BMS 986165

BMS 986165

CAT N°: 33524
Price:

From €66.00 €56.10

BMS 986165 is an allosteric inhibitor of tyrosine kinase 2 (TYK2; IC50 = 0.2 nM for the recombinant TYK2 pseudokinase domain).{62105} It is selective for TYK2 over a panel of 249 protein and lipid kinases at 1 µM but does inhibit the JAK1 pseudokinase domain and bone morphogenetic protein receptor type II (BMPR2; IC50s = 1 and 193 nM, respectively). BMS 986165 inhibits IFN-?-induced phosphorylation of STAT1, -2, -3, and -5 in primary human peripheral blood mononuclear cells (PBMCs; IC50s = 1-6 nM). It also inhibits IL-12-induced production of IFN-? in human PBMCs (IC50 = 11 nM) and IL-12-induced phosphorylation of STAT4 in NK-92 cells (IC50 = 5 nM). BMS 986165 (1 and 10 mg/kg) reduces IL-12 and IL-18-induced production of IFN-? in mice. It inhibits IFN-regulated expression of IFIT3, IFIT1, and MX1, genes encoding innate antiviral response proteins, and reduces tubulointerstitial and glomerular nephritis in female NZB/W lupus-prone mice. BMS 986165 also inhibits anti-CD40 antibody-induced colitis and systemic wasting in mice.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 6-[(cyclopropylcarbonyl)amino]-4-[[2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl]amino]-N-(methyl-d3)-3-pyridazinecarboxamide
  • Correlated keywords
    • antiinflammatory BMS986165 TYK IL12 IL18 IFIT-3 IFIT-1
  • Product Overview:
    BMS 986165 is an allosteric inhibitor of tyrosine kinase 2 (TYK2; IC50 = 0.2 nM for the recombinant TYK2 pseudokinase domain).{62105} It is selective for TYK2 over a panel of 249 protein and lipid kinases at 1 µM but does inhibit the JAK1 pseudokinase domain and bone morphogenetic protein receptor type II (BMPR2; IC50s = 1 and 193 nM, respectively). BMS 986165 inhibits IFN-?-induced phosphorylation of STAT1, -2, -3, and -5 in primary human peripheral blood mononuclear cells (PBMCs; IC50s = 1-6 nM). It also inhibits IL-12-induced production of IFN-? in human PBMCs (IC50 = 11 nM) and IL-12-induced phosphorylation of STAT4 in NK-92 cells (IC50 = 5 nM). BMS 986165 (1 and 10 mg/kg) reduces IL-12 and IL-18-induced production of IFN-? in mice. It inhibits IFN-regulated expression of IFIT3, IFIT1, and MX1, genes encoding innate antiviral response proteins, and reduces tubulointerstitial and glomerular nephritis in female NZB/W lupus-prone mice. BMS 986165 also inhibits anti-CD40 antibody-induced colitis and systemic wasting in mice.

We also advise you

Any project? Any challenge? We are in!
Contact us

Headquarters:
Parc d’activités du Pas du Lac
10 bis avenue Ampère

78180 Montigny le Bretonneux
France

Call us
Information
My account
Follow us

Copyright © 2024 BERTIN BIOREAGENT. All rights reserved | Terms & conditions

Secure payment
Subscribe to our newsletter