Proteases

PCSK9-IN-10 is an effective, orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. It increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 can slow down the progression of atherosclerosis. It has potential for researching hyperlipidemia.

PCSK9-IN-11 (compound 5r) is an orally effective PCSK9 inhibitor. PCSK9-IN-11 exhibits transcriptional inhibition activity of PCSK9 in HepG2 cells with an IC50 of 5.7 μM. PCSK9-IN-11 increases the protein level of LDL receptor (LDLR). PCSK9-IN-11 can be used for atherosclerosis research.

PCSK9-IN-12 is a heteroaromatic compound. It has binding affinity to PCSK9 with a Kd value of

PFB-FDGlu is a cell membrane-permeable fluorescent substrate specifically used for detecting glucocerebrosidase (GCase) activity in living cells.

Propionyl-DL-carnitine chloride is a derivative of carnitine. It can be used for research on inflammation.

PU-H54 is a selective inhibitor of Grp94, which can be used for the study of breast cancer. The Hsp90 chaperone family includes Hsp90α, Hsp90β, Grp94 and Trap-1, which play important roles in malignant tumors.

RO5461111 is a highly specific and orally effective Cathepsin S inhibitor (IC50: 0.4 nM, human Cathepsin S; 0.5 nM, murine Cathepsin S). It can effectively inhibit antigen-specific T cell and B cell activation. RO5461111 has an improvement effect on pulmonary inflammation and lupus nephritis.

RPR132595A (NPC) hydrochloride is an active metabolite of CPT-11, which is produced by cytochrome P-450 3A4 (CYP3A4) and ultimately excreted through urine.

Rugonersen (RG6091; RO7248824) is an antisense oligonucleotide (ASO) modified with locked nucleic acid (LNA), which reduces the silencing of ubiquitin protein ligase E3A (UBE3A). Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A. Rugonersen has been used in research on AS.

Sampatrilat (UK-81252) is a potent orally active vasopeptidase inhibitor that inhibits both angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). Sampatrilat has 12.4 times greater inhibition of C-domain ACE (Ki=13.8 nM) compared to N-domain ACE (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for research related to chronic heart failure and blood pressure regulation.

Sarcosine-d3 is the deuterated form of Sarcosine. Sarcosine (N-Methylglycine) is an endogenous amino acid that acts as a competitive inhibitor of glycine transporter-1 (GlyT1) and a co-agonist at the glycine site of NMDA receptors. By increasing the concentration of glycine, sarcosine enhances the function of NMDA receptors. Sarcosine is commonly used in research on schizophrenia.

SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis in NSCLC cells and exhibits anti-tumor activity.

Sitagliptin phenylalanine is a dipeptidyl peptidase-4 (DPP-4) inhibitor.

Sitagliptin phenylalanine hydrochloride is a dipeptidyl peptidase-4 (DPP-4) inhibitor.

Skp2 inhibitor 1 (compound 14i) is a Skp2 inhibitor that disrupts the Skp2-Cks1 interaction, with an IC50 of 2.8 μM. Skp2 inhibitor 1 also exhibits anti-cancer activity.

(S)-Malic acid-d3 is the deuterated form of (S)-Malic acid. (S)-Malic acid ((S)-2-Hydroxysuccinic acid) is a naturally occurring dicarboxylic acid and a source of fruity sour taste, commonly used as a food additive.

Stearic acid-d7 is the deuterated form of stearic acid. Stearic acid is a long-chain dietary saturated fatty acid that exists in many animal and plant fats.

Sucrose-d14 is the deuterated form of sucrose. Sucrose (D-(+)-Saccharose) is a disaccharide composed of glucose and fructose. Sucrose can be used in some animal models, including metabolic diseases, obesity, picky eating, diabetes, etc.

Terephthalic acid-13C2 is a 13C-labeled Terephthalic acid. Terephthalic acid is an isomer of three phthalate salts and a precursor to the polyester PET, which can be used in clothing and plastic production.

TG-2-IN-1 (Compound D003) is a transglutaminase-2 (TGM-2) inhibitor. TG-2-IN-1 can be used for myopia research.

Tyrosinase-IN-2 (compound 67) is an effective tyrosinase inhibitor. Tyrosinase is a copper-containing enzyme responsible for the rate-limiting catalytic step in melanin biosynthesis and enzymatic browning. Tyrosinase-IN-2 has potential as a research tool for skin whitening agents and food preservatives.

UBA5-IN-1 (compound 8.5) is a selective inhibitor of UBA5 with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits the proliferation of Sk-Luci6 cancer cells that overexpress UBA5.

UDP-rhamnose is one of the substrates for pectin synthesis in cell walls. UDP-rhamnose can be recognized in fungi and is one of the most common sugar donors in plants.

WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. It inhibits the phosphorylation of OSR1 with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for research on blood pressure regulation and cancer treatment.