SHP2-IN-47 

SHP2-IN-47 is a selective and potent SHP2 inhibitor with an IC₅₀ of 0.80 μM. SHP2-IN-47 exhibits potent inhibitory activity against SHP2^E76K (IC₅₀ = 0.37 μM). SHP2-IN-47 functionally inhibits protein tyrosine phosphatase domains and downregulates SHP2-mediated phosphorylation of AKT and ERK. SHP2-IN-47 induces apoptosis and suppresses proliferation of cancer cells. SHP2-IN-47 can be used for the research of cancer, such as acute myelocytic leukemia^[1].

SHP2-IN-47 (Compound A4) (30 min) potently inhibits recombinant SHP2^WT (IC₅₀ = 0.80 μM), SHP2^E76K (IC₅₀ = 0.37 μM), and SHP2-PTP catalytic domain (IC₅₀ = 0.32 μM), while displaying no significant inhibition of SHP1 or PTP1B^[1].
SHP2-IN-47 (3 days) inhibits the proliferation of MV-4-11 (IC₅₀ = 2.12 μM), KYSE520 (IC₅₀ = 19.82 μM), HCT116 (IC₅₀ = 3.17 μM), MDA-MB-231 (IC₅₀ = 7.71 μM), and HepG2 (IC₅₀ = 4.16 μM) cancer cell lines, and has low toxicity to THP-1-derived macrophages (CC₅₀ > 50 μM)^[1].
SHP2-IN-47 (2-6 μM; 24 h) dose-dependently downregulates SHP2-mediated phosphorylation of AKT and ERK in MV-4-11 cells^[1].
SHP2-IN-47 (2-6 μM; 24 h) dose-dependently induces apoptosis^[1].

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

738.75

C₃₄H₃₇Cl₂N₉O₂S₂

ClC1=CC(N2C(SC)=NC3=NN(CCCCCNCCCCCN4N=C(N=C(SC)N(C5=CC(Cl)=CC=C5)C6=O)C6=C4)C=C3C2=O)=CC=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang Y, et al. Design, synthesis and biological activity of dimeric pyrazolo[3,4-d]pyrimidin-4-one derivatives as selective SHP2 orthosteric inhibitors. Bioorg Chem. 2026 Apr;171:109573.  [Content Brief]