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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
489 Results for "
profiling
" in MedChemExpress (MCE) Product Catalog:
Products (489)
489 Results for "profiling" in MCE Product Catalog:
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1 Cited Publications
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p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
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1 Cited Publications
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OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
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1 Cited Publications
Cat. No.: HY-W754777
CAS No.: 68054-73-9
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IPPD-Q is a p-phenylenediamine quinone and also Environmental pollutant. IPPD-Q can be present in tires, fine particulate matter and urban water bodies. IPPD-Q increases the activities of antioxidant enzymes (SOD, CAT), alters photosynthesis and energy metabolism pathways, and changes gene expression and metabolic profiles. IPPD-Q exhibits phytotoxic effects. IPPD-Q shows acute toxicity to zebrafish embryos and reduces their survival rate .
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1 Cited Publications
Cat. No.: HY-136576
CAS No.: 1306760-73-5
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RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile .
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1 Cited Publications
Cat. No.: HY-P99242
CAS No.: 2254029-91-7
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1 Cited Publications
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EDI048 is an orally active, gut-restricted parasiticidal agent. EDI048 specifically binds to the ATP-binding site of Cryptosporidium phosphatidylinositol 4-kinase (CpPI (4) K), blocks parasite membrane biogenesis, arrests the pathogen at the schizont stage, and thus irreversibly clears the infection. EDI048 is rapidly converted to an inactive carboxylic acid metabolite via hepatic first-pass metabolism, with extremely low systemic exposure, good safety profile, and no cardiotoxicity, genotoxicity or off-target effects. EDI048 is used in studies of intestinal cryptosporidiosis in children .
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1 Cited Publications
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
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Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
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1 Cited Publications
BCI-137 is a Argonaute 2 (AGO2) inhibitor. By inhibiting AGO2 function, reducing PTPN6/SHP-1 protein levels and enhancing STAT1 phosphorylation, BCI-137 restores the sensitivity of tumor cells to IFN-γ. BCI-137 effectively enhances the recruitment, activation and cytotoxicity of CD8 + T cells. BCI-137 exerts a synergistic effect with anti-PD-1 antibodies and significantly reduces tumor volume in preclinical mouse models. BCI-137 exhibits favorable safety profiles and does not cause significant weight loss or death in mice. BCI-137 can be used in research related to bladder cancer, colorectal cancer, melanoma and other related fields .
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1 Cited Publications
Cat. No.: HY-175324
CAS No.: 3098773-64-6
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MG-HuR2 is a molecular glue degrader targeting HuR (ELAVL1) with a Kd of 0.2018 μM. MG-HuR2 recruits the E3 ubiquitin ligase RNF126 and induces proteasome-dependent degradation of HuR. MG-HuR2 exhibits a unique biphasic degradation profile. MG-HuR2 reduces the expression of HuR and its downstream targets Bcl2/FOXQ1, inhibits breast cancer cell proliferation, enhances cytotoxicity and apoptosis (apoptosis), and suppresses the growth of 3D breast cancer tumor spheres. MG-HuR2 can be used in studies related to breast cancer and HuR-targeted protein degradation .
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1 Cited Publications
Cat. No.: HY-W725179
CAS No.: 2044520-06-9
VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
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Infection Phenols Polyphenols Plants Rhamnaceae Aconitum nagarum var. acaule (Finet & Gagnep.) Q. E. Yang Disease Research Fields
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Cat. No.: HY-W011053
CAS No.: 165450-17-9
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Neotame is a derivative of Aspartame (HY-B0361) and is a flavor enhancer and low-caloric, non-nutritive, high-intensity artificial sweetener that is 7000-13,000 times sweeter than sugar. Neotame causes intestinal epithelial cell death at high concentrations. Neotame induces Apoptosis of Caco-2 cells .
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SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
Synonyms: EPH 116 hydrochloride
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SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
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PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
Cat. No.: HY-119926
CAS No.: 15358-48-2
Synonyms: Hydroxylupanine
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13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
Cat. No.: HY-W075766
CAS No.: 10028-18-9
Synonyms: Nickel difluoride
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
