SHP2 Inhibitor

PB17-026-01 is a potent SHP2 allosteric inhibitor and shows the highest inhibitory activity with an IC₅₀ value of 38.9?nM. PB17-026-01 can be used for the research of tumor.

SHP2-IN-33 (Compound D13) is an allosteric inhibitor of SHP2 with an IC₅₀ of 1.2 μM. In cellular studies, SHP2-IN-33 demonstrates antiproliferative activity with an IC₅₀ of 38 μM against Huh7 cells by arresting the G0/G1 cell cycle, promoting apoptosis (Apoptosis), and suppressing the MAPK signaling pathway. In an in vivo Huh7 xenograft mouse model, SHP2-IN-33 exhibits significant antitumor activity and favorable pharmacokinetics, including 54% oral bioavailability and a half-life of 10.57 hours. SHP2-IN-33 is a promising compound for studying tumor diseases associated with SHP2.

SMARCA2/4 Ligand-Linker Conjugate 2 is a target protein ligand-linker conjugate that can be used to synthesize PROTAC AU-15330 (HY-145388).

SHP2-IN-45 (Compound 6) is a potent, highly selective, and orally active SHP2 allosteric inhibitor. SHP2-IN-45 significantly reduces the expressions of IL-6, TNF-α, IL-1β, and iNOS. SHP2-IN-45 inhibits the polarization of M1-type macrophages. SHP2-IN-45 can inhibit the NF-κB pathway. SHP2-IN-45 can be used in the research of sepsis and acute lung injury.

GL-4512 is an orally active LILRB4/ILT3 inhibitor with an IC₅₀ of 37 nM against human targets, and human K_d values of 18.1 nM and 39.2 nM, respectively. GL-4512 directly binds to the extracellular pockets of LILRB4/ILT3 that accommodate their ligands, blocks the LILRB4-SCG2 signaling pathway, and inhibits the downstream SHP1/SHP2 and STAT3 signaling pathways. GL-4512 restores anti-tumor immune activity, promotes the production of IFN-γ and IL-2, enhances the activation of cytotoxic T cells, reduces tumor cell viability, inhibits tumor growth, and strengthens intratumoral immune activation. GL-4512 can be used in research related to colorectal cancer and acute myeloid leukemia.

SHP2-IN-22 is SHP2 allosteric inhibitor with an IC₅₀ value of 17.7 nM. SHP2-IN-22 inhibits the proliferation, migration, and invasion of MIA PaCa-2 pancreatic cancer cells. SHP2-IN-22 can be used for Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research.

SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC₅₀=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC₅₀=5 nM.

SHP2-IN-41 (Compound 4) is a SHP2 inhibitor with an IC₅₀ of less than 0.1 μM. SHP2-IN-41 has an IC₅₀ against KYSE-520 cells also less than 0.1 μM. SHP2-IN-41 can be used in the study of cancer.

SHP2-IN-42 is a src homology 2 domain-containing phosphatase 2 (SHP2) inhibitor with an IC₅₀ of 15 nM. SHP2-IN-42 inhibits cell proliferation and induces apoptosis and G1 phase cell cycle arrest. SHP2-IN-42 can be used for the research of cancer, such as acute myeloid leukemia (AML).

JC-010a is a selective SHP2 allosteric inhibitor. JC-010a inhibits cancer cells proliferation. JC-010a can be used for the research of cancer.

SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC₅₀=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty.

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.

SHP2-IN-28 (Compound 7188-0011) is an inhibitor of SHP2 (IC₅₀=54.31 μM). SHP2-IN-28 exerts its inhibitory effect by binding to the variable site of SHP2 with high selectivity.

SHP2-IN-16 (compound 222) is a SHP2 inhibitor with an IC₅₀ value of 1 nM. SHP2-IN-16 can be used for glioblastoma research.

SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC₅₀ value of 23 nM and K_i of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 °C. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells.

SHP2-IN-32 (compound C6) is an orally active, allosteric SHP2 inhibitor with an IC₅₀ value of 0.13 nM. SHP2-IN-32 exhibits antitumor activity.

SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC₅₀ values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research.

SHP244 is a conformational inhibitor targeting the "latch allosteric site" (site 2) of the SHP2 protein with an IC₅₀ value for SHP2^WT of 60 μM. SHP244 has no significant effect on the level of p-ERK alone. SHP244 combined with RMC-4550 (HY-116009) ("tunnel site" site 1 inhibitor) can reduce p-ERK and inhibit the rebound of p-ERK, thereby reducing drug resistance. SHP244 can be used to study drug resistance in FGFR-driven cancers.

SHP2-IN-27 (compound 28) is an allosteric inhibitor of tyrosine phosphatase SH2.

NAT6-297775 (Compound 29) is a protein tyrosine phosphatase (PTP) inhibitor targeting non-receptor PTP SHP-2 with an IC₅₀ of 2.5 μM. NAT6-297775 can inhibit the RAS/MAP kinase signaling pathway. NAT6-297775 can be used for the research of cancer, such as leukemia.