IndraLab

Statements

ATP inhibits JAK1. 10 / 10
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"MMB is a small adenosine triphosphate (ATP)-a competitive molecule that effectively inhibits JAK1 and JAK2 in their typical forms and the mutant JAK2V617F variant (28)."
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"As an ATP competitive inhibitor of JAK1 and JAK2, AZD1480 was recently shown to inhibit activation of STAT3 and depress the growth of multiple adult tumors [XREF_BIBR, XREF_BIBR]."
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"AZD1480, an ATP competitive inhibitor of JAK1 and JAK2, has beneficial effects in cancer models by suppressing downstream activation of STATs, particularly STAT3."
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"Many compounds with JAK inhibitory activity have been generated, with several currently being assessed in clinical trials of human patients diagnosed with MPN and acute myeloid leukemia (AML).8 AZD14801 is a pyrazolopyrimidine ATP competitive inhibitor of JAK1 and JAK2, with some activity against JAK3, TYK2, and Aurora-A kinase at high maximal inhibitory concentration (IC) values."
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"AZD1480, an ATP competitive inhibitor of JAK1 and JAK2, was recently shown to inhibit the growth of solid tumors including breast, ovarian and prostate."
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"168 We have recently demonstrated that AZD1480, an ATP competitive inhibitor of JAK1 and JAK2, has striking protective effects in multiple models of EAE XREF_BIBR, XREF_BIBR (XREF_FIG)."
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"Next, we attempted to inhibit downstream of the IFN pathway by using a pan-JAK inhibitor, tetracyclic pyridone 6 (P6), a potent, cell-permeable, and ATP competitive inhibitor of JAK1, JAK2, JAK3, and Tyk2."
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"Upadacitinib (ABT494) (Table 3) is also a JAK inhibitor that competes with adenosine triphosphate (ATP), which potently inhibits JAK1 and weakly inhibits the other isoforms JAK2, JAK3 and TYK2 [18]."
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"To test whether inhibition of the JAK and STAT3 pathway would affect the growth of pediatric solid tumors, we evaluated the anti-tumor activity of AZD1480, an ATP competitive inhibitor of JAK1 and JAK2, which has been shown to decrease the growth of adult tumors in several pre-clinical models [XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR]."
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"We first reported that AZD1480, an ATP competitive inhibitor of JAK1 and JAK2 inactivated STAT3 mediated signaling and inhibited tumor growth in pediatric solid tumors such as NB, Ewing sarcoma, and rhabdomyosarcoma in vitro and in vivo."
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