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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
71 Results for "
SH2 domain
" in MedChemExpress (MCE) Product Catalog:
Products (71)
71 Results for "SH2 domain" in MCE Product Catalog:
314
314 Publications Verification
Research Areas:
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 SH2 domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .
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36
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C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .
9
9 Cited Publications
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.
8
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3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
8
8 Cited Publications
AC-4-130 is a potent STAT5 SH2 domain 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) .
3
3 Cited Publications
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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-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs) .
2
2 Cited Publications
Research Areas:
SI-109 is a potent STAT3 SH2 domain 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 .
1
1 Cited Publications
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STAT6-IN-1 (Compound 19a) is a STAT6 inhibitor with a high affinity for the SH2 domain 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 .
1
1 Cited Publications
Cat. No.: HY-18685
CAS No.: 1415834-63-7
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CPDA is a novel potent SH2 domain-containing inositol phosphatase 2 (SHIP2) inhibitor.
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1
1
1 Cited Publications
Cat. No.: HY-P3279
CAS No.: 147612-86-0
1
1 Cited Publications
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MN551 is a covalent modulator of SOCS2 and CISH, with selectivity for SOCS2 and CISH over SOCS4. MN551 covalently modifies Cys111 in the SH2 domain of SOCS2 and Cys144 in the EF loop of the CISH SH2 domain, while only minimally modifying Cys471 in the BG loop of the SOCS6 SH2 domain. MN551 increases the thermal stability of the recombinant SOCS2-ElonginB-ElonginC complex and competitively blocks the binding of SOCS2 to its substrate; when delivered via the prodrug MN714, it blocks the intracellular recruitment of substrates by SOCS2. MN551 can serve as a chemical probe for investigating the biological functions of SOCS2 and its CRL5 complex, and also act as an E3 ligase-binding module in proteolysis-targeting chimeras (PROTACs) .
1
1 Cited Publications
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STAT3-IN-13 (compound 6f) is a potent STAT3 inhibitor. STAT3-IN-13 has anti-proliferative effects and binds to the STAT3 SH2 domain 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 .
1
1 Cited Publications
Cat. No.: HY-P80518
Synonyms: ORCA, OSIL, SQSTM1, Sequestosome-1, EBI3-associated protein of 60 kDa, Phosphotyrosine-independent ligand for the Lck SH2 domain of 62 kDa, Ubiquitin-binding protein p62, EBIAP, p60, p62
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STAT6-IN-3 is a phosphopeptide mimic targeting the SH2 domain of STAT6 and has a high affinity for STAT6 (IC50: 0.04 μM). STAT6-IN-3 can be used in the research of inflammation such as asthma .
Cat. No.: HY-W035137
CAS No.: 22112-89-6
Synonyms: 5,15-DPP
5,15-Diphenylporphyrin (5,15-DPP) is an inhibitor of the oncogenic transcription factor STAT3. 5,15-Diphenylporphyrin specifically binds to the SH2 domain of STAT3, blocking the pTyr-SH2 interaction, thereby inhibiting the dimerization, nuclear translocation and DNA binding activity of STAT3, and ultimately inhibiting the expression of cancer cell-related genes. 5,15-Diphenylporphyrin can be used in research fields related to the development of anticancer drugs[1][2].
Cat. No.: HY-146127
CAS No.: 3069455-54-2
STAT3-SH2 domain inhibitor 1 is a potent Src Homology 2 (SH2) Domain of STAT3 (STAT3-SH2 domain) inhibitor with a Kd value of 1.57 μM. STAT3-SH2 domain inhibitor 1 inhibits STAT3 signaling transduction and transcriptional activation. STAT3-SH2 domain inhibitor 1 induces apoptosis in gastric cancer cells. STAT3-SH2 domain inhibitor 1 can be used in research of cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
