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Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms.
Constitutive JAK2 activation in hematopoietic cells by the JAK2V617F mutation recapitulates myeloproliferative neoplasm (MPN) phenotypes in mice, establishing JAK2 inhibition as a potential… Expand
Treatment methods for the remediation of nitroaromatic explosives.
The production and use of nitroaromatic explosives for military operations have resulted in their dissemination into the environment, where their presence in waterways and soil poses an ecological… Expand
Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050
Inhibiting signal transduction induced by inflammatory cytokines offers a new approach for the treatment of autoimmune diseases such as rheumatoid arthritis. Kinase inhibitors have shown promising… Expand
Metabolism, Excretion, and Pharmacokinetics of [14C]INCB018424, a Selective Janus Tyrosine Kinase 1/2 Inhibitor, in Humans
- A. Shilling, Frank M Nedza, +11 authors S. Yeleswaram
- Biology, Medicine
- Drug Metabolism and Disposition
- 1 November 2010
The metabolism, excretion, and pharmacokinetics of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile (INCB018424), a potent, selective inhibitor of Janus tyrosine… Expand
Preclinical evaluation of local JAK1 and JAK2 inhibition in cutaneous inflammation.
- J. Fridman, P. Scherle, +16 authors K. Vaddi
- The Journal of investigative dermatology
- 1 September 2011
JAKs are required for signaling initiated by several cytokines (e.g., IL-4, IL-12, IL-23, thymic stromal lymphopoietin (TSLP), and IFNγ) implicated in the pathogenesis of inflammatory skin diseases… Expand
Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction.
An enantioselective synthesis of INCB018424 via organocatalytic asymmetric aza-Michael addition of pyrazoles (16 or 20) to (E)-3-cyclopentylacrylaldehyde (23) using diarylprolinol silyl ether as the… Expand
Downmodulation of key inflammatory cell markers with a topical Janus kinase 1/2 inhibitor
- N. Punwani, T. Burn, +14 authors A. Gottlieb
- The British journal of dermatology
- 1 October 2015
INCB018424 is a novel, potent Janus kinase (JAK)1/JAK2 inhibitor that blocks signal transduction of multiple proinflammatory cytokines.
Inhibition of clinically relevant mutant variants of HIV-1 by quinazolinone non-nucleoside reverse transcriptase inhibitors.
- J. W. Corbett, S. Ko, +12 authors S. Erickson-Viitanen
- Chemistry, Medicine
- Journal of medicinal chemistry
- 18 May 2000
A series of 4-alkenyl and 4-alkynyl-3, 4-dihydro-4-(trifluoromethyl)-2-(1H)-quinazolinones were found to be potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) of human immunodeficiency… Expand
Expanded-Spectrum Nonnucleoside Reverse Transcriptase Inhibitors Inhibit Clinically Relevant Mutant Variants of Human Immunodeficiency Virus Type 1
- J. W. Corbett, S. Ko, +11 authors S. Erickson-Viitanen
- Biology, Medicine
- Antimicrobial Agents and Chemotherapy
- 1 December 1999
ABSTRACT A research program targeted toward the identification of expanded-spectrum nonnucleoside reverse transcriptase inhibitors which possess increased potency toward K103N-containing mutant human… Expand
Electrochemical oxidation of chlorinated phenols
Electrochemical oxidation has been proposed as a remediation method for chlorinated phenols but is hampered by anode fouling. In this work we explore the mechanism of anode fouling by chlorinated… Expand