Search Result
Results for "
apparent
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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-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-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-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-15294
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- HY-147807
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HIV
Cytochrome P450
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Infection
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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-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-119211
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- HY-153419
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Others
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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-D1417
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Fluorescent Dye
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Others
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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
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-
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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-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-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-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-W713312
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5-HT Receptor
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Neurological Disease
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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-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-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-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-171185
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Drug Metabolite
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Others
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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 .
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- HY-164484
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Raf
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Cancer
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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-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-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-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-136251
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CRISPR/Cas9
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Infection
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BRD0539 is a cell-permeable and non-toxic inhibitor of CRISPR-Cas9. BRD0539 inhibits Streptococcus pyogenes Cas9 (SpCas9) (apparent IC50=22 μM) in an in vitro DNA cleavage assay .
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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-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-107604
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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-N10239
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Others
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Metabolic Disease
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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-115755
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6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5'-triphosphate; 6-Thio-ITP
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DNA/RNA Synthesis
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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-125776
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BAS 490 F
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Fungal
Mitochondrial Metabolism
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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-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-123189
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Dopamine Receptor
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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-136453A
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Mucin
Drug Isomer
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Cancer
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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-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-146407
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Apoptosis
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Cancer
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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
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Cholinesterase (ChE)
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Neurological Disease
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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-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-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-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-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-D0861
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Biochemical Assay Reagents
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Inflammation/Immunology
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EGTA is a 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-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-D0861A
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Biochemical Assay Reagents
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Inflammation/Immunology
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EGTA tetrasodium is a 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-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-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[1].
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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-125776R
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Fungal
Mitochondrial Metabolism
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Infection
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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-125209A
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DNA/RNA Synthesis
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Cancer
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TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells .
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- HY-15772
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Osimertinib
Maximum Cited Publications
119 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-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-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-160061
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Biochemical Assay Reagents
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Cancer
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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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- HY-111125
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Parasite
Reactive Oxygen Species
Apoptosis
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Infection
Cancer
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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-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-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-147841
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HIV
Reverse Transcriptase
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Infection
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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 .
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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[1].
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- HY-114076
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GABA Receptor
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Neurological Disease
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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 .
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- HY-15772R
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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-15772AR
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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-161732
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Bcl-2 Family
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Cancer
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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 .
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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-159959
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Proton Pump
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Others
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cis-3-Indoleacrylic acid is a nematicidal compound that can be isolated from Streptomyces youssoufiensis YMF3.862. cis-3-Indoleacrylic acid is also a V‑ATPase inhibitor, and inhibits V-ATPase expression and enzyme activity. cis-3-Indoleacrylic acid causes Meloidogyne incognita juveniles to have swollen bodies with apparent cracks on the cuticle surface (LC50: 16.31 μg/mL). cis-3-Indoleacrylic acid inhibits H + accumulation in nematode bodies .
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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-P1411A
-
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PcTx1 TFA; Psalmopoeus cambridgei toxin-1 TFA
|
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-19350
-
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-D1583
-
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DBCO-Cy5; Cyanine5 dibenzocyclooctyne
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Fluorescent Dye
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Others
|
|
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-P1210A
-
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|
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 .
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-
- HY-144637
-
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Apoptosis
Autophagy
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Cancer
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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 .
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-
- HY-172236
-
|
BNC210; IW-2143
|
nAChR
|
Neurological Disease
|
|
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-159190
-
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MAPKAPK2 (MK2)
|
Cancer
|
|
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-144123
-
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HIV
|
Infection
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|
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 .
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-
- HY-109014
-
|
CMX-157
|
HIV
HBV
Nucleoside Antimetabolite/Analog
|
Infection
|
|
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-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 .
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-
- 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 .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D1583
-
|
DBCO-Cy5; Cyanine5 dibenzocyclooctyne
|
Fluorescent Dyes/Probes
|
|
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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| Cat. No. |
Product Name |
Type |
-
- HY-D0861
-
|
|
Chelators
|
|
EGTA is a 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-D0861A
-
|
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Biochemical Assay Reagents
|
|
EGTA tetrasodium is a 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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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-111173
-
|
|
Dipeptidyl Peptidase
|
Others
|
|
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-P1105
-
|
|
Chloride Channel
|
Neurological Disease
|
|
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
-
|
|
Calcium Channel
|
Others
|
|
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-P1411
-
|
PcTx1; Psalmopoeus cambridgei toxin-1
|
Sodium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
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 .
|
-
- HY-P1411A
-
|
PcTx1 TFA; Psalmopoeus cambridgei toxin-1 TFA
|
Sodium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
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 .
|
-
- 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-114150
-
|
|
PAI-1
|
Others
|
|
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 .
|
-
- HY-P10823
-
|
|
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 .
|
-
- 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 .
|
-
- 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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-144354S
-
|
|
|
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[1].
|
-
-
- HY-15772S1
-
|
|
|
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.
|
-
-
- HY-15772S
-
|
|
|
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[1].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-164185
-
|
|
|
Aptamers
|
|
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.
|
-
- HY-160061
-
|
|
|
Aptamers
|
|
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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