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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
431 Results for "
iBH3 profiling
" in MedChemExpress (MCE) Product Catalog:
Products (431)
431 Results for "iBH3 profiling" in MCE Product Catalog:
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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 [3] .
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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 [3] .
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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 [3].
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Infection Phenols Polyphenols Plants Aconitum nagarum var. acaule (Finet & Gagnep.) Q. E. Yang Disease Research Fields Rhamnaceae Extract
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BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1) apelin-13. BMS-986224 has the potential for the research of heart failure .
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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AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .
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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 .
WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile [3].
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 .
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
Cat. No.: HY-D1082
CAS No.: 51306-35-5
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YM-26734 is a competitive inhibitor of secretory phospholipase A 2 (PLA 2) that exhibits a broad inhibitory profile to several PLA2s .
Cat. No.: HY-16421
CAS No.: 222834-30-2
Synonyms: (-)-DRF 2725; NNC 61-0029
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Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
Cat. No.: HY-W075766
CAS No.: 10028-18-9
Synonyms: Nickel difluoride
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AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
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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
