sh2

Stattic (STAT3 Inhibitor V) is a STAT3 inhibitor (IC50=5.1 μM) that selectively inhibits STAT3 activation, dimerization, and nuclear translocation. Stattic has antitumor activity and induces apoptosis.

740 Y-P (740YPDGFR) is a potent and cell-permeable activator of PI3K.

Stafia-1 is a potent STAT5a inhibitor (IC50=22.2 μM), displaying high selectivity over STAT5b and other STAT family members.

Grb2 SH2 Domain Inhibitor 1 TFA is a cyclic cell-penetrating peptide (CPP) featuring a conformationally restricted d-pro-l-pro motif ring (AF Φ Rpprrfq), where Φ represents L-naphthylalanine, R signifies D-arginine, and P stands for D-proline. It primarily functions as a cyclic peptide inhibitor.

Grb2 SH2 Domain Inhibitor 1 is a cyclic cell-penetrating peptide (CPP) featuring a conformationally restricted d-pro-l-pro motif ring (AF Φ Rpprrfq), where Φ represents L-naphthylalanine, R denotes D-arginine, and P indicates D-proline. This compound primarily functions as a cyclic peptide inhibitor.

740 Y-P acetate (740YPDGFR acetate) is a potent and cell-permeable PI3K activator.740 Y-P acetate tends to bind to GST fusion proteins containing the N- and C-terminal SH2 structural domains of p85, but not to GST alone.

STAT5-IN-1 (STAT5 Inhibitor) is a cell-permeable inhibitor which suppresses Stat5 via binding to the SH2 domain.

GluR6 antagonist-1 inhibits the pY binding site of tyrosine kinase p56lck SH2 domain.

CGP78850 is a potent and selective Grb2 SH2-phosphopeptide interaction antagonist with potential applications in cancer research.

Phosphopeptide; binds to the src SH2 domain.

C188 is a cell-permeable naphthol compound and a STAT3 inhibitor. C188 inhibits IL-6-stimulated STAT3 Tyr705 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket, while exhibiting little effect agai

5,15-Diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist with IC50 values of 0.28 μM for STAT3 and 10 μM for STAT1 [1].

PM-81I, a potent STAT6 inhibitor targeting the SH2 structural domain, effectively reduces STAT6 phosphorylation levels. It is applicable in the research of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, or cancer [1].

AQX-435 is a potent activator of SHIP1 (SH2 domain-containing inositol-5′-phosphatase 1). AQX-435 decreases B-cell receptor (BCR) downstream PI3K activity, induces apoptosis in malignant B cells, and exhibits inhibitory effects on lymphoma growth.

STAT3-IN-32 (compound 4c) is an orally active, potent dual phosphorylation inhibitor of STAT3. It demonstrates significant inhibition of STAT3 luciferase activity in HEK293T cells, with an IC50 of 5.3 nM, and inhibits ATP production in BxPC-3 cells with an IC50 of 4.2 nM. By targeting the STAT3 SH2 domain (KD=21.3 nM), STAT3-IN-32 effectively blocks p-Tyr705 and p-Ser727, leading to the attenuation of STAT3 nuclear transcription and mitochondrial oxidative phosphorylation. Furthermore, this compound displays notable suppressive effects in a pancreatic cancer xenograft model.

G7-18NATE, a peptide inhibitor of Grb7, exhibits micromolar affinity (K D = 18.1 μM) for binding to the Grb7-SH2 domain. It effectively inhibits cell proliferation, motility, invasion, and 3D culture formation in various cancer cell lines [1] [2].

AP-22161 selectively binds the Src SH2 domain by targeting highly conserved phosphotyrosine binding to cysteine residues in the pocket. AP-22161 selectively inhibits Src SH2 binding and can be used to inhibit osteoclast absorption.

AQX-MN115 is an SH2- containing inositol 5- phosphatase modulator.

STAT3-IN-13 is a potent STAT3 inhibitor.STAT3-IN-13 has antiproliferative and anticancer activity and acts by binding to the structural domain of STAT3 SH2.STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705, which induces apoptosis and inhibits tumor cell growth and metastasis.STAT3-IN-13 can be used to study breast cancer and liver cancer. The study of breast cancer and hepatocellular carcinoma.

STAT3-IN-35 is a STAT3 inhibitor that binds to the SH2 domain. This compound inhibits the phosphorylation of STAT3 and exhibits antiproliferative activity in triple-negative breast cancer (TNBC) cell lines. Additionally, STAT3-IN-35 has demonstrated toxicity and potent antitumor activity in TNBC xenograft models.

STAT3-IN-38 (Compound 4m) is a STAT3 inhibitor with a dissociation constant (K_D) of 45.33 µM for rhSTAT3, and is a derivative of Celastrol. It binds to the SH2 domain of the STAT3 protein, inhibiting phosphorylation at the pTyr705 site and suppressing downstream gene expression of Survivin and Mcl-1. STAT3-IN-38 can arrest the cell cycle and induce apoptosis in colorectal cancer cells.

Phosphopeptide ligand for the src SH2 domain (IC50 = 1 μM). Blocks src interactions with EGFR and FAK.

EPQpYEEIPIYL, a phosphopeptide, is a ligand for the Src homology 2 (SH2) domain, activating Src family members such as Lck, Hck, and Fyn through binding interactions with SH2 domains.

SHP2-IN-27 (compound 28) functions as an allosteric inhibitor targeting the tyrosine phosphatase SH2 [1].