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Anthra[1,9-cd]pyrazol-6(2H)-one inhibits MAPK8. 54 / 112
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"As shown in Fig. 8 A, SP600125 efficiently attenuated the alkannin-induced increases in p-JNK and p-c-Jun in the MDA-MB-231, HCT116 and Huh7 cells."
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"Importantly, inhibition of JNK1 by SP600125 blocked the reduction of apoptotic cell number (XREF_FIG) and apoptotic markers (i.e., cleavage of caspase-3 and PARP) caused by metformin (XREF_FIG)."
23223177
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"As SP600125 inhibits both JNK1 and JNK2, to further evaluate the relationship between JNK2 and the UPR, BiP and CHOP were analyzed by western blot after JNK2 silencing."
23171849
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"JNK1 can be inhibited by the anthrapyrazole SP600125, even though this compound also mildly impairs the function of p38beta and ERK2 [XREF_BIBR]."
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"Whether these distinctions have the potential to confer therapeutic benefits remains untested, however, since direct comparisons with JNK-1 active-site inhibitors such as SP600125 [ 28 ] have not yet [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Our Western blot results showed that repeated intrathecal injections of SP600125 significantly reduced the up-regulation of p-JNK and p-c-Jun in the spinal cord (Figure 6(b) and (c)), and immunofluorescence results further showed that p-JNK and p-c-Jun co-localization in both the microglia and astrocytes also decreased (Figure 7(a) and (b), Supplementary Figure 3(a) and (b))."
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"The JNK specific inhibitor; SP600125 also inhibited JNK1 activation."
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"The inhibitor SP600125 selectively binds and inhibits JNK1, 2, and 3 in a reversible manner [ xref ]."
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"As SP600125 inhibits both JNK1 and JNK2, to further evaluate the relationship between JNK2 and the UPR, BiP and CHOP were analyzed by western blot after JNK2 silencing."
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"The increased p-JNK/JNK ratio observed 3 h after MCAO was significantly suppressed by SP600125 administration ( Fig. 3 A)."
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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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"Alcohol activates JNK1 to upregulate transcription of Brf1 and Pol III genes, whereas inhibition of JNK1 by SP600125 or its siRNA significantly decreases the induction of these genes."
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"These data indicate that JNK1 inhibits TAp63γ transactivity via phosphorylation of Ser12 residue.To investigate whether endogenous JNK1 is involved in regulation of TAp63γ transactivity, we treated ce[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"SP600125, a potent JNK1 inhibitor, reduces the JNK1 activity associated with GLUT4 and the phosphorylation of two minor GLUT4 species in serum starved 3T3-L1 adipocytes."
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"Western blot analysis demonstrated that SP600125 significantly inhibited the activation of the p-JNK/JNK signaling pathway caused by SSA in AML cells (Figure 7B)."
40124558
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"As expected, 20 μM SB202190 and 30 μM SP600125 profoundly inhibited TCDD induced up-regulation of p-p38 and p-JNK, respectively."
23969120
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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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"JNK has three kinds of subfamily, JNK1, JNK2, and JNK3, which can be inhibited by SP600125."
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"SP600125 inhibits JNK1, JNK2, and JNK3 with similar potencies ( xref )."
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"Since JNK-1 is required for the development of bone resorption activity by osteoclasts, the inhibition of bone resorption may be related to JNK-1 inhibition by SP600125 in vivo ."
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"SB203580 (an inhibitor of p38 MAPK; 10microM), PD98059 (an inhibitor of ERK2; 20microM), and SP600125 (an inhibitor of JNK1; 10microM) markedly inhibited p38 MAPK (XREF_FIG), ERK2 (XREF_FIG), and JNK1 (XREF_FIG) phosphorylation in collagen activated platelets, respectively."
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"TG-101348 (special JAK2 inhibitor, from MCE), JAK2 siRNA (sc-39099, from Santa Cruz Biotechnology), SP600125 (the inhibitor of JNK1, from Santa Cruz), and FR180204 (the inhibitor of ERK1, from Santa Cruz) were purchased."
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"SP600125 inhibits the JNK1, -2, and -3 pathways [XREF_BIBR]."
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"SP600125 inhibits JNK1, JNK2, and JNK3 with a high specificity and markedly inhibits the activation/phosphorylation of c -Jun as well as expression of inflammatory genes xref ."
25428720
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"Inhibition of Jun-N terminal kinase 1 ( JNK1 ) by ( A ) SP600125 and by ( B ) 3,6 - dihydroxyflavone ( 3,6 - DHF ) in an ADP-Glo kinase assay ."
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"Importantly, inhibition of JNK1 by SP600125 blocked the reduction of apoptotic cell number ( xref ) and apoptotic markers (i.e., cleavage of caspase-3 and PARP) caused by metformin ( xref )."
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"We applied p-ERK blocker U0126 and p-JNK blocker SP600125 in the Jurkat T cells and found that LrB did not further inhibit the IL-2 release under stimulation of PHA ( Figure 7F )."
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"Hence, inhibition of JNK1 and JNK2 by SP600125 reduces the expression of these transcription factors and cell cycle genes, thereby reducing cell proliferation."
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"Furthermore, SP600125 was used to inhibit the potential downstream factor JNK1, and the osteogenic differentiation ability of DPSCs was evaluated."
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"In this study, SP600125 was used at an IC50 of 90 nM to inhibit JNK1, JNK2, and JNK3 as indicated by the manufacturer."
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"SP600125 is an anthrapyrazolone capable of inhibiting JNK1, JNK2, and JNK3 with high affinity ( xref , xref )."
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"JNK1 activity was suppressed in rats by SP600125 treatment (XREF_FIG)."
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"Both AS-IV and SP600125 reduced p-JNK, Bid, CytC, Apaf-1, caspase-3, and cleaved caspase-3 levels in rats while decreasing CytC, caspase-3, and caspase-9 levels in serum."
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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 the JNK1, -2, and -3 pathways [ xref ]."
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"TGFβ also induced phosphorylation of (S351) NR4A1, JNK1, c-jun and c-fos which was also inhibited by SP600125, demonstrating that TGFβ induces JNK and genes downstream from JNK."
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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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"Thus, after an osmotic stress induced by 0.4 M sorbitol for 10 min, immunoblot analysis demonstrates that 25 μM SB203580 and 25 μM SP600125 reduced p-p38 and p-JNK over 75% of the control value (data [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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."
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"In contrast, SP600125 that is known to inhibit JNK1, JNK2 and JNK3 with about equal potency ( Bennett et al., 2001 ) significantly reduced the IL-8 response at 10–40 μM."
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"SP600125, which inhibits JNK-1, -2 and -3, is a commonly used JNK inhibitor to delineating JNK functions, and has been shown to block the phosphorylation of c-Jun in cells with an IC 50 of 10 μM and a[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Firstly, cells were cultivated for a period of 16 h using either 10 μM SP600125 or 10 μM SB203580, and next, incubated at the concentration of 0.4 μM of brusatol for 8 h. Study shown in Fig. 4 A and B[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Furthermore, inhibition of JNK1 by SP600125 promoted Epo withdrawal induced apoptosis (XREF_FIG)."
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"The results indicated that SP600125 reversed the accumulation of p-JNK caused by Cd."
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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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"Our results demonstrated that SP600125 inhibited OVA-induced, increased activity of p-JNK and counteracted the accompanying increased expression of TLR9 in the lung tissues, suggesting that TLR9 may b[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
26139014
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"One compound, SP600125 ( 7 ), was found to inhibit JNK1, JNK2 and JNK3 with K i values of ∼190 nM [ 55 ]."
15501728
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"The H 2 O 2 levels could be decreased by pcDNA3 (FLAG)-JNK1-wt transfection in A2780 and DDP cells and this effect could be counteracted by a JNK1 antagonist SP600125."
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"SP600125 inhibits JNK1, JNK2, and JNK3 with similar potencies."
18651635
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"Meanwhile, c-jun activity was significant attenuated by SP600125 or after transfection with the JNK1 siRNA in XREF_FIG."
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"SP600125 is an anthrapyrazolone capable of inhibiting JNK1, JNK2, and JNK3 with high affinity [ xref ]."
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"JNK1 and ERK1 activation was completely abrogated by SP600125 and PD98059 treatment, respectively."
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"JNK1, 2, and 3 are selectively inhibited by SP600125 [26]."
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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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