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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
25 Results for "
THP-1 human monocytes
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "THP-1 human monocytes" in MCE Product Catalog:
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2
2 Cited Publications
Research Areas:
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2 Cited Publications
Target:
PF-04217903 is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
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2 Cited Publications
Cat. No.: HY-122542A
CAS No.: 82188-90-7
Synonyms: Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl
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PPACK dihydrochloride is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK dihydrochloride specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK dihydrochloride exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK dihydrochloride binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK dihydrochloride is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases .
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2 Cited Publications
Target:
PF-04217903 mesylate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 mesylate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 mesylate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 mesylate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 mesylate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 mesylate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
Cat. No.: HY-157421
CAS No.: 2847156-05-0
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Nampt activator-4 is an orally active NAMPT activator, with an EC50 of 58 nM and a Ka of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD +, thereby enhancing enzymatic activity and significantly increasing intracellular NAD + levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders .
Cat. No.: HY-P11072
CAS No.: 1601299-92-6
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Cat. No.: HY-122542
CAS No.: 71142-71-7
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Cat. No.: HY-B1451
CAS No.: 89396-94-1
Synonyms: TA-6366
Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions .
Synonyms: HMC-C-01-A; MBS2320
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Leramistat (HMC-C-01-A; MBS2320) is a mitochondrial complex 1 inhibitor, involving in cell metabolism immune metabolism regulation. Leramistat also inhibits ATP production in Thp1 human monocytes (IC50: 0.63 μM). Leramistat inhibits atopic dermatitis and other skin diseases autoimmune diseases, inflammatory diseases, cancer; and also inhibits osteoclast mediated disease .
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Pomalidomide-PEG1-azide is an E3 ligase lgand-linker conjugate. Pomalidomide-PEG1-azide incorporates the Pomalidomide based cereblon ligand and a linker. Pomalidomide-PEG1-azide can be used to synthesis PROTAC BRD4 Degrader-1 (HY-133131) . PROTAC BRD4 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 41.8 nM against BRD4 BD1. PROTAC BRD4 Degrader-1 can effectively degrade BRD4 protein and suppress c-Myc expression.
Cat. No.: HY-145726
CAS No.: 250755-32-9
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ISIS 104838 is an antisense oligonucleotide targeting TNF-α. ISIS 104838 specifically binds to human TNF-α mRNA via Watson-Crick base pairing to form a DNA:RNA hybrid duplex, thereby recruiting the ubiquitously expressed intracellular enzyme RNase H to degrade the target mRNA and inhibit TNF-α protein synthesis at the transcriptional level. ISIS 104838 induces moderate, self-limiting thrombocytopenia in cynomolgus monkeys. ISIS 104838 can be used for the study of inflammatory diseases .
Cat. No.: HY-171692
CAS No.: 2780391-08-2
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G3-YSD is a cGAS agonist. G3-YSD directly interacts with cGAS to enhance its enzymatic activity, promote the conversion of ATP and GTP into cGAMP, and trigger STING-dependent IFN-α/β secretion. G3-YSD acts as a viral mimic to replace actual viral DNA . G3-YSD is applicable to research related to long COVID and type 1 human immunodeficiency virus infection .
Cat. No.: HY-134375
CAS No.: 1507367-51-2
Synonyms: Cyclic Adenosine-Inosine Monophosphate
Research Areas:
cAIMP (Cyclic Adenosine-Inosine Monophosphate) is an effective synthetic cyclic dinucleotide. cAIMP activates IRF and NF-κB in the THP1 human monocyte reporter cell line (THP1-Dual). cAIMP induces the secretion of IFNs and pro-inflammatory cytokines in vitro in human blood, with an EC50 of 6.4 μmol/L .
Cat. No.: HY-163280
CAS No.: 3011930-28-9
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JGB-1-155 is a nicotinamide phosphoribosyltransferase (NAMPT) activator and also a reactive oxygen species (ROS) inhibitor. JGB-1-155 binds to NAMPT, thereby enhancing its catalytic activity and increasing intracellular NAD + levels. JGB-1-155 alleviates the elevation of ROS levels induced by various types of damage. JGB-1-155 can be used in research related to neurodegenerative diseases .
Cat. No.: HY-12017B
CAS No.: 1159490-85-3
Target:
PF-04217903 phenolsulfonate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 phenolsulfonate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 phenolsulfonate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 phenolsulfonate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 phenolsulfonate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 phenolsulfonate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
Cat. No.: HY-124693
CAS No.: 869767-86-2
DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34+ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia[1].
Cat. No.: HY-184797
Target:
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Zp17 is a PROTAC degrader that targets the STING protein for degradation by recruiting cereblon, with a DC50 of 956 nM in THP-1 cells. Zp17 induces proteasome-dependent STING protein degradation and inhibits the activity of the STING signaling pathway. Zp17 alleviates renal function injury in a mouse model of acute kidney injury induced by Cisplatin (HY-17394). Zp17 exhibits STING-degrading activity in human monocytes and STING-inhibiting activity in mouse macrophage reporter cells. Zp17 can be used for research on inflammation and acute kidney injury .
Cat. No.: HY-150941
CAS No.: 2133902-07-3
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BRD4 ligand 2 is a BRD4 BD1 inhibitor with an IC50 of 46.4 nM. BRD4 ligand 2 inhibits the proliferation of lymphoma cells. BRD4 ligand 2 also serves as a target protein ligand for PROTACs, and is used in the synthesis of PROTAC BRD4 Degrader-1 (HY-133131). BRD4 ligand 2 is applicable to research related to lymphoma .
Cat. No.: HY-183530
CAS No.: 152121-51-2
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p38 MAPK-IN-11 is a CSBP (p38 MAPK) kinase inhibitor with IC50 values of 0.15 μM (binding activity) and 0.21 μM (inhibitory activity). p38 MAPK-IN-11 shows weak inhibitory activity against PKCα kinase, with an IC50 of 7.6 μM. p38 MAPK-IN-11 inhibits the production of IL-1. p38 MAPK-IN-11 also acts as a β-lactam antibiotic potentiator, but has no antibacterial activity itself .
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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
