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CAS No. 504433-23-2
GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.
Selleck's GW441756 has been cited by 12 publications
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Thermal latency and mechanical allodynia were normalized in the RTXw1 + 4MC group (n= 6). In these mice, thermal hypoalgesia reappeared within 2 days of GW441756 injection (D). GW441756 did not affect mechanical thresholds (E) in the RTXw1 + 4MC group. (F, G) The diagrams show behavioral responses of naïve mice to either gambogic amide (open square, n = 6) or GW441756 (open circle, n =6). Gambogic amide induced mild thermal hyperalgesia within 2 days of injection but GW441756 did not affect thermal latencies (F). Both gambogic amide and GW441756 did not affect mechanical responses. *P < 0.05, **P < 0.01, and ***P < 0.001: paired t-test comparing preinjection vs. postinjection effects. #P < 0.05, ##P < 0.01, and ###P < 0.001: between drugs and saline treatments.
Exp Neurol, 2018, 300:87-99. GW441756 purchased from Selleck.
Effect of TrkA inhibitorGW441756 on vorinostat andNGFmediated ERK phosphorylation. A)NS-1 cellswere treatedwith vorinostat (1 and 2.5 μM) andNGF (2.5 ng/mL)with and without GW441756 (1 μM) for 3 h. The blots were probed with anti-pERK.1/2 antibody. Vorinostat mediated activation of ERK1/2 phosphorylation (pErk) was abolished in presence of GW441756. Total ERK levels were checked using ERK 1/2 antibody. B) Bar graph represents the densitometric analysis of immunoblots. X axis represents treatments and Y axis represents the ratio of absolute relative density of pERK to the total ERK. The data sets are the mean ± SE of two biological replicates from two independent experiments (values compared to control vs vorinostat 1 μM and 2.5 μM, vorinostat 1 μM and 2.5 μM Vs GW441756 + vorinostat 1 and 2.5 μM respectively). *P < 0.05, **P < 0.001, ***P < 0.0001 indicate significant differences and ns indicates non-significant difference.
Mol Cell Neurosci, 2016, 77:11-20.. GW441756 purchased from Selleck.
Neurite extension of PC12 cells was visualized by immunostaining (×200 magnification; scale bar, 50 µm) with anti-neurofilament H antibody (red) and nuclei were stained with DAPI (blue). SCDC2 cells (2×104 cells) and rat pheochromocytoma cells PC12 (1×104 cells) were co-cultured and treated with or without TGF-β1 (10 ng/ml) for 4 days. Cells were also treated with TGF-β type I receptor inhibitor SB-431542 (10 µM), TrkA inhibitor GW441756 (2 nM), IL-1β (10 ng/ml), or TNF-α (10 ng/ml) from the beginning of the co-culture. In addition, ATPγS (100 µM) was added to all cultures during cell seeding. Dimethyl sulfoxide was added to cell cultures as a vehicle control for SB-431542 and GW441756, respectively.
Int J Mol Med, 2018, 42(3):1484-1494. GW441756 purchased from Selleck.
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|Description||GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.|
|In vitro||DMSO||25 mg/mL (90.81 mM)|
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