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STAT3-SH2domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2domain inhibitor 1 can be used in research of cancer .
STAT6-IN-3 (Compound 18a) is a STAT6 inhibitor (IC50= 44 nM). STAT6-IN-3 targets the Src Homology 2 (SH2) domain of STAT6. STAT6-IN-3 can be used for research of inflammation such as asthma .
EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2domains .
Syk-IN-6 is an inhibitor of the lipid-SH2domain interaction, control the cellular activity of kinases containing SH2domain. Syk-IN-6 blocks Syk kinase activity, which associated hematopoietic malignancies, including acute myeloid leukemia (AML) .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions .
AC-4-130 is a potent STAT5 SH2domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727) . Stattic inhibits the binding of a high affinity phosphopeptide for the SH2domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .
MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines .
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70SH2domain with immunoreceptor tyrosine-based activation motif (ITAMs) .
740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2domains of p85 but fails to bind GST alone .
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer [1].
740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2domains of p85 but fails to bind GST alone .
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a high affinity for the SH2domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer .
SI-109 is a potent STAT3 SH2domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36 .
C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).
STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2domain with a KD of 0.46 μM. STAT3-IN-13 inhibits the phosphorylation of STAT3 Y705 and downstream target gene expression. STAT3-IN-13 induces apoptosis in vitro and suppresses the growth and metastasis of tumor in vivo. STAT3-IN-13 can be used for cancer research .
STAT3-IN-20 (Compound 40) is a selective STAT3 inhibitor (IC50: 0.65 μM). STAT3-IN-20 binds the SH2domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC50: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis .
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Grb2 SH2domain inhibitor 1 TFA is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2domains .
Grb2 SH2domain inhibitor 1 is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions .
IRS1-derived peptide is a biological active peptide. (This is a peptide fragment (979-989) of the insulin receptor substrate-1 containing the sequence motif YMXM known to bind to the two domains of SH2 on the 85kDa subunit of phosphoinositide 3-kinase.)
740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2domains of p85 but fails to bind GST alone .
G7-18NATE is a peptide inhibitor of Grb7. HY-P10224 binds to the Grb7-SH2domain with micromolar affinity (KD = 18.1 μM). G7-18NATE inhibits cell proliferation, motility, cell invasion and 3D culture formation in several cancer cell lines .
740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2domains of p85 but fails to bind GST alone .
SH2D1A protein regulates receptors of the SLAM family (SLAMF1, CD244, LY9, CD84, SLAMF6, and SLAMF7). SH2D1A Protein, Human (His) is the recombinant human-derived SH2D1A protein, expressed by E. coli , with N-6*His labeled tag. The total length of SH2D1A Protein, Human (His) is 128 a.a., with molecular weight of ~16.0 kDa.
The SLP-76 protein is critical in T cell antigen receptor-mediated signaling and participates in multiple molecular interactions. Its association with SLA coordinates T cell signaling, whereas its interaction with CBLB emphasizes regulatory effects. SLP-76 Protein, Human (His-T7) is the recombinant human-derived SLP-76 protein, expressed by E. coli , with N-T7, C-6*His labeled tag. The total length of SLP-76 Protein, Human (His-T7) is 533 a.a., with molecular weight of ~70.0 kDa.
SHC1; SHC; SHCA; SHC-transforming protein 1; SHC-transforming protein 3; SHC-transforming protein A; Src homology 2 domain-containing-transforming protein C1; SH2 domain protein C1
