SHP2 Inhibitor

SHP2-IN-43 (Compound 5) is a SHP2 inhibitor with an IC₅₀ of 98.7 nM. SHP2-IN-43 can be used as a PROTAC target ligand in the synthesis of SHP2-D26 (HY-145162).

SHP2-IN-30 (compound 14i) is an allosteric SHP2 inhibitor with an IC₅₀ of 104 nM. SHP2-IN-30 shows low inhibitory effect on SHP2-PTP. SHP2-IN-30 induces cell apoptosis and arrests the cell cycle at the G0/G1 phase.

TK-642 is a highly active, selective, orally activity SHP2 inhibitor based on pyrazole and pyrazine (IC₅₀=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer.

SDUY038 is a SHP2 allosteric inhibitor, with an IC₅₀ of 1.2 μM and K_D of 0.29 μM, respectively. SDUY038 exhibits pan-antitumor activity (IC₅₀ = 7-24 μM) by suppressing pERK expression. SDUY038 exhibits t_1/2 of 3.95 h by oral administration.

TK-685 is an orally active, selective, and allosteric SHP2 inhibitor with an IC₅₀ of 2.1 nM. TK-685 inhibits esophageal cancer cell proliferation and induced apoptosis by targeting SHP2-mediated AKT and ERK signaling pathways.

SHP2/NAMPT-IN-1 is an orally active dual inhibitor of SHP2 and NAMPT, with IC₅₀ values of 30.5 nM and 24.4 nM, respectively. SHP2/NAMPT-IN-1 reduces NAD⁺ levels and p-ERK expression by inhibiting NAMPT. SHP2/NAMPT-IN-1 can inhibit the migration and colony formation of MDA-MB-231 cells and promote apoptosis. SHP2/NAMPT-IN-1 has anti-proliferative activity against a variety of tumor cell lines and can reverse PD-L1-mediated T-cell immunosuppression. SHP2/NAMPT-IN-1 can be used for breast cancer research.

RMC-3943 is an allosteric SHP2 inhibitor (inhibition of full-length SHP2 in biochemical assay, IC₅₀ = 2.19 nM).

SHP504 is a SHP2 phosphatase inhibitor, with an IC₅₀ of 21 μM for SHP2^1–525.

SHP2-IN-24 (compound 111675) is a potent SHP2 inhibitor with an IC₅₀ value of 0.878 µM and a K_i value of 0.118 µM.

CDK12-Cyclin K ligand-1 is a ligand of PROTAC degrader that binds to the E3 ligase. CDK12-Cyclin K ligand-1 can be used in the synthesis of PROTAC degrader such as PP-C8 (HY-144691).

SHP2-IN-34 (compound A8) is a phenyl urea SHP2 inhibitor with anti-cancer activity. SHP2-IN-34 significantly suppresses tumor growth in CT26 mouse model.

SHP099 (Standard) is the analytical standard of SHP099. This product is intended for research and analytical applications. SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth.

SHP099 (monohydrochloride) (Standard) is the analytical standard of SHP099 (monohydrochloride). This product is intended for research and analytical applications. SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC50 of 70 nM.

SHP2-IN-29 (Compound 3) is a potent SHP2 inhibitor with an IC₅₀ value of 0.18 μM. SHP2-IN-29 also has inhibitory activity against PTP1B and TCPTP, with IC₅₀ values of 4.27 and 4.74 μM, respectively.

SHP2-IN-38 is a novel green-fluorescent SHP2 inhibitor with IC₅₀ values of 2.89 μM (SHP2), 8.73 μM (SHP1), 11.08 μM (PTP1B), 33.07 μM (TCPTP). SHP2-IN-38 blocks the SHP2-mediated ERK signaling pathway and inhibits MV4-11 cells proliferation in vitro with IC₅₀ of 7.90 μM. SHP2-IN-38 has an excitation wavelength of 360 nm, with a maximum emission wavelength of 550 nm in DMSO and 540 nm in DMF. SHP2-IN-38 shows green fluorescence imaging in HeLa cells and zebrafish.

CNBDA is a selective SHP2 inhibitor with an IC₅₀ of 5 μM. CNBDA binds to the active site of SHP2 through interactions with surrounding positively charged and polar amino acids, inhibits the PTPase activity of SHP2, and blocks the autodephosphorylation of SHP2. CNBDA inhibits the transformed phenotype, proliferation, anchorage-independent growth, and mammosphere formation of breast cancer cells, as well as EGF-induced Ras-ERK and PI3K-Akt signaling pathways, downregulates HER2 expression, and induces cell death. CNBDA can be used in breast cancer-related research.

SHP2-IN-46 is an orally active SHP2 inhibitor (IC₅₀ = 11.76 μM). SHP2-IN-46 inhibits SHP2 enzymatic activity and mediates anti-tumor activity. SHP2-IN-46 suppresses cell proliferation in various cancer cells. SHP2-IN-46 can be used in research related to lung adenocarcinoma, pancreatic cancer and hepatoblastoma.

SHP2-IN-31 is a SHP2 inhibitor, with IC₅₀s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models.