2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR JAK/STAT Signaling Epigenetics Apoptosis
  3. Phosphatase SHP2 ERK Akt STAT JAK Apoptosis
  4. SHP2 inhibitor LY6

SHP2 inhibitor LY6 (LY6) is a selective SHP2 inhibitor with an IC50 of 9.8 μM, showing 7-fold selectivity over SHP1. SHP2 inhibitor LY6 inhibits SHP2-mediated cell signaling pathways and suppresses cell proliferation. SHP2 inhibitor LY6 elicits induces apoptosis and G2/M cell cycle arrest in lung cancer cells. SHP2 inhibitor LY6 can be used for the research of B cell acute lymphoblastic leukemia, acute myeloid leukemia, and lung cancer.

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SHP2 inhibitor LY6

SHP2 inhibitor LY6 Chemical Structure

CAS No. : 2296718-09-5

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SHP2 inhibitor LY6 Related Antibodies

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Description

SHP2 inhibitor LY6 (LY6) is a selective SHP2 inhibitor with an IC50 of 9.8 μM, showing 7-fold selectivity over SHP1. SHP2 inhibitor LY6 inhibits SHP2-mediated cell signaling pathways and suppresses cell proliferation. SHP2 inhibitor LY6 elicits induces apoptosis and G2/M cell cycle arrest in lung cancer cells. SHP2 inhibitor LY6 can be used for the research of B cell acute lymphoblastic leukemia, acute myeloid leukemia, and lung cancer[1].

IC50 & Target

IC50: 9.8 µM (SHP2)[1]
In Vitro

SHP2 inhibitor LY6 selectively inhibits full-length WT SHP2 (IC50 = 9.8 μM) and full-length SHP2E76K mutant (IC50 = 7.67 μM)[1].
SHP2 inhibitor LY6 (10 μM; 15 min) does not inhibit the phosphatase activity of WT SHP2, SHP2E76K mutant, or SHP2 PTP domain when using pNPP as a substrate[1].
SHP2 inhibitor LY6 binds specifically to His-tagged SHP2 with a Kd of 69 μM[1].
SHP2 inhibitor LY6 (2.5-20 μM; 48 h) dose-dependently inhibits the proliferation of IL-3-dependent Ba/F3 cells[1].
SHP2 inhibitor LY6 (5-40 μM; 4 h) dose-dependently inhibits IL-3-induced phosphorylation of Erk, Akt, Jak2, and Stat5 in Ba/F3 cells[1].
SHP2 inhibitor LY6 (6 μM; 1-3 days) inhibits proliferation of WT MEFs but not SHP2-deficient MEFs, confirming SHP2 as its primary cellular target[1].
The SHP2 inhibitor LY6 (6 μM; 1-3 days) inhibits the proliferation of Ptpn11E76K/+ MEFs more effectively than that of Ptpn11+/+ MEFs[1].
SHP2 inhibitor LY6 (2.5-20 μM; 48 h) dose-dependently inhibits proliferation of human lung cancer cells, with greater potency against H661 cells carrying the PTPN11N58S/+ activating mutation than WT H596 cells[1].
SHP2 inhibitor LY6 (10-20 μM; 24 h) induces dose-dependent apoptosis and G2/M cell cycle arrest in H661 human lung cancer cells carrying the PTPN11N58S/+ activating mutation[1].
SHP2 inhibitor LY6 inhibits phosphatase activity of SHP2WT and SHP2E76K by binding to a novel pocket between the C-SH2 and catalytic domains[2].

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

SHP2 inhibitor LY6 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: IL-3-dependent murine pro-B lymphoma Ba/F3 cells
Concentration: 2.5; 5; 10; 20 μM
Incubation Time: 48 h
Result: Significantly suppressed Ba/F3 cell proliferation in a dose-dependent manner, with statistically significant decreases at all tested concentrations.

Western Blot Analysis[1]

Cell Line: Ba/F3 cells
Concentration: 5; 10; 15; 20; 30; 40; 60 μM
Incubation Time: 4 h
Result: Inhibited IL-3-induced phosphorylation of Erk, Akt, Jak2, and Stat5 across all stimulation time points at 20 μM.
Exhibited dose-dependent inhibitory effect, with increasing suppression of phosphorylation observed as concentration increased from 0 to 40 μM.

Cell Proliferation Assay[1]

Cell Line: PTPN11 conditional knockout (Ptpn11fl/fl/Ad-Cre+) and WT (Ptpn11+/+/Ad-Cre+) mouse embryonic fibroblasts (MEFs)
Concentration: 6 μM
Incubation Time: 1; 2; 3 days
Result: Markedly decreased proliferation of WT MEFs.
Had no significant effect on proliferation of SHP2-deficient PTPN11 conditional knockout MEFs.

Cell Proliferation Assay[1]

Cell Line: Ptpn11E76K/+ and Ptpn11+/+ control MEFs
Concentration: 6 μM
Incubation Time: 1; 2; 3 days
Result: Decreased proliferation of both Ptpn11E76K/+ and Ptpn11+/+ MEFs.
Ptpn11E76K/+ mutant cells were much more sensitive to LY6 inhibition than WT cells.

Cell Proliferation Assay[1]

Cell Line: human lung cancer H661 cells (PTPN11N58S/+ activating mutation) and H596 cells (WT PTPN11)
Concentration: 2.5; 5; 10; 20 μM
Incubation Time: 48 h
Result: Inhibited proliferation of both cell lines in a dose-dependent manner, with statistically significant decreases at all tested concentrations.
H661 cells carrying the PTPN11 activating mutation were more sensitive to LY6 than H596 WT cells.

Apoptosis Analysis[1]

Cell Line: human lung cancer H661 cells (PTPN11N58S/+ activating mutation)
Concentration: 10; 20 μM
Incubation Time: 24 h
Result: Induced dose-dependent apoptosis in H661 cells, with statistically significant increases in apoptotic cell numbers at 10 μM and 20 μM.

Cell Cycle Analysis[1]

Cell Line: human lung cancer H661 cells (PTPN11N58S/+ activating mutation)
Concentration: 10; 20 μM
Incubation Time: 24 h
Result: Showed pronounced G2/M arrest, onsistent with the positive role of SHP2 in cell cycle
progression.
Molecular Weight

564.46

Formula

C30H27Cl2N3O4
CAS No.
SMILES

O=C1N(C2=CCCN(CC3=CC(C(/C=C/C4=CC=C(Cl)C=C4Cl)=O)=C(O)C=C3OCC)C2)C5=CC=CC=C5N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SHP2 inhibitor LY6 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:

SHP2 inhibitor LY62296718-09-5LY6LY 6LY-6PhosphataseSHP2ERKAktSTATJAKApoptosisSrc homology phosphatase 2PTPN11Extracellular signal regulated kinasesPKBProtein kinase BJanus kinaseacute myeloid leukemiaSHP1myelodysplastic syndromeB cell acute lymphoblastic leukemialung cancerBa/F3 cellsMEFsjuvenile myelomonocytic leukemiaInhibitorinhibitorinhibit

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