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.
For research use only. We do not sell to patients.
- CAS No.: 2296718-09-5
- Formula: C30H27Cl2N3O4
- Molecular Weight:564.46
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
IC50: 9.8 µM (SHP2)[1]
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.
-
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.
-
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 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 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 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.
-
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 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.
Chemical Information
-
CAS No. 2296718-09-5
-
Molecular Weight 564.46
-
Formula C30H27Cl2N3O4
-
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
-
Synonyms
LY6
-
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
[1]. Wu X, et al. Small Molecule Inhibitor that Stabilizes the Autoinhibited Conformation of the Oncogenic Tyrosine Phosphatase SHP2. J Med Chem. 2019 Feb 14;62(3):1125-1137. [Content Brief]
[2]. Mi D, et al. Small-molecule Modulators Targeting SHP2 for Cancer Therapy. Anticancer Agents Med Chem. 2023;23(5):498-504. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SHP2 inhibitor LY6 Related Classifications
HY-125257 Related Classifications
Powered by Bioz