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Anthra[1,9-cd]pyrazol-6(2H)-one inhibits MAPK8. 44 / 93
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"SB, but not SP, was very effective in lowering the activation of p38 MAPK produced by AA plus 3-MA to below basal levels (XREF_FIG B and C; lanes 3 and 4) while SP, but not SB, effectively blocked the 2-3 fold elevated ratio of pJNK1 and JNK1 to below basal levels (XREF_FIG D and E : lanes 3 and 5), validating their specific inhibitory effectiveness."
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"In the present study, the Western blotting, IHC, and TTC staining results revealed that SP and D+YZR-0.8 g treatments effectively reversed the increased p-ASK1/ASK1 and p-JNK/JNK ratios, and the increased expression of TLR4, Iba1, GFAP, T3JAM, TRAF3, NF-κB, iNOS, COX-2, TNF-α, and IL-6 in the penumbral cortex and subsequently reduced the percentage of cerebral infarct areas and NDSs at 1 day after reperfusion."
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"We found that the up-regulated level of Netrin-1 and its receptor DCC promoted axonal regeneration and synaptic formation; the overexpression of Netrin-1 activated the JNK1 signaling pathway; these effects were partially reduced when JNK1 signaling pathway was inhibited by SP600125 (JNK specific inhibitor)."
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"As shown in XREF_FIG (MTT assay) and XREF_FIG (annexin-V and PI double staining), SP600125 (an inhibitor of JNK-1, -2 and -3), SB202190 (an inhibitor of p38 MAPK-beta), and U0126 (an inhibitor of MEK1/2) each significantly reduced glutamate induced cell death in a concentration dependent manner."
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"Additionally, in MPHs isolated from Jnk1 -/- and Jnk2 -/- mice, the response of nuclear RXRalpha to IL-1beta could only be inhibited by complete abrogation of JNK activation by pretreatment of SP600125 but not in the hepatocytes lacking each individual Jnk1 or Jnk2 gene (XREF_FIG)."
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"Indeed, when Ubisol-Q -treated PSAF were treated with autophagy inhibitor SP600125 (a known inhibitor of beclin-1 via JNK1 inhibition [29, 30]), we saw a drastic decrease in autophagosome formation (Figures 4(a), 4(c), and 3) as well as the return of the SIPS phenotype (Figures 2, 3(a), and 3(b))."
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"SP600125 inhibits JNK-1, JNK-2, and JNK-3 (cell-free IC 50 of 40 nM
for JNK1 and 2, and 90 nM for JNK3). xref It has been shown that activated JNK isomers directly phosphorylate the
BMAL1-CLOCK complex to regulate the speed and phase of circadian oscillations in cells; xref thus, treatment with SP600125 increased periods."