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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC81177 NSC 121182
NSC 121182 is a compound selected from NCI Diversity Set II by structure-based virtual screening. NSC 121182 can be used to study the Vitronectin-uPAR interaction. NSC 121182 can be used for cancer research.
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DC81156 Nivimedone
Nivimedone (BRL 10833 free base) is an orally active antiallergic agent. Nivimedone inhibits IgE-mediated passive cutaneous anaphylaxis in rats. Nivimedone suppresses antigen-induced histamine release from lung tissues passively sensitized with atopic serum. Nivimedone can be used in research related to bronchial asthma.
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DC81149 NFYi5
NFYi5 is a nuclear transcription factor-Y (NF-Y) inhibitor. NFYi5 disrupts the binding of NF-Y to DNA, accelerates the ubiquitin-independent degradation of the NF-YA subunit, and reduces the transcriptional activity of NF-Y. As an antimitotic agent, NFYi5 decreases the mRNA levels of NF-Y target genes without affecting the expression of housekeeping genes, and inhibits cell proliferation. NFYi5 can be used in the research of tissue fibrosis.
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DC81122 Nav1.8-IN-22
Nav1.8-IN-22 (Formula I) is a Nav1.8 sodium channel inhibitor. Nav1.8-IN-22 regulates sodium channel activity by directly binding to Nav1.8. Nav1.8-IN-22 is applicable for pain-related research.
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DC81112 nAChR antagonist 3
nAChR antagonist 3 is a selective α7 nAChR antagonist with an IC50 of 0.86 μM. nAChR antagonist 3 exerts a protective effect against paraoxon-induced toxicity. nAChR antagonist 3 can be used for the research of organophosphate poisoning.
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DC81082 MS 857
MS 857 is an orally active nonglycoside and nonsympathomimetic cardiotonic agent. MS 857 exhibits cardiac and coronary vasodilator effect.
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DC81079 MrgprX2 antagonist-9
MrgprX2 antagonist-9 (compound 10) is a potent Mas-related G protein-coupled receptor X2 (MrgprX2) antagonist with an IC50 value of 0.1-100 nM. MrgprX2 antagonist-9 has the potential for the research of inflammatory.
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DC81052 Mitoflaxone
Mitoflaxone (flavoneacetic acid) is a synthetic flavonoid compound with vascular targeting properties. Mitoflaxone exerts anti-proliferative effects on endothelial cells through a superoxide-dependent mechanism, this effect leads to changes in the permeability of tumor blood vessels, thereby exerting anti-tumor effects[1][2].
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DC81044 MeV-IN-1
MeV-IN-1 (OX-1) is an inhibitor of specific specific Measles virus (MeV) entry with an IC50 of 100 M. MeV-IN-1 has an IC50 of 55 M against live MeV-Edm. MeV-IN-1 efficiently suppresses the formation of infectious centers. MeV-IN-1 exhibits negligible cytotoxicity. MeV-IN-1 potently suppresses R18 redistribution in MV-H- and MV-F-expressing cells, preventing membrane merging.
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DC81032 Methoctramine
Methoctramine is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine can inhibit Muscarine-induced bradycardia in vivo. Methoctramine can be used in the study of cardiovascular diseases.
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DC81012 MC-Gly-Gly-Phe-Gly-cyclopropylacetic acid
MC-Gly-Gly-Phe-Gly-cyclopropylacetic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC81008 Masoprocol tetrapivalate
Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors.
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DC81001 MAO-B-IN-50
MAO-B-IN-50 (Compound C20) is a selective MAO-B inhibitor with an IC50 value of 0.06 μM. MAO-B-IN-50 shows good inhibitory effects on the aggregation of Aβ40/42 and Tau proteins, with overall IC50 values around 1 μM. MAO-B-IN-50 exhibits potent and selective AChE inhibition (IC50 = 1.78 μM). MAO-B-IN-50 can be used in the research of Alzheimer's disease.
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DC81000 MAO-B-IN-49
MAO-B-IN-49 is a selective and reversible MAO-B inhibitor (IC50 of 1 nM for human MAO-B). MAO-B-IN-49 shows much higher selectivity for MAO-B than for MAO-A (IC50 = 633.9 μM). MAO-B-IN-49 can reduce ROS production induced by Lipopolysaccharides (LPS) in HT22 cells. MAO-B-IN-49 demonstrates substantial neuroprotective properties and significantly improves motor dysfunction in MPTP-induced mouse models of Parkinson’s disease (PD). MAO-B-IN-49 can be used for the study of PD.
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DC80998 Mal-Pip-ValCit-PAB-AZ7550
Mal-Pip-ValCit-PAB-AZ7550 is a prodrug of EGFR inhibitor. Mal-Pip-ValCit-PAB-AZ7550 selectively binds covalently to albumin via its maleimide moiety. Mal-Pip-ValCit-PAB-AZ7550 exhibits potent in vivo anticancer activity in non-small cell lung cancer xenograft models. Mal-Pip-ValCit-PAB-AZ7550 can be used in research related to non-small cell lung cancer.
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DC80986 LY-73497
LY-73497 is a Phenethylthiazolythioureas derivative. LY-73497 has anti-HIV-1 activity.
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DC80983 LY3295668 erbumine
LY3295668 (AK-01) erbumine is a highly specific and orally active inhibitor of Aurora-A kinase with a Ki values for AurA and AurB of 0.8 nM and 1038 nM respectively. LY3295668 erbumine can effectively inhibit the autophosphorylation of AurA, induce mitotic arrest and apoptosis. LY3295668 erbumine avoids the formation of polyploids related to AurB inhibition. LY3295668 erbumine can be used for the study of small cell lung cancer.
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DC80962 L-Kynurenine-5-F
L-Kynurenine-5-F (Compound 2h) is the 5-F derivative of L-Kynurenine.
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DC80954 Lerimazoline
Lerimazoline is a selective 5-HT1D receptor agonist with Ki values of 72 and 3480 nM for h5-HT1D and h5-HT1B. Lerimazoline inhibits Forskolin-stimulated cAMP production and induces contractions in rabbit saphenous vein preparations. Lerimazoline can be used for the research of migraine.
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DC80948 LCK degrader-3
LCK degrader-3 (Compound 20) is a CRBN-based LCK molecular glue degrader. LCK degrader-3 can be used in the research of acute lymphoblastic leukemia.
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DC80945 LCB-2122
LCB-2122 is an adenosine-like nucleoside analogue bearing a C2'-stereogenic all-carbon quaternary center. LCB-2122 can prevent Doxorubicin-induced cardiomyocytes apoptosis with an IC50 of 0.5 μM and prevent Imatinib-induced apoptosis. LCB-2122 can activate AMPK signaling and induce the phosphorylation of AMPK and its downstream substrate, acetyl-CoA carboxylase (ACC). LCB-2122 can reduce Doxorubicin-induced mitochondrial damage. LCB-2122 can be used for the research of heart failure.
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DC80931 L-163958
L-163958 is an efficient, orally active, balanced angiotensin II receptor (AII receptor) antagonist. L-163958 has balanced high affinity for AT1 and AT2, with its IC50 values being 0.16, 0.12, 0.50, and 0.64 nM in rabbit aorta (AT1), rat midbrain (AT2), human adrenal gland (AT1), and human adrenal gland (AT2), respectively. L-163958 has a strong inhibitory effect on the pressor activity in rats. L-163958 can be used for the study of hypertension and related cardiovascular diseases.
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DC80906 Knoxiadin
Knoxiadin (Compound 4) is an anthraquinone found in the roots of Knoxia valerianoides.
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DC80886 JNJ-10450232
NTM-006 is a selective and brain-penetrant adenosine A3 receptor (A3AR) agonist. NTM-006 selectively interacts with adenosine A3AR via π-π stacking with Phe168 and π-alkyl interactions receptor residues. NTM-006 inhibits Acetic acid-induced writhing responses in mice. NTM-006 can be used for the research of chronic neuropathic pain, cancer-related pain, osteoarthritis-associated pain.
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DC80854 INCB059872 TFA
INCB059872 TFA is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 TFA can be used for the research of myeloid leukemia.
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DC80848 IL-17-IN-6
IL-17-IN-6 is a IL-17 inhibitor with a pIC50 of 7.6 against human targets. IL-17-IN-6 binds to IL-17A and blocks downstream pro-inflammatory signaling pathways. IL-17-IN-6 inhibits the release of IL-6 from normal human skin fibroblasts stimulated by IL-17A and TNF. IL-17-IN-6 can be used for research on inflammatory and autoimmune diseases.
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DC80838 IDO1-IN-32
IDO1-IN-32 (Compound 45) is a potent and orally effective IDO1 inhibitor with an IC50 of 10 pM. IDO1-IN-32 exhibits significant anti-proliferative activity against Hela cells. IDO1-IN-32 can significantly inhibit tumor growth in CT26 and LCC transplanted mouse models by activating anti-tumor immunity. IDO1-IN-32 can be used for research on colon cancer and breast cancer.
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DC80837 IDO1-IN-31
IDO1-IN-31 (Compound 17g) is an IDO1 agonist with an IC50 of 77 nM. IDO1-IN-31 can be used for the study of neurological diseases and cancers.
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DC80799 HIF-1α-IN-10
HIF-1α-IN-10 is a ligands for target protein for PROTAC (HIF-1α). HIF-1α-IN-10 can be used to synthesize PROTAC HIF-1α degrader-2.
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DC80791 HER2-IN-23
HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer.
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