k252a  (Tocris)

Journal: Cancer Biology & Therapy

Article Title: Deguelin inhibits perineural invasion in esophageal squamous cell carcinoma via targeting BDNF/TrkB axis

doi: 10.1080/15384047.2026.2644788

Figure Lengend Snippet: BDNF/TrkB regulate the abilities of cell proliferation, migration and invasion in KYSE-150 cells. (A and B) CCK-8 assay checked cell proliferation affected by hrBDNF and k252a; (C and D) plate cloning assay analyzed cloning formation ability of KYSE-150 cell affected by hrBDNF and k252a; (E–H) the abilities of cell invasion and migration affected by hrBDNF and k252a evaluated by scratch wound healing assays and Boyden chamber migration and invasion assays; and (I) the expression of MMP9, N-cadherin, S100B, and NGF affected by hBDNF and k252a with WB. * p < 0.05, ** p < 0.01, and *** p < 0.001.

Article Snippet: Recombined human BDNF protein (Cat#450-02), k252a (Cat#HY-N6732), and Deguelin (Cat#HY-13425) were obtained from PeproTech and Med Chem Express (MCE), respectively.

Techniques: Migration, CCK-8 Assay, Cloning, Expressing

Journal: Cancer Biology & Therapy

Article Title: Deguelin inhibits perineural invasion in esophageal squamous cell carcinoma via targeting BDNF/TrkB axis

doi: 10.1080/15384047.2026.2644788

Figure Lengend Snippet: BDNF/TrkB regulate the interaction between DRG and KYSE-150 cells. (A–C) The distance of ESCC cell migration and the numbers of newborn ganglion synapses in the DRG-ESCC cells co-culture model treated with BDNF and k252a, respectively. Scale bar: 100 μM; green arrow: newborn ganglion synapses; yellow arrow: KYSE-150 cell. *** p < 0.001.

Article Snippet: Recombined human BDNF protein (Cat#450-02), k252a (Cat#HY-N6732), and Deguelin (Cat#HY-13425) were obtained from PeproTech and Med Chem Express (MCE), respectively.

Techniques: Migration, Co-Culture Assay

Journal: Cancer Biology & Therapy

Article Title: Deguelin inhibits perineural invasion in esophageal squamous cell carcinoma via targeting BDNF/TrkB axis

doi: 10.1080/15384047.2026.2644788

Figure Lengend Snippet: The role of BDNF/TrkB in ESCC PNI development in vivo . (A) The experimental flowchart of the PNI model treated with 500 μg/kg and 750 μg/kg k252a ( n = 5/group); (B and C) representative images and quantitative analysis of PNI development assessed with IVIS Spectrum in vivo imaging system; (D) representative images and quantitative analysis of the xenograft tumor in the PNI models treated with k252a; (E) representative images of the PNI model checking with HE and IHC with S100B and SCCA1; (F) The occurrence rate of PNI treated with k252a; (G–I) WB analysis and quantitative analysis of the protein expression of N-cadherin, MMP9, NGF and S100B during PNI development (40-, 50-, 60-d) and in the PNI models of the control and k252a-treated groups; (J) WB and quantitative analysis of the expression of BDNF and TrkB during PNI progress with CDX and PNI models. Red arrow: ESCC cells; black arrow: neuron; scale bar: 50 μM; * p < 0.05, ** p < 0.01, and *** p < 0.001.

Article Snippet: Recombined human BDNF protein (Cat#450-02), k252a (Cat#HY-N6732), and Deguelin (Cat#HY-13425) were obtained from PeproTech and Med Chem Express (MCE), respectively.

Techniques: In Vivo, In Vivo Imaging, Expressing, Control

Journal: Cancer Biology & Therapy

Article Title: Deguelin inhibits perineural invasion in esophageal squamous cell carcinoma via targeting BDNF/TrkB axis

doi: 10.1080/15384047.2026.2644788

Figure Lengend Snippet: BDNF/TrkB regulated ESCC PNI through Akt signaling. (A) Representative images and fluorescence intensity of the PNI model treated with k252a using IVIS spectrum in vivo imaging system ( n = 3/group); (B) representative images and quantitative analysis of the xenograft tumor in PNI models treated with k252a; (C) the clustering diagram of differentially expressed genes (DEGs) analyzed by transcriptome sequencing with xenograft tumor tissues from the k252a·PNI groups and PNI groups; (D) pathway analysis of downregulated DEGs using the GO database; (E and F) the mRNA expression levels of Akt in the PNI and k252a·PNI groups, CDX, and PNI groups using qRT-PCR; and (G–J) WB and quantitative analysis of the protein expression levels of Akt and pAkt in the PNI and k252a·PNI groups and the CDX and PNI groups at 40-, 50-, and 60-d. * p < 0.05, ** p < 0.01, and *** p < 0.001.

Article Snippet: Recombined human BDNF protein (Cat#450-02), k252a (Cat#HY-N6732), and Deguelin (Cat#HY-13425) were obtained from PeproTech and Med Chem Express (MCE), respectively.

Techniques: Fluorescence, In Vivo Imaging, Sequencing, Expressing, Quantitative RT-PCR

Journal: CNS Neuroscience & Therapeutics

Article Title: KCC2 Dysfunction Mediated by Microglial BDNF / TrkB Signaling Exacerbates Early Post‐Stroke Seizure Susceptibility

doi: 10.1002/cns.70795

Figure Lengend Snippet: CLP290 inhibition of KCC2 expression downregulation reduces epilepsy susceptibility after MCAO‐R. (A, B) Western blot quantification of mKCC2 relative to GAPDH (A) and NeuN (B) in whole hippocampal tissue (Sham: N = 4, MCAO‐R: N = 7, MCAO‐ R + CLP290: N = 7). CLP290 attenuated the downregulation of mKCC2 in surviving neurons. (C, D) Proportions of mice at each seizure level in each group at the initial PTZ dose of 40 mg/kg (C) and cumulative 50 mg/kg PTZ (D). (E) Proportion of mice with seizure Racine IV‐V at 40, 50, 60, and 70 mg/kg cumulative dose of PTZ. CLP290 pretreatment significantly reduced the proportion of MCAO‐R mice with seizure Racine IV‐V at 40 mg/kg, 50 mg/kg, and 60 mg/kg PTZ doses. (F) Mean Racine seizure scores at cumulative PTZ doses of 40, 50, 60, and 70 mg/kg. CLP290 pretreatment significantly reduced the mean seizure scores in MCAO‐R mice. (G) Cumulative PTZ dose required to reach Racine IV–V seizures in each group. CLP290 pretreatment significantly increased the cumulative dose of PTZ associated with causing seizures to Racine IV‐V (Sham: N = 10, MCAO‐R: N = 13, MCAO‐ R + CLP290: N = 10). (H) Simplified schematic summarizing that CLP290, acting downstream on KCC2, restores KCC2 function after MCAO‐R, thereby normalizing E GABA , reducing neuronal hyperexcitability, and ultimately lowering seizure susceptibility. * p < 0.05, ** p < 0.01, and *** p < 0.001 compared to the Sham group; # p < 0.05 and ## p < 0.01 compared to the MCAO‐R group.

Article Snippet: FUR was purchased from Sigma‐Aldrich, and minocycline, K252a, and CLP290 were from MedChemExpress.

Techniques: Inhibition, Expressing, Western Blot