Search Result
Results for "
binding assays
" in MedChemExpress (MCE) Product Catalog:
8
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-145817A
-
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RP-6306
|
Wee1
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Cancer
|
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lunresertib (RP-6306) is a potent, selective and orally active PKMYT1 inhibitor with an IC50 of 14 nM. lunresertib shows a high degree of selectivity over other kinases in cellular binding assays. lunresertib shows anticancer effects .
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-
-
- HY-15682
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TTNPB
5 Publications Verification
Ro 13-7410; Arotinoid acid; AGN191183
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RAR/RXR
Autophagy
Apoptosis
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Cancer
|
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TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
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-
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- HY-13928
-
-
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- HY-103663
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MAK683
4 Publications Verification
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Histone Methyltransferase
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Cancer
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MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay .
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-
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- HY-134471
-
|
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TNF Receptor
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Inflammation/Immunology
Cancer
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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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- HY-10569
-
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ACT-128800
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LPL Receptor
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Inflammation/Immunology
|
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Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-127111
-
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ATP Citrate Lyase
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Cancer
|
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NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate .
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-
-
- HY-122611A
-
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Androgen Receptor
Apoptosis
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Cancer
|
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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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- HY-D1314
-
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6-FAM azide
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Fluorescent Dye
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Others
|
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FAM azide, 6-isomer (6-FAM azide) is a 6-carboxyfluorescein derivative with an azide functional group and coupling partner in copper-catalyzed azide-alkyne cycloaddition. FAM azide, 6-isomer participates in synthesis of fluorescently tagged disparlure enantiomers for pheromone-binding protein binding assays. FAM azide, 6-isomer is widely used for labeling oligonucleotides (Ex/Em = 493/517 nm) .
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-
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- HY-16582A
-
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Erismodegib; LDE225; NVP-LDE225
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Smo
|
Cancer
|
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Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
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- HY-10858
-
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sFRP-1
Wnt
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Cancer
|
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WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM .
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- HY-126077
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MTI-31
1 Publications Verification
LXI-15029
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mTOR
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Inflammation/Immunology
Cancer
|
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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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- HY-16582
-
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Erismodegib diphosphate; LDE225 diphosphate; NVP-LDE225 diphosphate
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Smo
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Cancer
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Sonidegib diphosphate (Erismodegib diphosphate) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
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- HY-P0179
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-
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- HY-10835
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DG-041
3 Publications Verification
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Prostaglandin Receptor
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Cardiovascular Disease
|
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DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier .
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- HY-10037
-
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MK-591
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FLAP
Apoptosis
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Inflammation/Immunology
|
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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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- HY-152231
-
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Fluorescent Dye
Ligands for E3 Ligase
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Others
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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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- HY-136379
-
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Cdc42-IN-1
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Ras
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Cancer
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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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- HY-B1486
-
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Ba 39089
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Adrenergic Receptor
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Cardiovascular Disease
|
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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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- HY-115510
-
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SPRi3
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Carbonyl Reductase
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Inflammation/Immunology
|
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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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- HY-12220A
-
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HMTase Inhibitor IX TFA
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WDR5
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Cancer
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MM-102 TFA (HMTase Inhibitor IX TFA) is a potent WDR5/MLL interaction inhibitor, achieves IC50 = 2.4 nM with an estimated Ki < 1 nM in WDR5 binding assay, which is >200 times more potent than the ARA peptide.
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- HY-P1096
-
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Cholecystokinin Receptor
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Metabolic Disease
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A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
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- HY-120635
-
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PD-1/PD-L1
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Inflammation/Immunology
Cancer
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BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
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- HY-P9949
-
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Sch 55700; CDP-835; JES1-39D10
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Interleukin Related
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Inflammation/Immunology
|
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Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
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- HY-19381
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-
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- HY-P4581
-
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Suc-ALPF-pNA
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FKBP
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Others
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Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a synthetic polypeptide substrate that targets FK506-binding protein (FKBP). Suc-Ala-Leu-Pro-Phe-pNA can be used to determine peptidyl-prolyl cis-trans isomerase activity via the chymotrypsin-coupled assay. Suc-Ala-Leu-Pro-Phe-pNA serves as a substrate for human FK506-binding protein hFKBP-12 in the chymotrypsin-FKBP coupled PPIase assay. Suc-Ala-Leu-Pro-Phe-pNA is applicable for the detection and research of PPIase activity .
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- HY-13466
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-
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- HY-16999
-
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
|
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RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
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- HY-107587
-
|
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Integrin
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Inflammation/Immunology
|
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A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively .
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-
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- HY-100383
-
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BHI1
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Bcl-2 Family
MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
|
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BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
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- HY-W755033
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-
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- HY-112157
-
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Beta-secretase
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Neurological Disease
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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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-
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- HY-14460
-
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FLAP
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Inflammation/Immunology
|
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AM679 is a potent, selective 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 2 nM in a human FLAP membrane binding assay. AM679 markedly reduces the respiratory syncytial virus-driven ocular pathology as well as the synthesis of cysteinyl leukotrienes (CysLTs) in the eye .
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- HY-D1190
-
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RAR/RXR
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Others
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DC271 is a RAR agonist and synthetic retinoid that binds to the retinoid-binding site of cellular retinoic acid-binding protein II (CRBP-II). DC271 exhibits solvatochromic fluorescence properties: it produces intense blue-shifted emission in nonpolar environments and weak red-shifted emission in polar environments, and its severe fluorescence quenching in aqueous solutions can be reversed by embedding in the hydrophobic retinoid-binding protein pocket. DC271 enables direct detection of the binding between unlabeled compounds and related retinoid-binding proteins via fluorescence competition assays (Ex/Em = 355 nm/460 nm) .
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- HY-174962A
-
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Biochemical Assay Reagents
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Others
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mPEG2000-Biotin is a biotin-conjugated PEG derivative used for biotinylation of biomolecules or other surfaces. Biotin can be detected by biotin/streptavidin binding assays and is widely used for molecular target detection .
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- HY-10858A
-
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sFRP-1
Wnt
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Cancer
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WAY 316606 hydrochloride is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM .
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- HY-176537
-
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Microtubule/Tubulin
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Cancer
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RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
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- HY-W436424
-
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DNA/RNA Synthesis
|
Infection
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DMA-IN-1 is a DNA adenine methyltransferase (DAM) inhibitor, IC50: 48 μM. DMA-IN-1 inhibits Caulobacter growth with an MIC of 35 μM .
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- HY-151884
-
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c-Myc
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Cancer
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FUBP1-IN-2 (compound 9) is a potent FUBP1 (far upstream binding protein 1) inhibitor. FUBP1-IN-2 inhibits the KH4 FUBP1-FUSE interaction in a gel shift assay. FUBP1-IN-2 binds to FUBP1 in a ChIP assay. FUBP1-IN-2 reduces both c-Myc mRNA and protein expression, increases p21 mRNA and protein expression, and depletes intracellular polyamines .
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-
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- HY-122611
-
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Androgen Receptor
Apoptosis
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Cancer
|
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CSRM617 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 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
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- HY-128466
-
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Biochemical Assay Reagents
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Others
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N-Biotinyl-L-cysteine is a biotinylated biochemical assay reagent, which is used to detect avidin and biotin through a competitive binding reaction .
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- HY-P5367
-
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PMDM6-F
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Fluorescent Dye
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Others
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5-FAM-PMDM6 (PMDM6-F) is a biological active peptide. (PMDM6-F is a fluorescent-labeled probe for MDM2-binding assay.)
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- HY-175250
-
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TNF Receptor
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Inflammation/Immunology
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TNF-α-IN-25 is an orally active TNF-α inhibitor. TNF-α-IN-25 shows Fluorescence Polarization (FP) assay IC50 of 103 nM in FP binding assays and L929 assay IC50 of 505 nM in cell-based assays. TNF-α-IN-25 inhibits paw swelling in the glucose-6-phosphate isomerase (GPI) arthritis model. TNF-α-IN-25 can be used for the study of arthritis .
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- HY-123434
-
-
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- HY-128111
-
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Transmembrane Glycoprotein
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Neurological Disease
|
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ASN02563583, a compound that regulates the activity of the GPR17 receptor, has a IC50 value of 0.64 nM in [35S]GTPγS binding assay. ASN02563583 can be used in the study of neurological diseases .
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- HY-B1486AS
-
-
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- HY-103663A
-
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Histone Methyltransferase
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Cancer
|
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MAK683 hydrochloride is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay .
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- HY-14250
-
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Androgen Receptor
|
Endocrinology
|
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PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC50 of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research .
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-
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- HY-120647
-
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PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
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BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
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- HY-B1486A
-
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Ba 39089 free base
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Adrenergic Receptor
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Cardiovascular Disease
|
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Oxprenolol (Ba 39089 free base) 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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- HY-119544
-
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UP-2696
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Angiotensin Receptor
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Cardiovascular Disease
|
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Ripisartan (UP-2696) is an angiotensin II receptor antagonist. Ripisartan is orally available. Ripisartan binds to angiotensin II receptors, dilates blood vessels, and lowers blood pressure .
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- HY-16582AR
-
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Erismodegib (Standard); LDE225 (Standard); NVP-LDE225 (Standard)
|
Smo
Reference Standards
|
Cancer
|
|
Sonidegib (Standard) is the analytical standard of Sonidegib. This product is intended for research and analytical applications. Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
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- HY-144397
-
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Glucocorticoid Receptor
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Inflammation/Immunology
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LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical research., LEO 134310 showed high affinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases .
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- HY-B1486S
-
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Ba 39089-d7
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Adrenergic Receptor
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Cardiovascular Disease
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Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. 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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- HY-14442
-
-
- HY-108507
-
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Smo
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Cancer
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MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .
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- HY-13928R
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-
- HY-123928
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-
- HY-116065
-
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5-HT Receptor
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Neurological Disease
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CUMI-101 (compound 8) is a 5-HT1AR agonist (Ki=0.15 nM) with an EC50 of 0.1 nM in the [35S]GTPγS binding assay. CUMI-101 can be used in the research of neurological diseases .
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- HY-169415
-
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WDR5
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Others
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DBL-6-13 is an inhibitor for WDR5 with a moderate binding affinity of 6.8 μM (microscale thermophoresis assay) and 9.1 μM (fluorescence polarization assay) .
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- HY-147366
-
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Lipocalin Family
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Metabolic Disease
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RBP4 ligand-1 is a non-retinoid ligands for (RBP4) retinol-binding protein 4. The hRBP4SPA IC50 and RBP4-TTR FRET IC50 values are 0.23±0.11 and 0.13±0.12 μM in the radioligand binding assay and FRET assay, respectively .
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- HY-120134
-
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Angiotensin Receptor
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Cardiovascular Disease
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BMS 183920 is a diacidic and potent angiotensin II receptor antagonist, with a Ki value of 2.9 nM in the rat adrenal cortex binding assay and a KB value of 0.061 nM in the rabbit aorta functional assay. BMS 183920 can be used for research of antihypertensive .
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- HY-P0179A
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- HY-16582AS
-
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Erismodegib-d4; LDE225-d4; NVP-LDE225-d4
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Isotope-Labeled Compounds
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Others
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Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
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- HY-144784
-
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CXCR
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Inflammation/Immunology
Cancer
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CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
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- HY-144783
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CXCR
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Inflammation/Immunology
Cancer
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CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM) [ 1].
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- HY-144781
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CXCR
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Inflammation/Immunology
Cancer
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CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM) [ 1].
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- HY-U00423
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-
- HY-160292
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- HY-174962B
-
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Biochemical Assay Reagents
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Others
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mPEG5000-Biotin is a biotin-conjugated PEG derivative used for biotinylation of biomolecules or other surfaces. Biotin can be detected by biotin/streptavidin binding assays and is widely used for molecular target detection .
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- HY-174962
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Biochemical Assay Reagents
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Others
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mPEG1000-Biotin is a biotin-conjugated PEG derivative used for biotinylation of biomolecules or other surfaces. Biotin can be detected by biotin/streptavidin binding assays and is widely used for molecular target detection .
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- HY-120760
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Lipoxygenase
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Others
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L-691831 is a ligand for 5-lipoxygenase activating protein binding assays that has utility as a tool for studying 5-lipoxygenase activating protein (FLAP) related activities. L-691831 can be used to measure the affinity of FLAP on the leukocyte membrane for leukotriene synthesis inhibitors, with binding being correlated with inhibition of leukotriene synthesis.
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- HY-W008226R
-
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2,4,6-trihydroxyacetophenone (Standard); 1-(2,4,6-Trihydroxyphenyl)ethanone (Standard)
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Reference Standards
Cytochrome P450
Bacterial
Antibiotic
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Infection
Metabolic Disease
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Oxprenolol (hydrochloride) (Standard) is the analytical standard of Oxprenolol (hydrochloride). This product is intended for research and analytical applications. 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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- HY-B1486R
-
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Ba 39089 (Standard)
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Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
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Oxprenolol (hydrochloride) (Standard) is the analytical standard of Oxprenolol (hydrochloride). This product is intended for research and analytical applications. 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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- HY-14250A
-
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Androgen Receptor
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Endocrinology
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(Rac)-PF-998425 is a potent, selective, nonsteroidal androgen receptor (AR) antagonist. (Rac)-PF-998425 has IC50 values of 26 and 90 nM in the AR binding and cellular assays, respectively. (Rac)-PF-998425 has the potential for the research of the androgenetic alopecia .
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- HY-149005
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Histone Methyltransferase
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Cancer
|
|
PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
|
-
- HY-15682R
-
|
Ro 13-7410 (Standard); Arotinoid acid (Standard); AGN191183 (Standard)
|
Reference Standards
RAR/RXR
Autophagy
Apoptosis
|
Cancer
|
|
TTNPB (Standard) is the analytical standard of TTNPB. This product is intended for research and analytical applications. TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
|
-
- HY-120792
-
|
|
mAChR
|
Others
|
|
DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
|
-
- HY-126230
-
|
|
Endogenous Metabolite
|
Others
|
|
PAT-494 is an ATX inhibitor with significant activity in biochemical and plasma assays. PAT-494 can reduce LPA levels in rat plasma through oral administration. The structure-activity relationship study of PAT-494 shows that its binding mode with ATX is novel and it can effectively occupy the hydrophobic pockets and channels of ATX .
|
-
- HY-11051
-
|
|
Opioid Receptor
|
Inflammation/Immunology
|
|
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
|
-
- HY-151968
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
|
-
- HY-N8295
-
|
Kitasamycin A13
|
Antibiotic
|
Infection
|
|
Leucomycin A13 is a macrolide antibiotic and a component of the leucomycin complex originally isolated from S. kitasatoensis. It is active against B. subtilis, S. aureus, M. luteus, and E. coli with MIC values of 0.16, 0.16, 0.08 and >10 μg/mL, respectively. It binds to ribosomes with an IC50 value of 1.2 μM in a radioligand binding assay.
|
-
- HY-P1376A
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
- HY-23848
-
|
non-8-ynoic acid
|
Bacterial
|
Infection
|
|
8-Nonynoic acid (non-8-ynoic acid) is a fatty acid that belongs to the group of octynoic acids. It exhibits antibacterial activity against gram-positive bacteria by binding to bacterial fatty acids. 8-Nonynoicacid also inhibits growth of gram-negative bacteria by inhibiting the synthesis of fatty acids. It is also capable of inhibiting growth of both aerobic and anaerobic bacteria in biochemical assays.
|
-
- HY-10275
-
|
AR-H067637
|
Thrombin
|
Cardiovascular Disease
|
|
Atecegatran (AR-H067637) is an orally active competitive thrombin inhibitor with a Ki of 2-4 nM. AR-H067637 inhibits platelet activation and aggregation by blocking thrombin binding to fibrin and thrombomodulin. Atecegatran demonstrates significant anticoagulant effects in various plasma coagulation assays, with an IC50 ranging from 93 to 220 nM. Atecegatran can be used in research related to thromboembolic disorders .
|
-
- HY-158385
-
|
|
Biochemical Assay Reagents
|
Others
|
|
5-Azido-PEG4-SS-UTP tristriethylamine is a biochemical assay reagent, which can be used in click chemistry. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity .
|
-
- HY-W806047
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
|
-
- HY-159920
-
|
|
Orphan Nuclear Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PSB-22269 is a GPR17 antagonist with a Ki value of 8.91 nM. PSB-22269 further demonstrated significant inhibitory effects in cAMP and G protein activation assays. Molecular docking studies revealed that the binding site of PSB-22269 contains positively charged arginine residues and a hydrophobic pocket. PSB-22269 provides a strategy to promote remyelination and holds promise for research in the field of multiple sclerosis .
|
-
- HY-126115
-
|
15-epi Latanoprost
|
Prostaglandin Receptor
|
Cardiovascular Disease
Others
|
|
15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
|
-
- HY-175505
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kd of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder .
|
-
- HY-11024
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
ADP receptor-IN-1 (compound 21) is a platelet ADP receptor inhibitor. ADP receptor-IN-1 shows both IC50 values <10 μM at a platelet ADP receptor binding assay and aggregation using a platelet-rich plasma assay .
|
-
- HY-183344
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
IL-1β-IN-4 is a selective IL-1β competitive binder. IL-1β-IN-4 interferes with the interaction between IL-1β and its cognate receptor IL-1R1, with an IC50 of 8.3 μM. IL-1β-IN-4 can be used in studies related to inflammatory and immune diseases .
|
-
- HY-W1123937A
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Biotin-PEG2000-CHO is a biotin-conjugated PEG derivative that can be used to biotinylate biomolecules or other surfaces. Biotin can be easily detected by biotin/streptavidin binding assay and is widely used in molecular targeted detection .
|
-
- HY-W1123937B
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Biotin-PEG3400-CHO is a biotin-conjugated PEG derivative that can be used to biotinylate biomolecules or other surfaces. Biotin can be easily detected by biotin/streptavidin binding assay and is widely used in molecular targeted detection .
|
-
- HY-W1123937
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Biotin-PEG1000-CHO is a biotin-conjugated PEG derivative that can be used to biotinylate biomolecules or other surfaces. Biotin can be easily detected by biotin/streptavidin binding assay and is widely used in molecular targeted detection .
|
-
- HY-P11481
-
|
|
Fluorescent Dye
E1/E2/E3 Enzyme
|
Others
|
|
FITC-Acp-RpYTPEP-NH2 is a potent fluorescent tracer. FITC-Acp-RpYTPEP-NH2 shows a binding affinity (Kd = 0.07 μM) for the Cbl-b SH2 domain. Fluorescence polarization assay based on FITC-Acp-RpYTPEP-NH2 can be for evaluating Cbl-b SH2 domain inhibitors .
|
-
- HY-10858R
-
|
|
Reference Standards
sFRP-1
Wnt
|
Cancer
|
|
WAY 316606 (Standard) is the analytical standard of WAY 316606 (HY-10858). This product is intended for research and analytical applications. WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM .
|
-
- HY-103663R
-
|
|
Reference Standards
Histone Methyltransferase
|
Cancer
|
|
MAK683 (Standard) is the analytical standard of MAK683 (HY-103663). This product is intended for research and analytical applications. MAK683 is an embryonic ectoderm development (EED) inhibitor extracted from patent US20160176882 A1, compound example 2. MAK683 exhibits IC50s of 59, 89, 26 nM in EED Alphascreen binding, LC-MS and ELISA assay .
|
-
- HY-P992342
-
|
|
Tim3
|
Cancer
|
|
DCB-8 is a specific inhibitor targeting human TIM-3. DCB-8 regulates T cell function, enhances cytokine secretion, and inhibits tumor growth in disease animal models. DCB-8 can be used for cancer research .
|
-
- HY-W043574
-
|
|
Bcl-2 Family
Drug Derivative
|
Cancer
|
|
6-Ethyl-7-hydroxy-4-methyl-2H-chromen-2-one (Compound 32), a derivative of Coumarin (HY-N0709), acts as a Mcl-1 inhibitor with a Ki of 5.47 μM and an IC50 of 30.88 μM. 6-Ethyl-7-hydroxy-4-methyl-2H-chromen-2-one is applicable for cancer research .
|
-
- HY-135303
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis . GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-183180
-
|
|
CGRP Receptor
|
Neurological Disease
|
|
CGRP antagonist-8 is a CGRP receptor antagonist with an IC50 of 2.7 nM. CGRP antagonist-8 can be used for the research of migraine .
|
-
- HY-108507R
-
|
|
Reference Standards
Smo
|
Cancer
|
|
MRT-10 (Standard) is the analytical standard of MRT-10 (HY-108507). This product is intended for research and analytical applications. MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer .
|
-
- HY-158685
-
|
|
MDM-2/p53
|
Cancer
|
|
RG7112D is a potent MDM2 inhibitor with IC50s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC50=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels .
|
-
- HY-W142795
-
|
4-sec-BP
|
Androgen Receptor
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
4-sec-Butylphenol (4-sec-BP) is an androgen receptor ligand that binds to the androgen receptor with a pIC50 of 4.07 . 4-sec-Butylphenol is an estrogen receptor agonist. 4-sec-Butylphenol can be found in industrial effluents, in production water of oil and gas platforms, as well as in river water samples .
|
-
- HY-D0014
-
|
|
Environmental Pollutants
Biochemical Assay Reagents
|
Others
|
|
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
|
-
- HY-182272
-
|
|
FAP
|
Cancer
|
|
FAP-IN-9 (compound P12) is a fibroblast activation protein (FAP) inhibitor with an IC50 of 0.38 nM against human FAP. FAP-IN-9 functionally inhibits FAP activity, and its specific binding is verified by in vitro and in vivo blocking assays. FAP-IN-9 forms stable complexes and acts as a tumor-targeting agent. When labeled with 99mTc, FAP-IN-9 serves as a SPECT probe and is applicable to research related to glioblastoma .
|
-
- HY-10569R
-
|
ACT-128800 (Standard)
|
Reference Standards
LPL Receptor
|
Inflammation/Immunology
|
|
Ponesimod (Standard) is the analytical standard of Ponesimod. This product is intended for research and analytical applications. Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
|
-
- HY-122630
-
TH-257
1 Publications Verification
|
LIM Kinase (LIMK)
|
Cancer
|
|
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 .
|
-
- HY-10835R
-
|
|
Reference Standards
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
DG-041 (Standard) is the analytical standard of DG-041 (HY-10835). This product is intended for research and analytical applications. DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier .
|
-
- HY-119366
-
|
|
ROR
|
Inflammation/Immunology
|
|
S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC50>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations .
|
-
- HY-122611R
-
|
|
Reference Standards
Androgen Receptor
Apoptosis
|
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 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 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-D2415
-
|
|
Fluorescent Dye
|
Others
|
|
BODIPY-FL staurosporine (Compound 8a) is a fluorescence probe based on staurosporine, exhibiting high specificity towards tyrosine kinases (TK) and tyrosine kinase-like (TKL) family kinases. BODIPY-FL staurosporine has the potential to develop binding assays for kinases that are not recommended for use with Kinase Tracer 236, such as PIM3, CDC42BPG, MAP2K7, TXK, and SIK3. BODIPY-FL staurosporine can be a powerful tool for analyzing kinase selectivity in kinase drug discovery .
|
-
- HY-10037R
-
|
MK-591 (Standard)
|
Reference Standards
FLAP
Apoptosis
|
Inflammation/Immunology
|
|
Quiflapon (Standard) is the analytical standard of Quiflapon. This product is intended for research and analytical applications. 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 .
|
-
- HY-N1486R
-
|
3-Ketoursolic acid (Standard)
|
Reference Standards
Apoptosis
Endogenous Metabolite
NF-κB
|
Inflammation/Immunology
Cancer
|
|
CSRM617 (Standard) is the analytical standard of CSRM617. This product is intended for research and analytical applications. CSRM617 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 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model
|
-
- HY-114678
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY302148 is a receptor ligand for 5-HT1F. Compared to the Emax of 5-HT, LY302148 behaves as a partial agonist for the 5-HT1F receptor. In the [ 35S]GTPγS binding assay targeting human 5-HT1F receptors, LY302148 exhibits good potency with an EC50 value of 5.23 nM. LY302148 can be used in the research of migraine .
|
-
- HY-122038
-
|
|
MDM-2/p53
|
Cancer
|
|
NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines .
|
-
- HY-W800831
-
|
|
Fluorescent Dye
|
Others
|
|
Tetra-sulfo-Cy7 DBCO is a bright and photostable near-IR probe. The Cy7 DBCO is water-soluble, hydrophilic dye often a reagent of choice for assay where minimal non-specific binding and exceptional brightness is required. The fluorescence of Cy7 DBCO is pH insensitive from pH 4 to pH 10 and produces minimal autofluorescence of biological specimens in this region of the spectrum. Fluorescence of this long-wavelength Cyanine dye is not visible to the human eye but is readily detected by most imaging systems.
|
-
- HY-145899
-
|
|
PKC
|
Cancer
|
|
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 .
|
-
- HY-173275
-
|
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRα D842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRα D842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study .
|
-
- HY-10569S
-
|
ACT-128800-d4
|
Isotope-Labeled Compounds
LPL Receptor
|
Others
|
|
Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
|
-
- HY-123244
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
YC137 is a potent Bcl-2 antagonist with Kis of 1.3 μM and >100 μM for Bcl-2 and Bcl-xL when assayed in Bis-Tris buffer, respectively. YC137 inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2. YC137 selectively induces apoptosis of Bcl-2-dependent cells. YC137 has the potential for breast cancer research .
|
-
- HY-P4863
-
|
|
CGRP Receptor
|
Neurological Disease
Metabolic Disease
|
|
Biotinyl-Amylin (human) is a biotin-labeled derivative of Amylin, amide, human (HY-P1070). Biotinyl-Amylin (human) acts as a competitive agonist for the Calcitonin Receptor (CTR) and for the Amylin receptors (AMY1, AMY2, and AMY3) formed by the association of CTR with RAMP1/2/3. By mimicking endogenous human amylin, Biotinyl-Amylin (human) binds to and activates CTR and AMY receptors, thereby initiating downstream signaling pathways involving cAMP, CREB, and ERK1/2, while retaining high-affinity receptor binding and activation capabilities. Biotinyl-Amylin (human) is primarily utilized in studies investigating the metabolic regulatory mechanisms underlying obesity and diabetes; it is also applicable to pharmacological research, receptor localization studies, and ligand-binding assays related to Amylin receptors in the context of Alzheimer's disease .
|
-
- HY-182355
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
|
-
- HY-181533
-
|
|
Ligands for E3 Ligase
IAP
|
Cancer
|
|
IAP ligand 9 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 9 selectively targets cIAP1-BIR3, XIAP-BIR3, exhibits extremely weak binding affinity for XIAP-BIR2, with a KD of 100 nM for cIAP1-BIR3 and 10 nM for XIAP-BIR2. IAP ligand 9 can be used to synthesize IAP-recruiting protein degraders (IPD), and can calibrate the cell permeability and cellular-level target binding assays of the IPD molecule SNIPER (TEAD)-1 (HY-181607). IAP ligand 9 and its series of degraders can be used in the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway .
|
-
- HY-126115R
-
|
15-epi Latanoprost (Standard)
|
Prostaglandin Receptor
Reference Standards
|
Cardiovascular Disease
Others
|
|
15(S)-Latanoprost (Standard) is the analytical standard of 15(S)-Latanoprost. This product is intended for research and analytical applications. 15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
|
-
- HY-169311
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
|
-
- HY-D2908
-
|
|
Fluorescent Dye
|
Others
|
SYTO9 is a green fluorescent nucleic acid dye (Ex = 485 nm, Em = 498 nm (DNA)/501 nm (RNA)). SYTO9 can penetrate the intact cell membrane of viable bacteria. When the cell membrane is damaged (cell death), its rate of entry into cells increases, and it competes with propidium iodide (PI) (HY-D0815), another membrane-impermeable dye, for nucleic acid binding sites. SYTO9 is widely used in fluorescence microscopy, flow cytometry, and fluorometric assays in microbiology for bacterial counting, viability assessment, and cell imaging .
|
-
- HY-10569S1
-
|
ACT-128800-d7
|
Isotope-Labeled Compounds
|
Others
|
|
Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
|
-
- HY-135985
-
|
|
Fluorescent Dye
|
Cancer
|
|
DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC) .
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-
- HY-183867
-
|
|
Autophagy
|
Others
|
|
ATG5 PPI-IN-6 (Compound 17a) is an inhibitor of ATG5 interactions with other proteins, with an IC50 value of 26.92 μM against ATG5-ATG16L1 and 16.34 μM against ATG5-TECAIR. ATG5 PPI-IN-6 inhibits Autophagy in cells .
|
-
- HY-182702
-
|
|
TREM receptor
Syk
|
Neurological Disease
|
|
As48 is a selective TREM2 agonist with a KD value of 12.48 μM in TRIC binding assay. As48 binds near the TREM2 cleavage region, forms hydrogen bonds with Gly68, reduces conformational flexibility in regions 58-102, restricts protease accessibility to the cleavage site. As48 activates SYK phosphorylation, enhances microglial phagocytosis, and induces downstream calcium signaling in TREM2-expressing cells. As48 inhibits TREM2 ectodomain shedding without affecting ADAM10/17 protease activities. As48 can be used for the research of Alzheimer's disease .
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-
- HY-124346
-
|
|
Stearoyl-CoA Desaturase (SCD)
|
Metabolic Disease
|
|
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 .
|
-
- HY-183838
-
|
|
Autophagy
|
Cancer
|
|
Autophagy-IN-11 is an ATG5-targeting autophage inhibitor. Autophagy-IN-11 disrupts protein-protein interactions between ATG5 and ATG16L1, and between ATG5 and TECAIR. Autophagy-IN-11 can be used for cancer research .
|
-
- HY-17378
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
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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-
- HY-179653
-
|
|
CX3CR1
|
Cardiovascular Disease
|
|
CX3CR1-IN-1 (Compound 24) is a CX3CR1 inhibitor with an IC50 of 9 nM. CX3CR1-IN-1 can be used for the study of cardiovascular diseases .
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-
- HY-133031A
-
|
|
Histone Methyltransferase
|
Others
|
|
CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
|
-
- HY-178166
-
|
|
Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
ETI41 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.63 μM) and TLR9 (IC50 = 0.16 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI41 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI41 suppresses the expression of inflammation-associated genes and effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI41 can be used for autoimmune and inflammatory diseases research .
|
-
- HY-P11306
-
|
|
Proteasome
NF-κB
|
Inflammation/Immunology
|
|
Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .
|
-
- HY-178169
-
|
|
Toll-like Receptor (TLR)
p38 MAPK
TNF Receptor
ERK
JNK
NF-κB
Interleukin Related
|
Inflammation/Immunology
|
|
ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research .
|
-
- HY-182372
-
|
|
Epoxide Hydrolase
|
Neurological Disease
|
|
SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
|
-
- HY-W727480
-
|
|
Insecticide
|
Infection
|
|
Tetrachlorantraniliprole is an anthranilic diamide insecticide that shows no significant affinity to the key odorant-binding proteins (DhelOBP4/DhelOBP21) of Dastarcus helophoroides .
|
-
- HY-W015050
-
|
1-Aminoanthracene
|
GABA Receptor
Chloride Channel
Fluorescent Dye
|
Neurological Disease
|
|
1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with Kd = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC50 value of 16 μM .
|
-
- HY-182921
-
|
|
GPR84
Enterovirus
|
Inflammation/Immunology
|
|
GPR84 antagonist 11 is a highly selective GPR84 antagonist, with a human pA2 of 8.41 and a pKi of 8.16. GPR84 antagonist 11 competitively inhibits the binding of agonists to the orthosteric site of GPR84 and has improved druglike properties, though its metabolic stability still requires optimization. GPR84 antagonist 11 can be used in the research of autoimmune diseases and fibrotic diseases .
|
-
- HY-134483
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .
|
-
- HY-N8501
-
|
|
Bacterial
|
Infection
|
|
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities. It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s=3.94, 0.6, 2.21, 4.55, and 2.21 μg/mL, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50=5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg/mL) induces apoptosis in HL-60 cells. It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.
|
-
- HY-W013403
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-183293
-
|
|
E1/E2/E3 Enzyme
|
Others
|
|
Cbl-b-IN-32 is a Cbl-b inhibitor with an IC50 of 6.83 μM. Cbl-b-IN-32 binds to the TKB-LH interface, stabilizes the inactive conformation of Cbl-b, engages Tyr363 via hydrogen bonds and water bridges, and forms hydrogen bonds with Phe261 and Phe263 .
|
-
- HY-W003486
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
Cancer
|
|
5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a Ki of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia .
|
-
![5,7-Dichloropyrazolo[1,5-a]pyrimidine](//file.medchemexpress.com/product_pic/hy-w003486.gif)
- HY-103247
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant - .
|
-
- HY-146248
-
|
|
SARS-CoV
Poly(ADP-ribose) Glycohydrolase (PARG)
Protease Activated Receptor (PAR)
|
Infection
|
|
TFMU-ADPr is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr is also applicable to COVID-19-related research .
|
-
- HY-146248B
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
SARS-CoV
Protease Activated Receptor (PAR)
|
Metabolic Disease
|
|
TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research .
|
-
- HY-146248A
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
SARS-CoV
Protease Activated Receptor (PAR)
|
Others
|
|
TFMU-ADPr triethylamine is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr triethylamine can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr triethylamine binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr triethylamine can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr triethylamine is also applicable to COVID-19-related research .
|
-
- HY-10898R
-
|
|
Reference Standards
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-674042 (Standard) is the analytical standard of SB-674042 (HY-10898). This product is intended for research and analytical applications. SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively .
|
-
- HY-10898
-
-
- HY-181824
-
|
|
Bacterial
|
Infection
|
|
Cholera toxin-IN-1 is a potent competitive inhibitor of cholera toxin B subunit (CTB) with an IC50 value of 11.78 μM. Cholera toxin-IN-1 forms stable hydrogen bonds and hydrophobic interactions. Cholera toxin-IN-1 competitively blocks the binding of CTB to GM1 ganglioside. Cholera toxin-IN-1 can be used for the research of cholera .
|
-
- HY-W013403S
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-116161
-
|
|
Drug Intermediate
|
Cardiovascular Disease
Others
|
|
15(R)-17-phenyl trinor Prostaglandin F2α isopropyl ester (15(R)-17-phenyl trinor PGF2α isopropyl ester) is the latanoprost-related isomer containing both a double bond at 13,14 and an inverted (β) hydroxyl group at C-15. Similar to 15(S)-latanoprost, 15(R)-17-phenyl trinor PGF2α isopropyl ester is a potential impurity in most commercial preparations of the latanoprost bulk drug product. The IC50 values for the free acid forms of 15(S)-17-phenyl trinor PGF2α and 15(R)-17-phenyl trinor PGF2α were determined to be 0.71 nM and 30 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle.1 A 3 μg dose of 15(R)-17-phenyl trinor PGF2α caused a 1.9 mmHg reduction of IOP in normotensive cynomolgus monkeys.
|
-
- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
|
-
- HY-137055
-
|
|
Others
|
Others
|
|
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function.
|
-
- HY-118156
-
|
|
Others
|
Others
|
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
-
-
HY-L0115V
-
|
|
10,091 compounds
|
|
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.
Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D2908
-
|
|
Fluorescent Dye
|
SYTO9 is a green fluorescent nucleic acid dye (Ex = 485 nm, Em = 498 nm (DNA)/501 nm (RNA)). SYTO9 can penetrate the intact cell membrane of viable bacteria. When the cell membrane is damaged (cell death), its rate of entry into cells increases, and it competes with propidium iodide (PI) (HY-D0815), another membrane-impermeable dye, for nucleic acid binding sites. SYTO9 is widely used in fluorescence microscopy, flow cytometry, and fluorometric assays in microbiology for bacterial counting, viability assessment, and cell imaging .
|
-
- HY-D1314
-
|
6-FAM azide
|
Fluorescent Dye
|
|
FAM azide, 6-isomer (6-FAM azide) is a 6-carboxyfluorescein derivative with an azide functional group and coupling partner in copper-catalyzed azide-alkyne cycloaddition. FAM azide, 6-isomer participates in synthesis of fluorescently tagged disparlure enantiomers for pheromone-binding protein binding assays. FAM azide, 6-isomer is widely used for labeling oligonucleotides (Ex/Em = 493/517 nm) .
|
-
- HY-D0014
-
|
|
Fluorescent Dye
|
|
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
|
-
- HY-D2415
-
|
|
Fluorescent Dye
|
|
BODIPY-FL staurosporine (Compound 8a) is a fluorescence probe based on staurosporine, exhibiting high specificity towards tyrosine kinases (TK) and tyrosine kinase-like (TKL) family kinases. BODIPY-FL staurosporine has the potential to develop binding assays for kinases that are not recommended for use with Kinase Tracer 236, such as PIM3, CDC42BPG, MAP2K7, TXK, and SIK3. BODIPY-FL staurosporine can be a powerful tool for analyzing kinase selectivity in kinase drug discovery .
|
-
- HY-146248
-
|
|
Fluorescent Dye
|
|
TFMU-ADPr is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr is also applicable to COVID-19-related research .
|
-
- HY-D1190
-
|
|
Fluorescent Dye
|
|
DC271 is a RAR agonist and synthetic retinoid that binds to the retinoid-binding site of cellular retinoic acid-binding protein II (CRBP-II). DC271 exhibits solvatochromic fluorescence properties: it produces intense blue-shifted emission in nonpolar environments and weak red-shifted emission in polar environments, and its severe fluorescence quenching in aqueous solutions can be reversed by embedding in the hydrophobic retinoid-binding protein pocket. DC271 enables direct detection of the binding between unlabeled compounds and related retinoid-binding proteins via fluorescence competition assays (Ex/Em = 355 nm/460 nm) .
|
-
- HY-W800831
-
|
|
Fluorescent Dye
|
|
Tetra-sulfo-Cy7 DBCO is a bright and photostable near-IR probe. The Cy7 DBCO is water-soluble, hydrophilic dye often a reagent of choice for assay where minimal non-specific binding and exceptional brightness is required. The fluorescence of Cy7 DBCO is pH insensitive from pH 4 to pH 10 and produces minimal autofluorescence of biological specimens in this region of the spectrum. Fluorescence of this long-wavelength Cyanine dye is not visible to the human eye but is readily detected by most imaging systems.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0014
-
|
|
Biochemical Assay Reagents
|
|
Brilliant Blue G-250 is a dye commonly used for the visualization of proteins separated by SDS-PAGE, offering a simple staining procedure and high quantitation. In the Bradford protein assay, protein concentrations are determined by the absorbance at 595 nm due to the binding of Brilliant Blue G-250 to proteins. Brilliant Blue G-250 is a safe highly selective P2×7R antagonist with promising consequent inactivation of NLRP3 inflammasome .
|
-
- HY-174962A
-
|
|
Biochemical Assay Reagents
|
|
mPEG2000-Biotin is a biotin-conjugated PEG derivative used for biotinylation of biomolecules or other surfaces. Biotin can be detected by biotin/streptavidin binding assays and is widely used for molecular target detection .
|
-
- HY-128466
-
|
|
Biochemical Assay Reagents
|
|
N-Biotinyl-L-cysteine is a biotinylated biochemical assay reagent, which is used to detect avidin and biotin through a competitive binding reaction .
|
-
- HY-174962B
-
|
|
Biochemical Assay Reagents
|
|
mPEG5000-Biotin is a biotin-conjugated PEG derivative used for biotinylation of biomolecules or other surfaces. Biotin can be detected by biotin/streptavidin binding assays and is widely used for molecular target detection .
|
-
- HY-174962
-
|
|
Biochemical Assay Reagents
|
|
mPEG1000-Biotin is a biotin-conjugated PEG derivative used for biotinylation of biomolecules or other surfaces. Biotin can be detected by biotin/streptavidin binding assays and is widely used for molecular target detection .
|
-
- HY-W1123937A
-
|
|
Biochemical Assay Reagents
|
|
Biotin-PEG2000-CHO is a biotin-conjugated PEG derivative that can be used to biotinylate biomolecules or other surfaces. Biotin can be easily detected by biotin/streptavidin binding assay and is widely used in molecular targeted detection .
|
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- HY-W1123937B
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Biochemical Assay Reagents
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Biotin-PEG3400-CHO is a biotin-conjugated PEG derivative that can be used to biotinylate biomolecules or other surfaces. Biotin can be easily detected by biotin/streptavidin binding assay and is widely used in molecular targeted detection .
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- HY-W1123937
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Biochemical Assay Reagents
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Biotin-PEG1000-CHO is a biotin-conjugated PEG derivative that can be used to biotinylate biomolecules or other surfaces. Biotin can be easily detected by biotin/streptavidin binding assay and is widely used in molecular targeted detection .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0179
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- HY-P5908F
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Peptides
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Others
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FAM-DEALA-Hyp-YIPD is a fluorescent HIF-1α peptide, with the Kd of 180-560 nM. FAM-DEALA-Hyp-YIPD can be used to assess VHL binding in Fluorescence Polarization (FP) displacement assay, and evaluate the effect of VHL binding on degradation activity .
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- HY-P1096
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Cholecystokinin Receptor
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Metabolic Disease
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A71623, a CCK-4-based peptide, is a potent and highly selective CCK-A full agonist. The IC50s for A-71623 are 3.7 nM in guinea pig pancreas (CCK-A) and 4500 nM in cerebral cortex (CCK-B) in radioligand binding assays, respectively .
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- HY-P11306
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Proteasome
NF-κB
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Inflammation/Immunology
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Biotin-(Oaa)3-epoxomicin is a biotin-labeled form of Epoxomicin (HY-13821), prepared by conjugating Epoxomicin with biotin via three hydrophilic oxaacetyl amino acid (Oaa) linkers. Biotin-(Oaa)3-epoxomicin is primarily used in proteomic studies for the capture, identification and target validation of proteasome complexes, to determine the intracellular targets of epoxomicin. Epoxomicin acts as a proteasome inhibitor and NF-κB inhibitor, which effectively blocks inflammatory responses in mouse ear edema assays. It inhibits proteasome activity via covalent binding to catalytic subunits including LMP7, X, MECL1 and Z, with the strongest inhibitory effect on chymotrypsin-like activity, and does not interfere with non-proteasomal proteases such as trypsin and papain .
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- HY-P4581
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Suc-ALPF-pNA
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FKBP
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Others
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Suc-Ala-Leu-Pro-Phe-pNA (Suc-ALPF-pNA) is a synthetic polypeptide substrate that targets FK506-binding protein (FKBP). Suc-Ala-Leu-Pro-Phe-pNA can be used to determine peptidyl-prolyl cis-trans isomerase activity via the chymotrypsin-coupled assay. Suc-Ala-Leu-Pro-Phe-pNA serves as a substrate for human FK506-binding protein hFKBP-12 in the chymotrypsin-FKBP coupled PPIase assay. Suc-Ala-Leu-Pro-Phe-pNA is applicable for the detection and research of PPIase activity .
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- HY-P5367
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PMDM6-F
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Fluorescent Dye
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Others
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5-FAM-PMDM6 (PMDM6-F) is a biological active peptide. (PMDM6-F is a fluorescent-labeled probe for MDM2-binding assay.)
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- HY-P4863
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CGRP Receptor
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Neurological Disease
Metabolic Disease
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Biotinyl-Amylin (human) is a biotin-labeled derivative of Amylin, amide, human (HY-P1070). Biotinyl-Amylin (human) acts as a competitive agonist for the Calcitonin Receptor (CTR) and for the Amylin receptors (AMY1, AMY2, and AMY3) formed by the association of CTR with RAMP1/2/3. By mimicking endogenous human amylin, Biotinyl-Amylin (human) binds to and activates CTR and AMY receptors, thereby initiating downstream signaling pathways involving cAMP, CREB, and ERK1/2, while retaining high-affinity receptor binding and activation capabilities. Biotinyl-Amylin (human) is primarily utilized in studies investigating the metabolic regulatory mechanisms underlying obesity and diabetes; it is also applicable to pharmacological research, receptor localization studies, and ligand-binding assays related to Amylin receptors in the context of Alzheimer's disease .
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- HY-P0179A
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- HY-P1376A
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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- HY-P11481
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Fluorescent Dye
E1/E2/E3 Enzyme
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Others
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FITC-Acp-RpYTPEP-NH2 is a potent fluorescent tracer. FITC-Acp-RpYTPEP-NH2 shows a binding affinity (Kd = 0.07 μM) for the Cbl-b SH2 domain. Fluorescence polarization assay based on FITC-Acp-RpYTPEP-NH2 can be for evaluating Cbl-b SH2 domain inhibitors .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P9949
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Sch 55700; CDP-835; JES1-39D10
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Interleukin Related
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Inflammation/Immunology
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Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
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(5)
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- HY-P992342
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Tim3
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Cancer
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DCB-8 is a specific inhibitor targeting human TIM-3. DCB-8 regulates T cell function, enhances cytokine secretion, and inhibits tumor growth in disease animal models. DCB-8 can be used for cancer research .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-W008226R
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- HY-N1486R
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- HY-N8501
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Structural Classification
Natural Products
Microorganisms
Source Classification
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Bacterial
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Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities. It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s=3.94, 0.6, 2.21, 4.55, and 2.21 μg/mL, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50=5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg/mL) induces apoptosis in HL-60 cells. It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B1486AS
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Oxprenolol-d7 is the deuterium labeled Oxprenolol. Oxprenolol (Ba 39089 free base) 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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- HY-B1486S
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Oxprenolol-d7 (hydrochloride) is the deuterium labeled Oxprenolol hydrochloride. 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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- HY-16582AS
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Sonidegib-d4 is a isotope of Sonidegib. Sonidegib is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively .
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- HY-10569S
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Ponesimod-d4 (ACT-128800-d4) is the deuterium labeled Ponesimod (HY-10569) . Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation .
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- HY-10569S1
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Ponesimod-d7 (ACT-128800-d7) is the deuterium-labeled Ponesimod (HY-10569). Ponesimod-d7 (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod-d7 activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod-d7 can protect against lymphocyte-mediated tissue inflammation .
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- HY-W013403S
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2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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| Cat. No. |
Product Name |
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Classification |
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- HY-D1314
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6-FAM azide
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Labeling and Fluorescence Imaging
Azide
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FAM azide, 6-isomer (6-FAM azide) is a 6-carboxyfluorescein derivative with an azide functional group and coupling partner in copper-catalyzed azide-alkyne cycloaddition. FAM azide, 6-isomer participates in synthesis of fluorescently tagged disparlure enantiomers for pheromone-binding protein binding assays. FAM azide, 6-isomer is widely used for labeling oligonucleotides (Ex/Em = 493/517 nm) .
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- HY-158385
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Azide
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5-Azido-PEG4-SS-UTP tristriethylamine is a biochemical assay reagent, which can be used in click chemistry. Click chemistry has great potential for use in binding between nucleic acids, lipids, proteins, and other molecules, and has been used in many research fields because of its beneficial characteristics, including high yield, high specificity, and simplicity .
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