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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 "
hydrophobic S1 pocket
" in MedChemExpress (MCE) Product Catalog:
Products (4)
4 Results for "hydrophobic S1 pocket" in MCE Product Catalog:
1
Target:
Research Areas:
Sebetralstat (KVD900) is an orally active and selective plasma kallikrein inhibitor, with an IC50 of 6.0 nM and a Ki of 3.0 nM against the human target. Sebetralstat binds to the active site of plasma kallikrein, inducing a conformational flip of Trp215 to form a U-shaped conformation; its P1 group interacts with the S1 pocket through hydrophobic interactions and displacement of high-energy water molecules, independent of the Asp189 ionic bond. Sebetralstat inhibits plasma kallikrein-kinin system activation in whole plasma, rapidly relieves laryngeal and abdominal attack symptoms of hereditary angioedema (HAE-C1INH), and reduces attack severity. Sebetralstat can be used in research related to hereditary angioedema (HAE) .
Cat. No.: HY-184117B
CAS No.: 3098808-75-1
Target:
Research Areas:
(R)-pMeO-Bz-SF, the R isomer of pMeO-Bz-SF (HY-184117), is an α-chymotrypsin inhibitor with an IC50 of 101 nM. (R)-pMeO-Bz-SF covalently modifies Ser195, Ser190, and Tyr146 in or near α-chymotrypsin’s hydrophobic S1 binding pocket. (R)-pMeO-Bz-SF inhibits α-chymotrypsin in a stereoselective manner .
Cat. No.: HY-132830A
CAS No.: 2163789-76-0
Synonyms: KVD900 hydrochloride
Target:
Research Areas:
Sebetralstat hydrochloride (KVD900 hydrochloride) is an orally active and selective plasma kallikrein inhibitor, with an IC50 of 6.0 nM and a Ki of 3.0 nM against the human target. Sebetralstat hydrochloride binds to the active site of plasma kallikrein, inducing a conformational flip of Trp215 to form a U-shaped conformation; its P1 group interacts with the S1 pocket through hydrophobic interactions and displacement of high-energy water molecules, independent of the Asp189 ionic bond. Sebetralstat hydrochloride inhibits plasma kallikrein-kinin system activation in whole plasma, rapidly relieves laryngeal and abdominal attack symptoms of hereditary angioedema (HAE-C1INH), and reduces attack severity. Sebetralstat hydrochloride can be used in research related to hereditary angioedema (HAE) .
Cat. No.: HY-183009
Target:
Research Areas:
Pf20S-IN-1 is a selective inhibitor of the 20S proteasome β5 subunit of Plasmodium falciparum. Pf20S-IN-1 exhibits antiparasitic activity against Plasmodium falciparum, with an EC50 of 20.1 nM against the Plasmodium falciparum W2 strain. Pf20S-IN-1 shows weak inhibitory effect on human 20S proteasome, has no obvious toxicity to human foreskin fibroblasts (HFF), and has a selectivity index > 25000. Pf20S-IN-1 can be used in malaria research .
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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
