2. LC-MG-5

LC-MG-5 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 231.7 nM (in KATO III cells). LC-MG-5 induces proteasomal degradation of FGFR2 via a covalent molecular glue mechanism. LC-MG-5 inhibits cancer cell proliferation. LC-MG-5 suppresses FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways. LC-MG-5 can be used for the research of gastric cancer.

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LC-MG-5

LC-MG-5 Chemical Structure

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LC-MG-5 Related Antibodies

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Description

LC-MG-5 is a selective molecular glue degrader targeting FGFR2, with a DC50 of 231.7 nM (in KATO III cells). LC-MG-5 induces proteasomal degradation of FGFR2 via a covalent molecular glue mechanism. LC-MG-5 inhibits cancer cell proliferation. LC-MG-5 suppresses FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways. LC-MG-5 can be used for the research of gastric cancer[1].

In Vitro

LC-MG-5 (1 μM; 12 h) significantly reduces the FGFR2 protein level in KATO III cells[1].
LC-MG-5 (10 nM-10000 nM; 12 h) induces dose-dependent degradation of FGFR2 in KATO III cells, with a DC50 of 231.7 nM[1].
LC-MG-5 (0-1000 nM; 12 h) inhibits FGFR2-mediated PI3K/AKT and MAPK/ERK signaling pathways in KATO III cells[1].
LC-MG-5 (1 μM; 6 h-12 h) induces the internalization of FGFR2 from the plasma membrane to intracellular vesicular compartments in KATO III cells[1].
LC-MG-5 (1 μM; 0 h-8 h) induces time-dependent degradation of FGFR2 in KATO III cells, with the maximum clearance achieved at 8 h[1].
LC-MG-5 (96 h) inhibits the proliferation of KATO III cells with an IC50 value of 65.49 nM[1].
LC-MG-5 (200 nM; co-incubated with 1 μM MG132 (HY-13259)) mediates the degradation of FGFR2 in KATO III cells, and this process is strictly dependent on the ubiquitin-proteasome system[1].
LC-MG-5 (1 μM; co-incubated with 1 μM Infigratinib) mediates the degradation of FGFR2 in KATO III cells by binding to the ATP-binding pocket of FGFR2, whereas pretreatment with the parental inhibitor Infigratinib (HY-13311) blocks this degradation process[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LC-MG-5 Related Antibodies

Western Blot Analysis[1]

Cell Line: KATO III cells
Concentration: 1 μM
Incubation Time: 12 h
Result: Induced significant depletion of FGFR2 protein levels.

Western Blot Analysis[1]

Cell Line: KATO III cells
Concentration: 0, 300, 1000 nM
Incubation Time: 12 h
Result: Abrogated both the PI3K/AKT and MAPK/ERK signaling cascades, as evidenced by the markedly diminished phosphorylation of the primary docking protein FRS2α (Tyr436), as well as
PLCγ (Tyr783), SHP2 (Tyr524), AKT (Ser473), ERK1/2, and the downstream terminal kinase RSK1 (Thr573).

Immunofluorescence[1]

Cell Line: KATO III cells
Concentration: 1 μM
Incubation Time: 0, 6, 12 h
Result: Triggered the rapid relocalization of FGFR2 from the plasma membrane into intracellular vesicular compartments.
Molecular Weight

622.52

Formula

C26H29Cl2N7O5S
SMILES

ClC1=C(OC)C=C(OC)C(Cl)=C1NC(N(C)C2=NC=NC(NC3=CC=C(N4CCN(S(C=C)(=O)=O)CC4)C=C3)=C2)=O
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Room temperature in continental US; may vary elsewhere.
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References
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LC-MG-5 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LC-MG-5gastric cancerKATO III cellsPI3K/AKTMAPK/ERKFGFR2DCAF16FGFR3ubiquitin-proteasome systemFGFR1fibroblast growth factor receptor 2Inhibitorinhibitorinhibit

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