subtilisin

Subtilisin (EC 3. 4. 21. 14) is a bacterially derived serine protease that promotes hepatic LDL receptor (LDLR) degradation and can be used in the study of cardiovascular disease.

Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

SBC-115076 is a potent extracellular proprotein convertase subtilisin kexin type 9 (PCSK9) antagonist.

PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.

Tripeptidyl peptidase II (TPPII) is a serine peptidase of the subtilisin-type which removes tripeptides from the free NH2 terminus of oligopeptides. AAF-CMK is an irreversible inhibitor of TPPII commonly used at 10-100 μM. It does not significantly interfere with the chymotrypsin-like activity of the proteasome. AAF-CMK also inhibits bleomycin hydrolase and puromycin-sensitive aminopeptidase when used at 50 μM.

Inclisiran sodium (ALN-PCSsc sodium) is a dual-strand siRNA conjugated with triantennary N-acetylgalactosamine (GalNAc), with antihypertensive activity. It inhibits the transcription of PCSK9, reducing the hepatic synthesis of proprotein convertase subtilisin kexin type 9, and can be used in cardiovascular disease research.

SBC-110736 is an inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9).

PCSK9 modulator-2 (Compound 1) is a potent PCSK9 modulator (EC 50 = 202 nM) with potential applications in hyperlipidemia research. Proprotein convertase subtilisin kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

MDK6465, also known as PCSK9-IN-8b, is a novel liver-targeted inhibitor of ribosomal synthesis of proprotein convertase subtilisin kexin type 9 (PCSK9). MDK6465 has CAS#1900686-46-5. the last 4 digits are used in its name.

PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.

PF-06815345 hydrochloride, an orally active potent inhibitor of proprotein convertase subtilisin kexin type 9 (PCSK9), has an IC50 value of 13.4 μM. It significantly decreases in vivo PCSK9 levels in mice.

PCSK9-IN-9, a natural isocoumarin, inhibits proprotein convertase subtilisin-kexin type 9 (PCSK9), IDOL, and SREBP2 mRNA expression, demonstrating specificity by inhibiting PCSK9 with an IC50 value of 11.9 μM [1].

Subtilisin, a bacterial serine protease [1] [2], can be detected through the activity of a fluorescent substrate designed specifically for subtilisin.

Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody to Subtilisin Kexin Protein Converting Enzyme Type 9 (PCSK9) that binds to the catalytic domain of PCSK9 and lowers low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia.Frovocimab is used in the study of hypercholesterolemia. Frovocimab is used to study hypercholesterolemia.

PCSK9-IN-15 (compound 5) is a potent inhibitor of proprotein convertase subtilisin kexin 9 (PCSK9, K D <200 nM) that plays a crucial role in cholesterol metabolism by regulating blood levels of low-density lipoprotein cholesterol (LDL-C). This compound is useful for researching cholesterol-lowering therapies and dyslipidemia [1].

PfSUB1-IN-1 (compound 4c) is an inhibitor of Plasmodium falciparum subtilisin-like serine protease 1 (PfSUB1), exhibiting potent activity with an IC50 value of 15 nM. PfSUB1 is a key target in antimalarial research. PfSUB1-IN-1 demonstrates a 13-fold greater inhibitory effect on the growth of transgenic Plasmodium falciparum strains (expressing lower levels of PfSUB1 compared to the wild-type) than on wild-type parasite strains.

Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9.

Pep 2-8 ammonium salt is Proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9.

Subtilisin/Kex2p-like proprotein convertase inhibitor; blocks activity of all seven convertases (PC1, PC2, PC4, PACE4, PC5, PC7 and furin). Abolishes proET-1 processing in endothelial cells; inhibits regulated secretion of the neuronal polypeptide VGF in

DEC-RVRK-CMK (Decanoyl-Arg-Val-Arg-Lys-chloromethylketone) TFA is a peptide-based CMK (chloromethylketone) inhibitor that targets and inactivates the secreted soluble kexin (Kex2) with a Ki value of 8.45 μM. Kex2, a yeast enzyme and a member of the mammalian subtilisin-like proprotein convertase family within the serine protease class, is a calcium-dependent transmembrane protease. The binding mechanism of Kex2 with different CMK inhibitors depends on substrate selectivity, particularly noting the differences in selectivity between lysine and arginine at the P1 position, which influences their varying binding affinities.