Search Result
Results for "
apparent
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-15772
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Osimertinib
Maximum Cited Publications
185 Publications Verification
AZD-9291; Mereletinib
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EGFR
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Cancer
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Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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- HY-D0861
-
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Biochemical Assay Reagents
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Inflammation/Immunology
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EGTA is a cell-impermeant specific calcium ion chelator. EGTA has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca 2+ over Mg 2+ (Mg 2+ Kd 1-10 mM). EGTA significantly inhibits the substrate adherence capacity of inflammatory macrophages .
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- HY-15772A
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AZD-9291 mesylate; Mereletinib mesylate
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EGFR
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Cancer
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Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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- HY-139361
-
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PIN1-3
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PIN1
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Cancer
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Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
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- HY-130463
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PG(16:0/18:1); 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol)
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Liposome
Biochemical Assay Reagents
Neurotensin Receptor
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Neurological Disease
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POPG sodium salt is a negatively charged phospholipid. POPG sodium salt affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG sodium salt increases the apparent affinity of Gαq and Gβ1γ1 for activated NTS1. POPG sodium salt can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research .
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- HY-123943
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STING
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Cancer
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STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function .
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- HY-15772R
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AZD-9291 (Standard); Mereletinib (Standard)
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Reference Standards
EGFR
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Cancer
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Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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- HY-D1583
-
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DBCO-Cy5 hexafluorophosphate; Cyanine5 dibenzocyclooctyne hexafluorophosphate
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Fluorescent Dye
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Others
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Cyanine5 DBCO (DBCO-Cy5) hexafluorophosphate is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO hexafluorophosphate has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO hexafluorophosphate can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
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- HY-112472
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Sodium Channel
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Metabolic Disease
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S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC50 for S3969 activation of hENaC is 1.2 μm .
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- HY-103017A
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IRAK
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Infection
Inflammation/Immunology
Cancer
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JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice . JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM .
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- HY-P990534
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K1-70
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TSH Receptor
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Endocrinology
Cancer
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Anti-TSHR Antibody (K1-70) is an anti-TSHR monoclonal antibody. Anti-TSHR Antibody (K1-70) incorporates a single-chain variable fragment into a chimeric antigen receptor to redirect T cells to TSHR-expressing cells. Anti-TSHR Antibody (K1-70) shows antitumor activity with no apparent toxicity. Anti-TSHR Antibody (K1-70) can be used for the research of differentiated thyroid cancer (DTC) .
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- HY-15772S1
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AZD-9291-13C,d3; Mereletinib-13C,d3
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EGFR
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Cancer
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Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
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- HY-19350
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BML-210
2 Publications Verification
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HDAC
Apoptosis
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Cancer
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BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC50 of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice .
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- HY-172236
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BNC210; IW-2143
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nAChR
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Neurological Disease
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Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders .
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- HY-15294
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- HY-W008344
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Nucleoside Antimetabolite/Analog
Apoptosis
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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2-Chloroadenosine is an adenosine analog, a transporter permeabilizer of nucleoside transporters, and a competitive uridine influx inhibitor (apparent Ki=33 μM). 2-Chloroadenosine binds to nitrobenzylthioinosine with high affinity (apparent Ki=0.18 mM). 2-Chloroadenosine promotes Apoptosis and increases cerebral blood flow. 2-Chloroadenosine has anticonvulsant properties. 2-Chloroadenosine is used to study infection, inflammatory diseases, cancer, blood-related diseases, lung injury, epilepsy, and kidney disease .
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- HY-D0861A
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Biochemical Assay Reagents
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Inflammation/Immunology
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EGTA tetrasodium is a cell-impermeant specific calcium ion chelator. EGTA tetrasodium has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca 2+ over Mg 2+ (Mg 2+ Kd 1-10 mM). EGTA tetrasodium significantly inhibits the substrate adherence capacity of inflammatory macrophages .
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- HY-U00443
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5-HT Receptor
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Neurological Disease
Cancer
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SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease .
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- HY-153419
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Biochemical Assay Reagents
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Others
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BTTES is a tris(triazolylmethyl)amine-based ligand for Cu(I) without apparent toxicity. BTTES IMPROVES the cycloaddition reaction rapidly in living systems .
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- HY-101226
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mGluR
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Neurological Disease
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MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
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- HY-B1626A
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BC-48
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Cholinesterase (ChE)
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Neurological Disease
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Demecarium Bromide (BC-48) is a potent cholinesterase inhibitor, with an apparent affinity (Kiapp) of 0.15 μM . Demecarium Bromide (BC-48) is used as a glaucoma agent .
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- HY-125776
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BAS 490 F
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Environmental Pollutants
Mitochondrial Metabolism
Fungal
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Infection
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Kresoxim-methyl (BAS 490 F), a Strobilurin-based fungicide, inhibits the respiration at the complex III (cytochrome bc1 complex). Kresoxim-methyl binds to complex III from yeast with an apparent Kd of 0.07 μM proving a high affinity for this enzyme .
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- HY-14567
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FUB-359
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Histamine Receptor
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Neurological Disease
Endocrinology
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Ciproxifan (FUB 359) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan displays low apparent affinity at other receptor subtypes. Ciproxifan can be used for the research of aging disorders and Alzheimer's disease .
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- HY-106008
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BAL27862
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Microtubule/Tubulin
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Cancer
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Avanbulin (BAL27862) is a potent, Colchicine site-binding, tubulin assembly inhibitor. Avanbulin inhibits tubulin assembly at 37 °C with an IC50 of 1.4 μM. Avanbulin binds to tubulin with an apparent Kd value of 244 nM. Avanbulin can be used for the research of cancer and cell division .
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- HY-15772S
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AZD-9291-d6; Mereletinib-d6
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EGFR
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Cancer
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Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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- HY-P1411
-
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PcTx1; Psalmopoeus cambridgei toxin-1
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Sodium Channel
Apoptosis
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Neurological Disease
Cancer
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Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease .
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- HY-120423
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Cannabinoid Receptor
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Neurological Disease
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AM6538 is a long-acting, high affinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability . AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-159190
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MAPKAPK2 (MK2)
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Cancer
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HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
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- HY-108643
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MAPKAPK2 (MK2)
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Cancer
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CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Ki app) of 330 nM .
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- HY-103222
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3',4'-Dimethoxy-αNF
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Aryl Hydrocarbon Receptor
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Inflammation/Immunology
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DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent .
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- HY-15289
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FUB 359 maleate
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Histamine Receptor
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Neurological Disease
Endocrinology
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Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease .
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- HY-W019901B
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Gypsum ustum (97%)
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Environmental Pollutants
Biochemical Assay Reagents
RUNX
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Metabolic Disease
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Anhydrous calcium sulfate (97%) serves as an oil-based drilling fluid additive and an osteogenic material. Anhydrous calcium sulfate (97%) increases the plastic viscosity, yield point, apparent viscosity and gel strength of oil-based drilling fluids. Anhydrous calcium sulfate (97%) upregulates the expression of bone-related genes FOSL1, RUNX2 and SPP1. Anhydrous calcium sulfate (97%) significantly affects the behavior of dental pulp stem cells, enhancing their proliferation, differentiation and matrix deposition .
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- HY-171177
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Phosphatase
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Neurological Disease
Cancer
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P5SA-2 is a selective allosteric activator of PPP5C. P5SA-2 exerts its effects by modulating the phosphatase domain of PPP5C and can increase PPP5C activity by 3.2-fold at 100 μM with an apparent affinity constant of 7.8 μM. P5SA-2 can be used in cancer and Alzheimer's disease research .
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- HY-110334
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Fluorescent Dye
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Others
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FFN 206 dihydrochloride, a fluorescent probe, is used as an excellent Vesicular Monoamine Transporter 2 (VMAT2) substrate with an apparent Km of 1.16 μM. FFN 206 dihydrochloride is capable of detecting VMAT2 activity in intact cells using fluorescence microscopy, with subcellular localization to VMAT2-expressing acidic compartments without apparent labeling of other organelles .
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- HY-N8531
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Drug Derivative
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Others
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4α-Methylcholesterol is a Cholesterol derivative. 4α-Methylcholesterol can oxidize 3-hydroxy steroid, with the apparent Km of 12.6 μM .
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- HY-111173
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Dipeptidyl Peptidase
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Others
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Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
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- HY-P2355
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BOC2; Boc-Phe-dLeu-Phe-dLeu-Phe
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Formyl Peptide Receptor (FPR)
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Inflammation/Immunology
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BOC-FlFlF (Boc-Phe-dLeu-Phe-dLeu-Phe) is a selective FPR1 antagonist. Boc-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. Boc-FlFlF can be used for the study of inflammation .
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- HY-P1105
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Chloride Channel
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Neurological Disease
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GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
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- HY-100743
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2-Amino-4-phosphonobutyric acid
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mGluR
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Neurological Disease
Metabolic Disease
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DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system .
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- HY-103123
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5-HT Receptor
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Neurological Disease
Cancer
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SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases .
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- HY-144354S
-
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Isotope-Labeled Compounds
ASCT
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Cancer
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S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2 .
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- HY-P5114A
-
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Calcium Channel
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Others
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Maurocalcine TFA is an agonist of ryanodine receptor (RyR) channel types 1, 2 and 3 with cellular permeability. Maurocalcine TFA induces [ 3H]ryanodine binding on RyR1 with an EC50 value of 2558 nM. Maurocalcine TFA exhibits a apparent affinity of 14 nM for RyR2. Maurocalcine TFA can be applied to in vivo cell tracking or other cell imaging techniques .
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- HY-150759
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HIV
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Infection
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HIV-1 inhibitor-45 is a potent HIV-1 RNase H inhibitor with an IC50 value of 0.067 μM. HIV-1 inhibitor-45 shows an antiviral activity. HIV-1 inhibitor-45 shows poor cell permeability (with an apparent permeability coefficient (Papp) lower than 0.48 × 10 −6 cm/s) .
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- HY-15772AR
-
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AZD-9291 mesylate (Standard); Mereletinib mesylate (Standard)
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Reference Standards
EGFR
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Cancer
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Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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- HY-P1411A
-
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PcTx1 TFA; Psalmopoeus cambridgei toxin-1 TFA
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Sodium Channel
Apoptosis
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Neurological Disease
Cancer
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Psalmotoxin 1 (PcTx1) TFA is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 TFA is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 TFA can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 TFA can be used in the research of cancers, or neurological disease .
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- HY-D2907
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DBCO-Cy5; Cyanine5 dibenzocyclooctyne
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Fluorescent Dye
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Others
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Cyanine5 DBCO (DBCO-Cy5) is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
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- HY-108525
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RAR/RXR
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Cancer
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Fluorobexarotene (compound 20) is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12 nM and an EC50 value of 43 nM for RXRα receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene .
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- HY-114150
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PAI-1
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Others
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D-Val-Leu-Arg-pNA is a glandular kininoreleasing enzyme substrate that also acts as a substrate for tissue-type plasminogen activator (t-PA) with no apparent affinity for fibrin .
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- HY-161181
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Biochemical Assay Reagents
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Others
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BTTES-acid is an analog of BTTES. BTTES is a tris(triazolylmethyl)amine-based ligand for Cu(I) without apparent toxicity. BTTES improves the cycloaddition reaction rapidly in living systems .
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- HY-144308
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Mps1
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Others
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RMS-07 is a covalent Monopolar Spindle Kinase 1 (MPS1/TTK) inhibitor, with an apparent IC50 of 13.1 nM. RMS-07 targets a poorly conserved cysteine in the kinase's hinge region .
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- HY-108657
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P2Y Receptor
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Neurological Disease
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MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
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- HY-109014
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CMX-157
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HIV
HBV
Nucleoside Antimetabolite/Analog
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Infection
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Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
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- HY-107604
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UBP 302
1 Publications Verification
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iGluR
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Neurological Disease
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UBP 302 is a potent and selective GLUK5-subunit containing kainate receptor antagonist (apparent Kd=402 nM), and displays very little affinity on GluK2 (GluR6) kainate receptors. Anxiolytic effects .
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- HY-14567A
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FUB-359 hydrochloride
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Histamine Receptor
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Neurological Disease
Endocrinology
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Ciproxifan (FUB 359) hydrochloride is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan hydrochloride displays low apparent affinity at other receptor subtypes. Ciproxifan hydrochloride can be used for the research of aging disorders and Alzheimer's disease .
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- HY-176089
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ADP-ribose phosphate sodium; P-ADP-Rib sodium
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HMG-CoA Reductase (HMGCR)
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Others
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Adenosine-5'-O-diphosphoribose phosphate sodium is a structural analog of NADPH (HY-113324). Adenosine-5'-O-diphosphoribose phosphate sodium is an HMG-CoA reductase inhibitor. Adenosine-5'-O-diphosphoribose phosphate sodium inhibits microsomal HMG-CoA reductase with an apparent Ki value of 550 μM at low thiol concentrations .
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- HY-175017
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Survivin
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Cancer
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Survivin-IN-2 is a survivin inhibitor. Survivin-IN-2 shows cytotoxicity in cells with IC50s of 0.53 μM (C4-2 cells) and 1.06 μM (PC-3 cells). Survivin-IN-2 effectively suppresses xenograft tumor growth without apparent toxicity and eliminates survivin in the tumors. Survivin-IN-2 can be used for the study of prostate cancer .
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- HY-174293
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Drug Derivative
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Cancer
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Osimertinib dimer is a dimer of Osimertinib (HY-15772). Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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- HY-171956
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Proteasome
Parasite
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Infection
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Carmaphycin-17 (CP-17) is a selective 20S proteasome inhibitor with an EC50 of 217 ?nM. Carmaphycin-17 has potent antimicrobial activity against Trichomonas vaginalis. Carmaphycin-17 overcomes Metronidazole (HY-B0318) resistance and significantly reduces parasite burden upon topical treatment without any apparent adverse effects in vaginal trichomonad infection mice model. Carmaphycin-17 can be used for sexually transmitted disease like trichomoniasis research .
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- HY-DY1068
-
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Fluorescent Dye
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Others
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Cyanine5 DBCO (DBCO-Cy5) hexafluorophosphate (solution) is a low-toxicity azide reactive probe (NIR fluorescent dye) , for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO hexafluorophosphate has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO hexafluorophosphate can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
Solvent and concentration: DMSO: 10 mM
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-
- HY-147807
-
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|
HIV
Cytochrome P450
|
Infection
|
|
HIV-1 inhibitor-40 (Compound 4ab) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an EC50 of 1.9 nM. HIV-1 inhibitor-40 displays weak CYP sensitivity with IC50 values of 5.16 μM and 4.51 μM against CYP2C9 and CYP2C19, respectively. HIV-1 inhibitor-40 has no apparent in vivo acute toxicity .
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-
- HY-119211
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-
- HY-D1417
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|
|
Fluorescent Dye
|
Others
|
|
P-BP-SFAC is a fluorescence molecule. P-BP-SFAC exhibits an apparent absorption band with a peak at about 377 nm, indicative of a stronger ICT effect .
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-
- HY-139045
-
-
- HY-W713312
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
2,6-DMA hydrochloride is classified as an amphetamine. 2,6-DMA hydrochloride is a serotonin 5-HT2 receptor agonist with an apparent pA2 value of 5.09.
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-
- HY-164484
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|
|
Raf
|
Cancer
|
|
IHMT-RAF-128, a highly potent pan-RAF inhibitor. IHMT-RAF-128 shows potent antitumor efficacy in xenograft mouse tumor models without causing any apparent toxicities .
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-
- HY-N10239
-
|
|
Others
|
Metabolic Disease
|
|
Aquastatin A is an inhibitor of mammalian adenosine triphosphatases. Aquastatin A is isolated from a fungus identified as Fusarium aquaeductuum. Aquastatin A inhibits Na+/K(+)-ATPase with an IC50 value of 7.1 μM, and H+/K(+)-ATPase with an apparent IC50 value of 6.2 μM .
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-
- HY-123189
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|
Dopamine Receptor
|
Neurological Disease
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|
LY 171859 is a D2 receptor agonist with significant reductase activity. LY 171859 exhibits enzymatic activity in the cytoplasm of liver, lung, and kidney, and also contains significant reductase activity in rat and human blood. LY 171859 has higher hepatic reductase activity in guinea pigs, followed by hamsters, rabbits, rats, and mice. The substrate of LY 171859 shows an apparent Km of 5.6 μM. The reduction reaction of LY 171859 is NADPH-dependent with an apparent Km of 14.8 μM. Only the A-side hydrogen of NADPH is incorporated in the reduction product of LY 171859. The reaction of LY 171859 is inhibited by cyanide and thiol reagents, and phenobarbital does not induce its activity in rats .
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-
- HY-115755
-
|
6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5'-triphosphate; 6-Thio-ITP
|
DNA/RNA Synthesis
|
Cancer
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|
Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I Ki: 40.9 μM; RNA polymerase II Ki: 38.0 μM) .
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-
- HY-P2355A
-
|
BOC2 TFA; Boc-Phe-dLeu-Phe-dLeu-Phe TFA
|
Formyl Peptide Receptor (FPR)
|
Inflammation/Immunology
|
|
BOC-FlFlF (TFA) (Boc-Phe-dLeu-Phe-dLeu-Phe (TFA)) is a selective FPR1 antagonist. BOC-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. BOC-FlFlF can be used for the study of inflammation .
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-
- HY-136453A
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|
|
Mucin
Drug Isomer
|
Cancer
|
|
CR-1-30-B is an inactive enantiomer of CR-1-31-B. CR-1-30-B, as a control, is inactive against eIF4A and has no apparent effect on the induction of MUC1-C translation .
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-
- HY-146407
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|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity .
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-
- HY-B1626AR
-
|
BC-48 (Standard)
|
Reference Standards
Cholinesterase (ChE)
|
Neurological Disease
|
|
Demecarium Bromide (Standard) is the analytical standard of Demecarium Bromide. This product is intended for research and analytical applications. Demecarium Bromide (BC-48) is a potent cholinesterase inhibitor, with an apparent affinity (Kiapp) of 0.15 μM . Demecarium Bromide (BC-48) is used as a glaucoma agent .
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-
- HY-P10823
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|
|
Amyloid-β
|
Neurological Disease
|
|
RI-OR2, a retro-inverso peptide, is an amyloid-β (Aβ) oligomerization inhibitor. RI-OR2 binds to immobilized β-Amyloid (1-42) (HY-P1363A) monomers and fibrils, with an apparent Kd of 9-12 μM, and also acted as an inhibitor of Aβ(1-42) fibril extension .
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-
- HY-125776R
-
|
BAS 490 F (Standard)
|
Reference Standards
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Kresoxim-methyl (Standard) is the analytical standard of Kresoxim-methyl. This product is intended for research and analytical applications. Kresoxim-methyl (BAS 490 F), a Strobilurin-based fungicide, inhibits the respiration at the complex III (cytochrome bc1 complex). Kresoxim-methyl binds to complex III from yeast with an apparent Kd of 0.07 μM proving a high affinity for this enzyme .
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-
- HY-P5114
-
|
|
Calcium Channel
|
Others
|
|
Maurocalcine is an agonist of ryanodine receptor (RyR) channel types 1, 2 and 3 with cellular permeability. Maurocalcine induces [ 3H]ryanodine binding on RyR1 with an EC50 value of 2558 nM. Maurocalcine exhibits a apparent affinity of 14 nM for RyR2. Maurocalcine can be applied to in vivo cell tracking or other cell imaging techniques .
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-
- HY-111125
-
|
|
Parasite
Reactive Oxygen Species (ROS)
Apoptosis
|
Infection
Cancer
|
|
AMRI-59 is a potent inhibitor of PrxI used for parasitic infections. AMRI-59 can increase cellular ROS, leading to activation of signaling pathways mediated by mitochondria and apoptosis signal-regulated kinase 1, thereby leading to apoptosis in A549 human lung adenocarcinoma. AMRI-59 exhibits significant antitumor activity without apparent acute toxicity .
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-
- HY-15289R
-
|
FUB 359 maleate (Standard)
|
Histamine Receptor
Reference Standards
|
Neurological Disease
Endocrinology
|
|
Ciproxifan (maleate) (Standard) is the analytical standard of Ciproxifan (maleate). This product is intended for research and analytical applications. Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease .
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-
- HY-160061
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
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-
- HY-114076
-
|
|
GABA Receptor
|
Neurological Disease
|
|
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .
|
-
- HY-147841
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
|
-
- HY-100743R
-
|
2-Amino-4-phosphonobutyric acid (Standard)
|
mGluR
Reference Standards
|
Neurological Disease
Metabolic Disease
|
|
DL-AP4 (Standard) is the analytical standard of DL-AP4. This product is intended for research and analytical applications. DL-AP4 (2-Amino-4-phosphonobutyric acid) is a glutamate antagonist. DL-AP4 behaves as a competitive inhibitor of glutamate binding with an apparent Kd of 66 μM. DL-AP4 can be used for the research of central nervous system and visual system .
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-
- HY-161732
-
|
|
Bcl-2 Family
|
Cancer
|
|
GQN-B37-E is a potent selective binder and inhibitor of MCL-1. GQN-B37-E binds to the BH3-domain-binding pocket in MCL-1. GQN-B37-E exhibits binding affinity for MCL-1 at the submicromolar range (Ki = 0.6 μM) without apparent binding to BCL-2 or BCL-XL .
|
-
- HY-P1210
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-P1210A
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-144637
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
- HY-178148
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
|
-
- HY-144123
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1 inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitory activity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitory activity or acute toxicity .
|
-
- HY-P11034
-
|
|
PKG
|
Inflammation/Immunology
|
|
BPDEtide is a synthetic peptide. BPDEtide has apparent Km values of 68 and 320 μM for cGK and cAK, respectively. BPDEtide is the most selective peptide substrate for measuring cGK activity .
|
-
- HY-171185
-
|
|
Drug Metabolite
|
Others
|
|
CP-611,781 is a diol metabolite of ezlopitant alkene (CJ-12,458). In human liver microsomes, the apparent KM value of 5.4 μM for the formation of CP-611,781 .
|
-
- HY-101226R
-
|
|
mGluR
Reference Standards
|
Neurological Disease
|
|
MSOP (Standard) is the analytical standard of MSOP (HY-101226). This product is intended for research and analytical applications. MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent KD of 51 μM for the L-AP4-sensitive presynaptic mGluR.
|
-
- HY-108643R
-
|
|
Reference Standards
MAPKAPK2 (MK2)
|
Cancer
|
|
CMPD1 (Standard) is the analytical standard of CMPD1 (HY-108643). This product is intended for research and analytical applications. CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330 nM .
|
-
- HY-103222R
-
|
3',4'-Dimethoxy-αNF (Standard)
|
Reference Standards
Aryl Hydrocarbon Receptor
|
Inflammation/Immunology
|
|
DiMNF (Standard) is the analytical standard of DiMNF (HY-103222). This product is intended for research and analytical applications. DiMNF (3',4'-Dimethoxy-αNF) is a selective aryl hydrocarbon receptor (AHR) modulator. DiMNF is a competitive AHR ligand (IC50 = 21 nM) with apparent antagonistic activity. DiMNF can be used as an anti-inflammatory agent .
|
-
- HY-P11770
-
|
|
Microtubule/Tubulin
|
Others
|
|
α-Tubulin (residues 440-451) (α-Tubulin Tail) is a Microtubule growth inhibitor. α-Tubulin (residues 440-451) transiently interacts with the longitudinal polymerization interface of α-tubulin, regulating the apparent association and dissociation rates of tubulin at the microtubule growing end. α-Tubulin (residues 440-451) inhibits microtubule growth .
|
-
- HY-106008R
-
|
BAL27862 (Standard)
|
Reference Standards
Microtubule/Tubulin
|
Cancer
|
|
Avanbulin (Standard) is the analytical standard of Avanbulin (HY-106008). This product is intended for research and analytical applications. Avanbulin (BAL27862) is a potent, Colchicine site-binding, tubulin assembly inhibitor. Avanbulin inhibits tubulin assembly at 37 °C with an IC50 of 1.4 μM. Avanbulin binds to tubulin with an apparent Kd value of 244 nM. Avanbulin can be used for the research of cancer and cell division .
|
-
- HY-180654A
-
|
|
Molecular Glues
Drug Derivative
E1/E2/E3 Enzyme
|
Cancer
|
|
JWZ-8-103 hydrochloride is an orally active PRLX-93936 (HY-119264) analog and TRIM21-targeting molecular glue. JWZ-8-103 hydrochloride increases the thermal stability of TRIM21. JWZ-8-103 hydrochloride promotes a robust and rapid interaction between TRIM21 and NUP98 (apparent EC50 = ∼20 μM for TRIM21 PRYSPRY and NUP98 APD). JWZ-8-103 hydrochloride has anti-cancer effects against pancreatic cancer .
|
-
- HY-180654
-
|
|
Molecular Glues
Drug Derivative
E1/E2/E3 Enzyme
|
Cancer
|
|
JWZ-8-103 is an orally active PRLX-93936 (HY-119264) analog and TRIM21-targeting molecular glue. JWZ-8-103 increases the thermal stability of TRIM21. JWZ-8-103 promotes a robust and rapid interaction between TRIM21 and NUP98 (apparent EC50 = ∼20 μM for TRIM21 PRYSPRY and NUP98 APD). JWZ-8-103 has anti-cancer effects against pancreatic cancer .
|
-
- HY-103017AR
-
|
|
Reference Standards
IRAK
|
Infection
Inflammation/Immunology
Cancer
|
|
JH-X-119-01 (Standard) is the analytical standard of JH-X-119-01 (HY-103017A). This product is intended for research and analytical applications. JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice . JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM .
|
-
- HY-182016
-
|
|
PROTACs
ATM/ATR
Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
Caspase
Bcl-2 Family
MDM-2/p53
|
Cancer
|
|
PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer .
|
-
- HY-180172
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA G667C degradation (DC50 = 24.69 nM; Dmax > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1 G667C cells with an IC50 value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research .
|
-
- HY-18654A
-
|
|
mGluR
|
Neurological Disease
|
|
ADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease .
|
-
- HY-10349
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist .
|
-
- HY-115596
-
|
|
Calcium Channel
|
Neurological Disease
|
|
BTT-369 is a CaVα1·CaVβ3 protein-protein complex antagonist with a Ki of 2.0 μM. BTT-369 inhibits CaV2.2 currents, with an apparent IC50 value of 31 μM. BTT-369 disrupts the interaction between CaVα1 and CaVβ3 subunits. BTT-369 reduces the current density of CaV2.2, and shifts the voltage dependence of steady-state inactivation and activation of CaV2.2 to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain .
|
-
- HY-168650
-
|
|
ROCK
HDAC
|
Inflammation/Immunology
Cancer
|
|
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .
|
-
- HY-109014R
-
|
CMX-157 (Standard)
|
HIV
HBV
Nucleoside Antimetabolite/Analog
Reference Standards
|
Infection
|
|
Tenofovir exalidex (Standard) is the analytical standard of Tenofovir exalidex. This product is intended for research and analytical applications. Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
|
-
- HY-10349R
-
|
|
Reference Standards
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
WAY-100635 (Standard) is the analytical standard of WAY-100635. This product is intended for research and analytical applications. WAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71.
WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist .
|
-
- HY-P99148
-
|
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-Mouse TNF alpha Antibody (TN3-19.12) is an anti-mouse TNF alpha IgG antibody inhibitor derived from host Armenian Hamster. Anti-Mouse TNF alpha Antibody (TN3-19.12) neutralizes cytotoxic activity in supernatants obtained from LNC-8 cells. Anti-Mouse TNF alpha Antibody (TN3-19.12) reduces the symptoms and severity of EAE (experimental allergic encephalomyelitis) in LNC-8 cells xenograft mice models. Anti-Mouse TNF alpha Antibody (TN3-19.12) prevents diabetes in NOD mice. Anti-Mouse TNF alpha Antibody (TN3-19.12) shows apparent radiosensitizing effect in CD2F1 mice .
|
-
- HY-174170
-
|
|
STING
|
Cancer
|
|
(S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide (compound 4) is a STING agonist containing a key amide benzimidazole (ABZI) component and shows reproducible inhibition of 3H-cGAMP binding to STING with an apparent inhibition constant IC50 of 14 μM. (S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide can be used for tumor research .
|
-
![(S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide](//file.medchemexpress.com/product_pic/hy-174170.gif)
- HY-173148
-
|
|
SARS-CoV
|
Infection
|
|
TKB272 is an orally active and selective antiviral agent targeting the main protease (Mpro) of SARS-CoV-2. It effectively blocks the infection and replication of various SARS-CoV-2 strains, including Omicron variants such as XBB.1.5 and EG.5.1. The enzymatic inhibitory activity of TKB272 shows an IC50 of 0.7 µM (against SARS-CoV-2WK-521 Mpro), and its antiviral activity at the cellular level reaches an EC50 as low as 2.6 nM (against BQ.1.1 strain in HeLahACE2-TMPRSS2 cells), with a cytotoxicity CC50 of 98 µM, indicating no apparent toxicity. In addition, TKB272 significantly suppresses the replication of SARS-CoV-2XBB.1.5 in B6.Cg-Tg(K18-hACE2)2-Prlmn/J transgenic mouse models. TKB272 holds promise for research in the field of SARS-CoV-2 infection .
|
-
- HY-W020780
-
|
mPEG5000-Maleimide
|
Biochemical Assay Reagents
|
Cancer
|
|
mPEG5000-Mal (mPEG5000-Maleimide) is a PEG-derived selective covalent binding agent for sulfhydryl groups (RSGs), which can form irreversible thioether bonds with sulfhydryl groups under near-neutral conditions via the maleimide group. The mechanism of action of mPEG5000-Mal can be divided into two categories: firstly, as an enzyme modifier, it binds to target proteins through hydrophobic interactions, hydrogen bonds, and van der Waals forces, altering the protein's secondary structure; secondly, as a nanoparticle surface modifier, it covalently binds to sulfhydryl groups on the surface of red blood cells, changing the surface properties and morphology of the red blood cells, leading to their phagocytosis by macrophages of the reticuloendothelial system. mPEG5000-Mal can react with free cysteine in proteins, increasing the apparent molecular weight of the modified protein by 10-15 kDa for detection purposes. mPEG5000-Mal can enhance the thermal stability and catalytic activity of enzymes, and improve the macrophage targeting of nanoparticles, enabling targeted drug delivery. mPEG5000-Mal can be applied in enzyme engineering research in the food industry and in oncology, assisting radiotherapy by inhibiting tumor-associated macrophage infiltration and enhancing anti-tumor immune responses .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-D1583
-
|
DBCO-Cy5 hexafluorophosphate; Cyanine5 dibenzocyclooctyne hexafluorophosphate
|
Fluorescent Dye
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Cyanine5 DBCO (DBCO-Cy5) hexafluorophosphate is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO hexafluorophosphate has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO hexafluorophosphate can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
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- HY-D2907
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DBCO-Cy5; Cyanine5 dibenzocyclooctyne
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Fluorescent Dye
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Cyanine5 DBCO (DBCO-Cy5) is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
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- HY-DY1068
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Fluorescent Dye
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Cyanine5 DBCO (DBCO-Cy5) hexafluorophosphate (solution) is a low-toxicity azide reactive probe (NIR fluorescent dye) , for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO hexafluorophosphate has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO hexafluorophosphate can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
Solvent and concentration: DMSO: 10 mM
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| Cat. No. |
Product Name |
Type |
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- HY-D0861
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Biochemical Assay Reagents
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EGTA is a cell-impermeant specific calcium ion chelator. EGTA has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca 2+ over Mg 2+ (Mg 2+ Kd 1-10 mM). EGTA significantly inhibits the substrate adherence capacity of inflammatory macrophages .
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- HY-W020780
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mPEG5000-Maleimide
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Biochemical Assay Reagents
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mPEG5000-Mal (mPEG5000-Maleimide) is a PEG-derived selective covalent binding agent for sulfhydryl groups (RSGs), which can form irreversible thioether bonds with sulfhydryl groups under near-neutral conditions via the maleimide group. The mechanism of action of mPEG5000-Mal can be divided into two categories: firstly, as an enzyme modifier, it binds to target proteins through hydrophobic interactions, hydrogen bonds, and van der Waals forces, altering the protein's secondary structure; secondly, as a nanoparticle surface modifier, it covalently binds to sulfhydryl groups on the surface of red blood cells, changing the surface properties and morphology of the red blood cells, leading to their phagocytosis by macrophages of the reticuloendothelial system. mPEG5000-Mal can react with free cysteine in proteins, increasing the apparent molecular weight of the modified protein by 10-15 kDa for detection purposes. mPEG5000-Mal can enhance the thermal stability and catalytic activity of enzymes, and improve the macrophage targeting of nanoparticles, enabling targeted drug delivery. mPEG5000-Mal can be applied in enzyme engineering research in the food industry and in oncology, assisting radiotherapy by inhibiting tumor-associated macrophage infiltration and enhancing anti-tumor immune responses .
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- HY-D0861A
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Biochemical Assay Reagents
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EGTA tetrasodium is a cell-impermeant specific calcium ion chelator. EGTA tetrasodium has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca 2+ over Mg 2+ (Mg 2+ Kd 1-10 mM). EGTA tetrasodium significantly inhibits the substrate adherence capacity of inflammatory macrophages .
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- HY-W019901B
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Gypsum ustum (97%)
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Biochemical Assay Reagents
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Anhydrous calcium sulfate (97%) serves as an oil-based drilling fluid additive and an osteogenic material. Anhydrous calcium sulfate (97%) increases the plastic viscosity, yield point, apparent viscosity and gel strength of oil-based drilling fluids. Anhydrous calcium sulfate (97%) upregulates the expression of bone-related genes FOSL1, RUNX2 and SPP1. Anhydrous calcium sulfate (97%) significantly affects the behavior of dental pulp stem cells, enhancing their proliferation, differentiation and matrix deposition .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1411
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PcTx1; Psalmopoeus cambridgei toxin-1
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Sodium Channel
Apoptosis
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Neurological Disease
Cancer
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Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease .
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- HY-111173
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Dipeptidyl Peptidase
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Others
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Diprotin B is a dipeptidyl aminopeptidase IV (DPP IV) inhibitor. The apparent competitive inhibition of DPP-IV by the diprotins is a kinetic artifact, derived from the substrate-like nature of tripeptides containing a penultimate proline residue .
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- HY-P2355
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BOC2; Boc-Phe-dLeu-Phe-dLeu-Phe
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Formyl Peptide Receptor (FPR)
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Inflammation/Immunology
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BOC-FlFlF (Boc-Phe-dLeu-Phe-dLeu-Phe) is a selective FPR1 antagonist. Boc-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. Boc-FlFlF can be used for the study of inflammation .
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- HY-P1105
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Chloride Channel
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Neurological Disease
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GaTx2 is a seletive and a high affinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
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- HY-P5114A
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Calcium Channel
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Others
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Maurocalcine TFA is an agonist of ryanodine receptor (RyR) channel types 1, 2 and 3 with cellular permeability. Maurocalcine TFA induces [ 3H]ryanodine binding on RyR1 with an EC50 value of 2558 nM. Maurocalcine TFA exhibits a apparent affinity of 14 nM for RyR2. Maurocalcine TFA can be applied to in vivo cell tracking or other cell imaging techniques .
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- HY-P1411A
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PcTx1 TFA; Psalmopoeus cambridgei toxin-1 TFA
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Sodium Channel
Apoptosis
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Neurological Disease
Cancer
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Psalmotoxin 1 (PcTx1) TFA is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 TFA is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 TFA can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 TFA can be used in the research of cancers, or neurological disease .
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- HY-114150
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PAI-1
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Others
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D-Val-Leu-Arg-pNA is a glandular kininoreleasing enzyme substrate that also acts as a substrate for tissue-type plasminogen activator (t-PA) with no apparent affinity for fibrin .
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- HY-P2355A
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BOC2 TFA; Boc-Phe-dLeu-Phe-dLeu-Phe TFA
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Formyl Peptide Receptor (FPR)
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Inflammation/Immunology
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BOC-FlFlF (TFA) (Boc-Phe-dLeu-Phe-dLeu-Phe (TFA)) is a selective FPR1 antagonist. BOC-FlFlF has an apparent dissociation constant (KD) of 230 nM as determined by the intracellular calcium mobilization assay. BOC-FlFlF can be used for the study of inflammation .
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- HY-P10823
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Amyloid-β
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Neurological Disease
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RI-OR2, a retro-inverso peptide, is an amyloid-β (Aβ) oligomerization inhibitor. RI-OR2 binds to immobilized β-Amyloid (1-42) (HY-P1363A) monomers and fibrils, with an apparent Kd of 9-12 μM, and also acted as an inhibitor of Aβ(1-42) fibril extension .
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- HY-P5114
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Calcium Channel
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Others
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Maurocalcine is an agonist of ryanodine receptor (RyR) channel types 1, 2 and 3 with cellular permeability. Maurocalcine induces [ 3H]ryanodine binding on RyR1 with an EC50 value of 2558 nM. Maurocalcine exhibits a apparent affinity of 14 nM for RyR2. Maurocalcine can be applied to in vivo cell tracking or other cell imaging techniques .
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- HY-P1210
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Melanocortin Receptor
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Endocrinology
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Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
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- HY-P1210A
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Melanocortin Receptor
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Endocrinology
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Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
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- HY-P11034
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PKG
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Inflammation/Immunology
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BPDEtide is a synthetic peptide. BPDEtide has apparent Km values of 68 and 320 μM for cGK and cAK, respectively. BPDEtide is the most selective peptide substrate for measuring cGK activity .
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- HY-P11770
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Microtubule/Tubulin
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Others
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α-Tubulin (residues 440-451) (α-Tubulin Tail) is a Microtubule growth inhibitor. α-Tubulin (residues 440-451) transiently interacts with the longitudinal polymerization interface of α-tubulin, regulating the apparent association and dissociation rates of tubulin at the microtubule growing end. α-Tubulin (residues 440-451) inhibits microtubule growth .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P990534
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K1-70
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TSH Receptor
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Endocrinology
Cancer
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Anti-TSHR Antibody (K1-70) is an anti-TSHR monoclonal antibody. Anti-TSHR Antibody (K1-70) incorporates a single-chain variable fragment into a chimeric antigen receptor to redirect T cells to TSHR-expressing cells. Anti-TSHR Antibody (K1-70) shows antitumor activity with no apparent toxicity. Anti-TSHR Antibody (K1-70) can be used for the research of differentiated thyroid cancer (DTC) .
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-
(5)
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- HY-P99148
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TNF Receptor
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Metabolic Disease
Inflammation/Immunology
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Anti-Mouse TNF alpha Antibody (TN3-19.12) is an anti-mouse TNF alpha IgG antibody inhibitor derived from host Armenian Hamster. Anti-Mouse TNF alpha Antibody (TN3-19.12) neutralizes cytotoxic activity in supernatants obtained from LNC-8 cells. Anti-Mouse TNF alpha Antibody (TN3-19.12) reduces the symptoms and severity of EAE (experimental allergic encephalomyelitis) in LNC-8 cells xenograft mice models. Anti-Mouse TNF alpha Antibody (TN3-19.12) prevents diabetes in NOD mice. Anti-Mouse TNF alpha Antibody (TN3-19.12) shows apparent radiosensitizing effect in CD2F1 mice .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-15772S1
-
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Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
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-
-
- HY-15772S
-
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Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
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-
-
- HY-144354S
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S-Benzyl-DL-cysteine-2,3,3-d3 is a deuterium labeled Benzylcysteine. Benzylcysteine is an ASCT2 inhibitor that binds to ASCT2 with an apparent Ki of 780 μM. Benzylcysteine inhibit ASCT2 function based on a competitive mechanism, indicating that Benzylcysteine binds to the substrate-binding site of ASCT2 .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-D1583
-
|
DBCO-Cy5 hexafluorophosphate; Cyanine5 dibenzocyclooctyne hexafluorophosphate
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|
DBCO
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Cyanine5 DBCO (DBCO-Cy5) hexafluorophosphate is a low-toxicity azide reactive probe (NIR fluorescent dye), for imaging azide-labeled biomolecules via a copper-free "click-through" reaction. Cyanine5 DBCO hexafluorophosphate has no apparent cytotoxicity or animal toxicity and shows no damage to the physiological functions of cells other than the target cells (azide-labeled cells). Cyanine5 DBCO hexafluorophosphate can be used to label and track cells in vitro and in vivo (Ex=635 nm, Em=650-700 nm) .
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| Cat. No. |
Product Name |
|
Classification |
-
- HY-130463
-
|
PG(16:0/18:1); 1-Palmitoyl-2-oleoyl-sn-glycero-3-phospho-(1'-rac-glycerol)
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|
Phospholipids
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POPG sodium salt is a negatively charged phospholipid. POPG sodium salt affects the interactions of membrane proteins with other molecules by changing the charge characteristics of the lipid environment. POPG sodium salt increases the apparent affinity of Gαq and Gβ1γ1 for activated NTS1. POPG sodium salt can interact with the positive charge of peptides. POPG sodium salt can be used in Parkinson's disease research .
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-
- HY-109014
-
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CMX-157
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|
Phospholipids
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Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
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-
- HY-164185
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Aptamers
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P12FR2 sodium is an aptamer targeting human pancreatic adenocarcinoma up-regulated factor (PAUF). P12FR2 specifically binds to human PAUF with an estimated apparent KD of 77 nM. P12FR2 inhibits PAUF-induced PANC-1 cell migration and pancreatic cancer xenograft growth.
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- HY-160061
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Aptamers
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P12FR2 aptamer sodium is a 2'-fluoropyrimidine-modified RNA aptamer targeting human PAUF with an estimated apparent KD of 77 nM. P12FR2 aptamer sodium inhibits PAUF-induced migration of PANC-1 (human pancreatic cancer cells) in wound healing assays and suppresses tumor growth in a mouse CFPAC-1 pancreatic cancer model .
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![(S)-2-(1-Ethyl-3-methyl-1H-pyrazole-5-carboxamido)-1-(2-hydroxy-2-phenylethyl)-1H-benzo[d]imidazole-5-carboxamide](http://file.medchemexpress.com/product_pic/hy-174170.gif)
