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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
202 Results for "
binding assays
" in MedChemExpress (MCE) Product Catalog:
Products (202)
202 Results for "binding assays" in MCE Product Catalog:
2
Forschungsgebiete:
Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis .
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2 Cited Publications
Synonyms: Cdc42-IN-1
CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe .
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2 Cited Publications
Synonyms: LY2940680
Taladegib is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC50 of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC50 of 7.6 nM in CGNP cell proliferation assays. Taladegib binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib can be used in studies of Hedgehog pathway-related cancers .
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Taladegib (LY2940680) hydrochloride is a Smoothened (SMO) antagonist. Taladegib hydrochloride inhibits the Hedgehog signaling pathway, with an IC50 of 5.5 nM for suppressing GLI1 mRNA expression in DAOY cells and an IC50 of 7.6 nM in CGNP cell proliferation assays. Taladegib hydrochloride binds to the extracellular loop region (site 1) of the transmembrane domain of the SMO receptor, competes with cyclopamine for SMO binding, and thereby inhibits Gli-dependent transcription. Taladegib hydrochloride can be used in studies of Hedgehog pathway-related cancers .
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1 Cited Publications
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TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis .
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1 Cited Publications
Synonyms: LXI-15029
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MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .
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Oxprenolol hydrochloride (Ba 39089) is an orally bioavailable β-adrenergic receptor (β-AR) antagonist with a Ki of 7.10 nM in a radioligand binding assay using rat heart muscle .
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SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels .
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1 Cited Publications
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PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
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1 Cited Publications
Art. -Nr.: HY-P1376A
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1 Cited Publications
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CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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1 Cited Publications
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TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM .
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1 Cited Publications
PKN1/2-IN-1 is a potent cell permeabilizer and selective PKN1/2 inhibitor with IC50 values of 16 nM and 210 nM for PKN1 and PKN2, respectively, and Ki values of 8 nM and 108 nM, respectively. PKN1/2-IN-1 exhibits strong intracellular PKN2 binding capacity in NanoBRET assays (IC50 = 2.1 μM). PKN1/2-IN-1 can be used to study physiological processes such as tumor cell migration .
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1 Cited Publications
Art. -Nr.: HY-17378
CAS. Nr.: 429658-95-7
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Dabigatran ethyl ester is an inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) and thrombin. Dabigatran ethyl ester inhibits NADH-dependent metabolism of mitomycin C mediated by purified recombinant human NQO2 .
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1 Cited Publications
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T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay .
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1 Cited Publications
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4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC50 values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [ 3H]-CQ competition assay and TR-FRET assay, respectively. The EC50 of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC50 in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP + or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease .
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1 Cited Publications
Art. -Nr.: HY-D1423
CAS. Nr.: 68654-25-1
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Dibromobimane is a Fluorescent dye and probe that can be used for the detection of intracellular reduced glutathione and the analysis of spatial proximity of closely adjacent cysteine thiol groups. Dibromobimane activates fluorescence through binding to thiol groups; its excitation/emission wavelengths are Ex/Em = 393/477 nm for glutathione detection, and Ex/Em = 385/477 nm for cysteine thiol cross-linking. Dibromobimane uses two equivalent bromomethyl groups to cross-link cysteine thiolates with a distance ranging from 3-6 Å. Dibromobimane can be applied to 96-well microplate-based high-throughput assays for labeling intracellular glutathione, and its fluorescence signal is normalized against nuclear staining results to eliminate the impact of cell density .
Art. -Nr.: HY-D1314
CAS. Nr.: 1386385-76-7
Synonyms: 6-FAM azide
Art. -Nr.: HY-P0179
CAS. Nr.: 72122-62-4
Synonyms: β-Casomorphin-7 (bovine); Bovine β-casomorphin-7
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BODIPY FL thalidomide is a high-affinity and selective human cereblon (CRBN)-targeting fluorescent probe with a Kd of 3.6 nM. BODIPY FL thalidomide enables use as a probe in time-resolved fluorescence resonance energy transfer (TR-FRET) binding assays for cereblon ligands. BODIPY FL thalidomide supports development of highly sensitive, selective, stable cereblon TR-FRET binding assays (Ex/Em = 502/510 nm) .
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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
