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.

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

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

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.

CPDA is a new potent inhibitor of SH2 domain-containing inositol phosphatase 2 (SHIP2).

SI-109 is a potent inhibitor of STAT3 SH2 domain (Ki=9 nM),and with antitumor activity.

3α-Aminocholestane (5α-Cholestan-3α-amine) is a potent inhibitor of inositol-5'-phosphatase 1 (SHIP1) containing the SH2 structural domain (IC50 : 2.5 μM) for research and immune-related diseases.

AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2]. AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM.

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.

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].

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

Stafib-1 is a selective inhibitor of STAT5β targeting SH2 domain with an IC50 of 154 nM and a Ki of 44 nM.

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

K118 is an inhibitor of SH2-containing inositol 5' phosphatase 1 (SHIP1). It reverses diet- and age-associated obesity and metabolic syndrome.

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.

AC-4-130, a powerful inhibitor of the SH2 domain of STAT5, effectively hinders STAT5 activation, dimerization, nuclear translocation, and transcription of genes reliant on STAT5. This compound directly binds to STAT5, ultimately leading to cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 exhibits notable anti-cancer properties and effectively suppresses abnormal STAT5 activity in acute myeloid leukemia (AML), making it a promising therapeutic option [1].

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.

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

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

STAT3-IN-10 (A11) is an inhibitor of STAT3 that directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells (IC 50 = 5.18 μM) [1].

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.