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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
18 Results for "
MAPK recruitment
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "MAPK recruitment" in MCE Product Catalog:
2
2 Cited Publications
LC-2 is an orally active PROTAC-class degrader targeting KRAS G12C and a MAPK inhibitor. LC-2 shows higher selectivity for KRAS G12C than wild-type KRAS and other KRAS mutants. LC-2 covalently binds to KRAS G12C via the MRTX849 (HY-130149) warhead, recruits the VHL E3 ligase to form a ternary complex, and induces ubiquitination and degradation of KRAS G12C. Meanwhile, LC-2 inhibits the MAPK signaling pathway, reduces the phosphorylation levels of CRAF and AKT, thereby inducing apoptosis and suppressing cancer cell and tumor growth. LC-2 can be used for the research of KRAS G12C-positive cancers, including non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-P10408
CAS No.: 1906866-53-2
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MD13 is a MIF PROTAC degrader with a DC50 of approximately 100 nM. MD13 induces ubiquitination and degradation of MIF by recruiting the Cereblon Cullin RING E3 ubiquitin ligase complex. MD13 inactivates the MAPK pathway and induces G2/M phase cell cycle arrest. MD13 exhibits antiproliferative effects in 3D tumor spheroid models. MD13 can be used in lung cancer-related research .
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PROTAC RIPK degrader-6 (Example 1) is a RIPK2 PROTAC degrader that recruits cereblon. PROTAC RIPK degrader-6 recruits the CRBN E3 ubiquitin ligase complex and induces the degradation of RIPK2 kinase via the ubiquitin-proteasome pathway, thereby blocking NOD1/NOD2-mediated pro-inflammatory signaling pathways of NF-κB and MAPK. PROTAC RIPK degrader-6 can be used in research related to RIPK2-mediated autoinflammatory diseases and cancer .
Cat. No.: HY-P3012
CAS No.: 107200-92-0
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Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases .
Cat. No.: HY-175435
CAS No.: 3094183-98-6
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CST905 is a potent BRAF-V600E PROTAC degrader with a DC50 of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma .
Cat. No.: HY-179047
CAS No.: 3040320-18-8
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SMU-L11-R is a selective TLR7 agonist with an EC50 of 0.012 μM for human TLR7. SMU-L11-R specifically activates TLR7, recruits MyD88, and triggers MAPK/NF-κB pathways, leading to TNF-α/IL-1β/IL-6 secretion in both mouse and human peripheral blood mononuclear cells. SMU-L11-R promotes M1-like macrophage polarization. SMU-L11-R exhibits excellent synergistic anti-tumor effects with PD-L1 inhibitors by upregulating CD8 +T cells. SMU-L11-R shows potential in colorectal cancer studies .
Cat. No.: HY-174858
CAS No.: 3100207-58-4
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dASK1-VHL is an ASK1 PROTAC degrader that recruits VHL. dASK1-VHL induces ubiquitination and proteasomal degradation of ASK1 by forming a ternary complex, and inhibits the downstream p38 MAPK signaling pathway. dASK1-VHL can be used in studies of metabolic dysfunction-associated steatohepatitis .
Cat. No.: HY-175273
MA191 is a FLT3 PROTAC degrader. MA191 targets and degrades mutant FLT3-ITD protein by recruiting the VHL E3 ligase in a manner dependent on ubiquitination and BIM, thereby blocking aberrant downstream MAPK/STAT5 signaling pathways and inducing apoptosis. MA191 can be used in research related to acute myeloid leukemia .
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SMU-L11 is a specific TLR7 agonist (EC50=0.024 μM), which recruits MyD88 adapter protein and activates downstream NF-κB and MAPK signaling pathways. In murine models, SMU-L11 significantly enhances immune cell activation and promotes the proliferation of CD4 + T and CD8 + T cells, thereby directly killing tumor cells and inhibiting tumor growth. SMU-L11 can be used for cancer research, and also has the potential for studying immune system diseases .
Cat. No.: HY-116088
CAS No.: 1345982-24-2
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W123, a FTY720 analog, is a competitive sphingosine 1-phosphate type 1 (S1P1) receptor antagonist. W123 is measured by GTPγS activation, MAPK recruitment, cell migration, and ligand-induced receptor internalization .
Cat. No.: HY-119234
CAS No.: 41609-06-7
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CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .
Cat. No.: HY-173437
CW-2 is a CRBN-recruited PARP1 PROTAC degrader. CW-2 triggers multiple downstream biological effects including DNA damage accumulation, impaired DNA repair, mitochondrial-mediated apoptosis, intracellular ROS buildup and G1/S cell cycle arrest, as well as the regulation of oxidative phosphorylation, p53, PI3K-Akt and MAPK alongside ubiquitin proteolysis pathways. CW-2 enhances cell membrane permeability and intracellular platinum enrichment, exhibits detectable pharmacokinetic profiles after intraperitoneal administration in rats and drives differential gene expression. CW-2 can be applied to research on triple-negative breast cancer, non-small cell lung cancer, cisplatin-resistant non-small cell lung cancer, colon cancer and pancreatic cancer .
Cat. No.: HY-187182
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MH-06 is an orally active 12-lipoxygenase (ALOX12) PROTAC degrader. MH-06 specifically binds to ALOX12 and recruits E3 ubiquitin ligase to mediate ubiquitination and degradation of the target protein. MH-06 inhibits the MAPK signaling pathway, reduces the production of reactive oxygen species (ROS), restores mitochondrial function, regulates macrophage polarization and decreases the release of pro-inflammatory cytokines. MH-06 can be used for the research of acute pancreatitis .
Cat. No.: HY-189468
CAS No.: 3128784-74-4
PROTAC SHP2 degrader-1 is a potent SHP2 PROTAC degrader with a DC50 of 7.406 μM. PROTAC SHP2 degrader-1 recruits DCAF16 E3 ligase to induce ubiquitination and proteasomal degradation of SHP2, thereby inhibiting the RAS/MAPK and PI3K/AKT/mTOR signaling pathways while simultaneously inducing IFN-γ/JAK/STAT1, apoptosis, and cell cycle arrest. PROTAC SHP2 degrader-1 can be used for cancer research .
Cat. No.: HY-138834
CAS No.: 1042673-20-0
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JH-I-25 is an orally active IRAK1 and IRAK4 inhibitor. JH-I-25 inhibits LPS-induced IRAK4 phosphorylation, IRAK1 degradation, MAPK activation, and the expression of proinflammatory cytokines TNF-α and IL-6 in lung tissues. JH-I-25 improves the survival rate of LPS-induced septic mice and serves as an IRAK4 recruiter in the design of proteolysis-targeting chimeric molecules. JH-I-25 can be used in research related to diffuse large B-cell lymphoma, Waldenström's macroglobulinemia, septic shock, rheumatoid arthritis, atherosclerosis, Alzheimer's disease, acute lung injury, sepsis, and psoriasis .
Cat. No.: HY-167151
CAS No.: 2107327-36-4
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PaPE-1 is a pathway-preferential estrogen receptor (ER) agonist that preferentially activates ER non-nuclear-initiated signaling while minimally activating nuclear-initiated signaling. PaPE-1 exhibits Ki values of 10 μM and 25 μM for human ERα and ERβ, respectively. The relatively low ER affinity and rapid receptor dissociation of PaPE-1 facilitate the triggering of non-nuclear mTOR/MAPK/AKT signaling, while reducing the recruitment of ERα to chromatin and sustained nuclear ER-dependent transcription. PaPE-1 is suitable for research related to non-nuclear ER signaling, metabolic disorders, ischemic brain injury, Alzheimer's disease, and ER-positive breast cancer .
Cat. No.: HY-P992401
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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
