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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
173 Results for "
Multitarget
" in MedChemExpress (MCE) Product Catalog:
Products (173)
173 Results for "Multitarget" in MCE Product Catalog:
Cat. No.: HY-165527
CAS No.: 200398-40-9
Target:
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S18327 is a multi-target antipsychotic agent. S18327 exerts its efficacy by acting on multiple neurotransmitter systems in the brain, and it has antagonistic effects on dopamine receptors (particularly the D2 receptor) and 5-hydroxytryptamine 2A receptors (5-HT2A receptor). S18327 can counteract excessive dopamine activity and hypo-function of glutamate. S18327 exhibits a multi-parameter pharmacological profile that is highly similar to that of Clozapine (HY-14539). S18327 can produce the same discriminative stimulus as Clozapine, improve cognitive filtering deficits associated with schizophrenia, and display anxiolytic properties. S18327 has relatively weak affinity for histaminergic receptors and muscarinic receptors, which avoids the side effects of Clozapine .
Cat. No.: HY-182245
Research Areas:
Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
Cat. No.: HY-183796
Research Areas:
GFAP/NF-κB/APOE/NLRP3-IN-1 is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC50 of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC50 of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ1-42 aggregation with an IC50 of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma .
Cat. No.: HY-184292
Research Areas:
COX-2-IN-67 is an orally active, blood-brain barrier permeable multi-target inhibitor that potently targets COX-2 (IC50=0.07 μM), hCA IX (Ki=62.7 nM) and hBuChE (IC50=0.47 μM). COX-2-IN-67 alleviates oxidative stress and liver stress, improves glucose homeostasis and insulin sensitivity, and optimizes lipid profiles. Meanwhile, COX-2-IN-67 effectively reduces the levels of neuroinflammatory markers and improves hippocampus-dependent cognitive function in a high-fat diet-induced rat model. COX-2-IN-67 can be used for the research of metabolic dysfunction-associated mild cognitive impairment .
Cat. No.: HY-184385
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PI3K/AKT/JAK2-IN-1 is a potent multi-target inhibitor of the PI3K/AKT/JAK2 signaling pathway. PI3K/AKT/JAK2-IN-1 suppresses NO production (IC50 = 1.0 μM), reduces pro-inflammatory cytokines (TNF-α, IL-6, IL-1β, IL-17A, IL-22), and inhibits keratinocyte hyperproliferation by downregulating Ki67 and PCNA. PI3K/AKT/JAK2-IN-1 can be used for psoriasis research .
Cat. No.: HY-184652
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LRRK2/JNK3-IN-1 is a brain-penetrant multi-target inhibitor of LRRK2 (including G2019S mutant and wild-type) and JNK3, with enzymatic IC50 values of 3.90 nM against LRRK2 G2019S, 3.24 nM against wild-type LRRK2, and 22.1 nM against JNK3. LRRK2/JNK3-IN-1 displays favorable selectivity in a 97-kinase profiling screen, and also shows inhibitory activity against JNK1, JNK2, and MKNK2. LRRK2/JNK3-IN-1 can be used for the research of Parkinson's disease .
Cat. No.: HY-114510
CAS No.: 1020399-52-3
PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC50 of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia .
Cat. No.: HY-119618
CAS No.: 303196-31-8
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R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
Cat. No.: HY-164530
CAS No.: 1970149-05-3
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
Cat. No.: HY-186224
CAS No.: 118458-58-5
GW296115 is a multi-target inhibitor with the following IC50 values against its targets: 8.4 nM for BRSK2, 21 nM for BRSK1, 1.8 μM for PDGFRβ, 5.5 nM for STK17B/DRAK2, 28 nM for DRAK1, 20 nM for PHKG1, and 89 nM for DCAMKL3. GW296115 downregulates the phosphorylation of S317 site on ULK1 and S351 site on P62, which are AMPK substrates driven by BRSK2. GW296115 does not alter the phosphorylation level of AMPK at T172, reduces nutrient deprivation-mediated Autophagy and autophagosome formation, and enhances Apoptosis. GW296115 exhibits anticancer activity against triple-negative breast cancer. GW296115 is applicable for breast cancer-related research .
Cat. No.: HY-B0380
CAS No.: 39133-31-8
Target:
Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Trimebutine is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Cat. No.: HY-B0380A
CAS No.: 34140-59-5
Target:
Opioid Receptor Toll-like Receptor (TLR) Calcium Channel Potassium Channel IRAK ERK JNK NF-κB Akt Apoptosis
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Trimebutine maleate is a multi-target inhibitor and opioid receptor agonist with antimuscarinic activity. Trimebutine maleate inhibits L-type Ca 2+ channels and large-conductance calcium-activated potassium channels (BKCa channels), thereby inhibiting extracellular calcium influx and potassium ion efflux. Trimebutine maleate also targets Toll-like receptors, inhibits Toll-like receptor 2/4/7/8/9 signals, and inhibits LPS-induced IRAK1 activation, as well as ERK1/2, JNK and NF-κB activation, thereby exerting anti-inflammatory effects. Trimebutine maleate also induces tumor cell apoptosis by inhibiting the AKT/ERK pathway. Trimebutine maleate also inhibits excessive contraction of smooth muscle and can be used in the study of gastrointestinal disorders such as irritable bowel syndrome (IBS) .
Cat. No.: HY-N1255A
CAS No.: 51486-68-1
Synonyms: (-)-Scoulerine hydrochloride; Discretamine hydrochloride
Cat. No.: HY-114214
CAS No.: 626252-75-3
Target:
Drug Derivative NF-κB MMP TNF Receptor Interleukin Related Cyclin G-associated Kinase (GAK) CDK PI3K Akt
Research Areas:
CKD-712 is an orally active multi-target tetrahydroisoquinoline derivatived and a potent inhibitor of the NF-κB pathway . CKD-712 selectively inhibits MMP-9 with no effect on MMP-2, downregulates the expression of TNF-α, IL-6, cyclin A, cyclin B, CDK-1 and other proteins, and activates the PI3K/Akt signaling pathway . CKD-712 blocks the activation and nuclear translocation of NF-κB, downregulates inflammatory factors and pro-tumor metastatic proteins, and induces G2/M phase arrest in tumor cells and thereby inhibits the invasion of cancer cells . CKD-712 can be used for the research of sepsis, myocardial ischemia-reperfusion injury and non-small cell lung cancer .
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1 .
Cat. No.: HY-B0380S1
CAS No.: 2747915-18-8
Cat. No.: HY-B0380S2
Cat. No.: HY-P11617
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Research Areas:
Cat. No.: HY-111137
CAS No.: 916890-10-3
Synonyms: XC-302 free base
Puquitinib (XC-302 free base) is a multi-target inhibitor with the activity of inducing autophagy in nasopharyngeal carcinoma cells by inhibiting the PI3K/AKT/mTOR signaling pathway. Puquitinib was able to inhibit the proliferation of CNE-2 cells, showing a dose-dependent antiproliferative effect. Puquitinib induced the formation of autophagosomes and autolysosomes in CNE-2 cells, which were observed by fluorescence microscopy and electron microscopy. Puquitinib promoted the formation of LC3-II and increased the expression of beclin 1, while reducing the level of p62. Puquitinib inhibited the PI3K/AKT/mTOR pathway by reducing the expression of p-AKT and p-mTOR. Puquitinib also induced apoptosis in CNE-2 cells, and when autophagy was inhibited, the apoptosis rate was reduced, which means that autophagy may interact with apoptosis to induce cell death .
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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
