In MCF-7 cells, GSK1292263 (10 μM) combined with gefitinib (10 μM) for 24 h reduced the LC3B-II immunoblot signal relative to gefitinib alone. This qualitative result does not by itself establish autophagic flux or GPR119 dependence. [1]
In LX-2 human hepatic stellate cells, GSK1292263 (10 and 20 μM; 1 h pretreatment) reduced collagen I and TGFβ protein signals after stimulation with TGFβ1 (2 ng/mL) for 24 h. The GSK-specific evidence is qualitative immunoblotting; receptor-dependence and downstream pathway controls in this paper used MBX-2982. [2]
Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.
GSK1292263 lowers gefitinib-associated LC3B-II in MCF-7 cells
Cell-based study · Human MCF-7 breast cancer cells [1]
In the displayed immunoblot, GSK1292263 plus gefitinib showed less LC3B-II than gefitinib alone. Untreated cells, gefitinib alone, gefitinib plus MBX-2982, and gefitinib plus chloroquine were displayed with actin loading controls. This is a qualitative LC3B endpoint, without an extracted effect size or proof of autophagic flux or receptor dependence.
Literature-Reported Treatment Conditions
- Treatment concentration
- GSK1292263 10 μM; gefitinib 10 μM
- Exposure duration
- 24 h
- Method
- Cell treatment followed by western blot analysis
- Co-treatment
- GSK1292263 with gefitinib; MBX-2982 10 μM and chloroquine 3 μM are separate comparator conditions, not components of the GSK combination.
- Reported limits
- Drug vehicle and replicate count specific to the Figure 3E GSK blot are not specified in the read methods/caption. No GSK-specific flux assay or receptor-loss control is shown in this panel.
Methods and source locations
Compound reported in the paper: GSK1292263; Compound label in the paper: GSK
Applies to the named research compound in this cell experiment; no salt conversion or Adooq batch equivalence is assumed.
Figure 3E and caption; Methods: Cell culture, Antibodies and reagents, Western blot analysis; Results Sec20: Inhibition of EGFR-TKI-induced autophagy by MBX-2982 in breast cancer cells
LC3B-I/II protein immunoblot, with actin loading control: Western blotting; the original Figure 3E image was viewed. No band densitometry or numerical magnitude was inferred. — Figure 3E and caption; Methods: Cell culture, Antibodies and reagents, Western blot analysis; Results Sec20: Inhibition of EGFR-TKI-induced autophagy by MBX-2982 in breast cancer cells
GSK1292263 reduces TGFβ1-induced fibrogenic protein signals in LX-2 cells
Cell-based study · LX-2 immortalized human hepatic stellate cells stimulated with TGFβ1 [2]
The GSK-labelled immunoblot showed lower collagen I and TGFβ protein signals with GSK1292263 plus TGFβ1 than with TGFβ1 alone. Basal and stimulated controls and GAPDH were shown. The displayed GSK experiment supports a qualitative protein response; the qPCR plots, receptor knockdown, Smad signaling and detailed AMPK experiments must not be attributed to GSK1292263.
Literature-Reported Treatment Conditions
- Treatment concentration
- GSK1292263 10 and 20 μM; TGFβ1 2 ng/mL
- Exposure duration
- 1 h pretreatment with GSK1292263 followed by 24 h TGFβ1 stimulation
- Method
- Cell pretreatment and cytokine stimulation followed by immunoblotting
- Co-treatment
- GSK1292263 with TGFβ1 stimulation; MBX-2982 is a separate experimental comparator.
- Reported limits
- Vehicle is not specified in the read cell-treatment methods/caption. The caption gives mean ± SD, n=3 for quantified Figure 3 data, but no GSK-specific quantification is displayed; no numerical replicate-based estimate is adopted. This panel does not establish whether cytotoxicity contributes.
Methods and source locations
Compound reported in the paper: GSK1292263; Compound label in the paper: GSK
Applies to the named research compound in this cell experiment; no salt conversion or Adooq batch equivalence is assumed.
Figure 3A (GSK-labelled immunoblot, lower left) and caption; Materials and Methods: Cell culture, Immunoblot analysis; Results sec18: GPR119 agonists inhibit TGFβ1-induced HSC activation
Collagen I and TGFβ protein expression with GAPDH loading control: Immunoblot analysis; Figure 3A GSK panel viewed. No fold change, concentration-specific significance or densitometric value inferred. — Figure 3A (GSK-labelled immunoblot, lower left) and caption; Materials and Methods: Cell culture, Immunoblot analysis; Results sec18: GPR119 agonists inhibit TGFβ1-induced HSC activation
