SHP2 Inhibitor

Ellagic acid is a natural antioxidant, and acts as a potent and ATP-competitive inhibitor of CK2 and SHP2, with an IC₅₀ of 40 nM and a K_i of 20 nM.

SHP099 is an allosteric SHP2 inhibitor, with IC₅₀s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2^D61Y, SHP2E69K, SHP2^A72V, SHP2^E76K. 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.

Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC₅₀=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors.

RMC-4550 is a potent, selective and allosteric inhibitor of SHP2, with an IC₅₀ of 0.583 nM.

Sitneprotafib (JAB-3312) is an orally effective anticancer phosphatase SHP2 inhibitor (IC₅₀: 1.9 nM) with anti-cancer activity. Sitneprotafib has good tolerability and significantly induced tumor regression in a KYSE-520 mouse xenograft model.

NSC-13030 is a SHP2 inhibitor with an IC₅₀ value of 3.2 μM. NSC-13030 reduces the proliferation and viability of breast cancer cells. NSC-13030 is applicable to breast cancer-related research.

IB15C is an ILT3 (LILRB4) inhibitor with a human K_d of 0.92 μM. IB15C binds to a specific ILT3 pocket, disrupts ApoE interaction, and interferes with downstream inhibitory signaling pathways. IB15C reduces SHP1 and SHP2 phosphorylation, suppresses pro-inflammatory cytokine secretion, enhances amyloid uptake, and attenuates NF-κB activation. IB15C can be used for the research of alzheimer's disease.

SDUY127 is a bivalent SHP2 inhibitor with an IC₅₀ value of 16 nM. SDUY127 binds simultaneously to the tunnel allosteric site and latch allosteric site of SHP2 at a 1:1 stoichiometric ratio, stabilizes the protein in an inactive conformation, and induces sustained inhibition of the MAPK signaling pathway. SDUY127 can be used in research related to leukemia and hepatocellular carcinoma.

NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC₅₀ values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).

Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice.

SHP099 hydrochloride is a potent, selective and orally available SHP2 inhibitor with an IC₅₀ of 70 nM.

PF-07284892 (ARRY-558) is a potent and orally active SHP2 inhibitor with an IC₅₀ value of 21 nM. PF-07284892 decreases the expression of pERK.

PHPS1 is a potent and selective Shp2 inhibitor with K_is of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.

Migoprotafib (GDC-1971) (compound 199) is a SHP2 inhibitor. Migoprotafib inhibits the MAPK/ERK signaling pathway, and exhibits antitumor activity.

PTP Inhibitor IV is a protein tyrosine phosphatase (PTP) inhibitor that competitively inhibits DUSP14 phosphatase activity with an ₅₀ of 5.21 μM. PTP Inhibitor IV inhibits SHP-2, PTP1B, PTP-ε, PTP Meg-2, PTP-σ, PTP-β, and PTP-μ with ₅₀s of 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively.

SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC₅₀s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC₅₀ of 15.7 nM and a K_d of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.

RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.

JAB-3068 (SHP2-IN-6) is a potent SHP2 inhibitor, extracted from patent WO2017211303A1, compound 7, has an IC₅₀ of 25.8 nM.

Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC₅₀s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.