agonist.html Interferon HYPERLINK https:/www.MedChemE/Interferon_receptor_agonist.html HYPERLINK https:/www.MedChemE/Interferon_receptor_agonis

31、t.html receptor HYPERLINK https:/www.MedChemE/Interferon_receptor_agonist.html HYPERLINK https:/www.MedChemE/Interferon_receptor_agonist.html inducer-1Cat. No.: HY-112189 HYPERLINK https:/www.MedChemE/ro8191.html RO8191(CDM-3008; RO4948191) Cat. No.: HY-W063968Interferon receptor inducer-1 (compound

32、 6) is aninterferon (IFN) receptor inducer. Used accordinglyin the treatment of a disorder in which theinduction of interferon is involved.RO8191 (CDM-3008), an imidazonaphthyridinecompound, is an orally active and potent interferon(IFN) receptor agonist. RO8191 directly binds toIFN/ receptor 2 (IFNAR2)