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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
4 Results for "
EP function
" in MedChemExpress (MCE) Product Catalog:
Products (4)
4 Results for "EP function" in MCE Product Catalog:
Cat. No.: HY-173499
CAS No.: 3077339-88-6
HLDA-212 is a non-covalent RIPTAC that targets FKBP (target protein, TP) and multiple CDK (effector protein, EP). HLDA-212 binds to FKBP and CDK to form a stable ternary complex (TP:RIPTAC:EP), and induces cell death by blocking FKBP function. HLDA-212 selectively inhibits the proliferation of CDK-expressing cells and accumulates in CDK-expressing cells in a CDK-dependent manner. HLDA-212 exhibits antiproliferative activity in 293_HFL cells (with a GI50 of 0.011 μM). HLDA-212 holds promise for the treatment of cancers with high FKBP expression .
Cat. No.: HY-187732
CAS No.: 76739-51-0
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EP-459 is a papain inhibitor (IC50=0.4 μg/mL) with no significant inhibitory activity against serine proteases such as trypsin, plasmin, thrombin, and urokinase. The effects of EP-459 are similar to those of E-64C (HY-100227), but differ from the functions of leupeptin and its analogs. EP-459 can serve as a titration reagent for mouse cathepsin L (precursor form/MEP) activity, covalently binding to the cysteine residue at its active site. EP-459 is also a Ca 2+-dependent active site-directed inhibitor that can inactivate chicken gizzard smooth muscle calpain II, and can be acetylated to generate Ac-Ep-459, which after radiolabeling can be used to prepare [ 3H]Ac-Ep-459 for calpain active site labeling .
Cat. No.: HY-187689
CAS No.: 1005056-10-9
RKN5755 is a β-arrestin1 inhibitor and a selective inhibitor of activated fibroblasts. RKN5755 binds to β-arrestin1 and interferes with the cofilin signaling pathway mediated by this protein to block its function. RKN5755 not only inhibits the enhanced migratory effect of fibroblasts co-cultured with cancer cells, but also prevents the inhibitory effect of EP3 agonists on the EP2 receptor-induced elevation of tetrodotoxin-resistant sodium currents in mouse dorsal root ganglion neurons. RKN5755 is widely used in research on related diseases such as cancer metastasis and pain .
Cat. No.: HY-182513
CAS No.: 459842-29-6
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ONO-8539 is an orally active prostanoid EP1 receptor antagonist with competitive, insurmountable binding and slow receptor dissociation for long-duration inhibition. ONO-8539 modulates afferent nerve function related to bladder activity, inhibits detrusor overactivity-related contractions, decreases nonvoiding contractions and voiding duration, and increases uroflow rate with ATP (HY-B2176)-induced detrusor overactivity. ONO-8539 attenuates acid-induced heartburn symptoms, extends time to first heartburn sensation, and prevents primary hypersensitivity after distal esophageal acidification. ONO-8539 can be used for the research of overactive bladder and gastroesophageal reflux disease .
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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
