Abcam, ab141167, Gabexate mesylate, General serine protease inhibitor

Size: 10mg / 50mg
MW 417.5 Da, Purity >99%. General serine protease inhibitor (K i values are 3.4 nM, 5, 1.8 μM and 2.6 mM at tryptase, thrombin, tyrpsin and kallikrein serine proteases respectively). Additionally inhibits nitric oxide synthase. Displays antithrombotic activity and antitumor effect. Active in vivo .
Key facts
CAS number:56974-61-9,
Purity:>99%,
Form:SolidSee storage information,
Molecular weight:417.5 Da,
Molecular formula:C17H27N3O7S,
PubChem:6604561,
Nature:Synthetic,
Solubility:Soluble in water to 100 mM,
Biochemical name:Gabexate mesylate,
Biological description:General serine protease inhibitor (Ki values are 3.4 nM, 5, 1.8 μM and 2.6 mM at tryptase, thrombin, tyrpsin and kallikrein serine proteases respectively). Additionally inhibits nitric oxide synthase. Displays antithrombotic activity and antitumor effect. Active in vivo.,
Canonical smiles:CCOC(=O)C1=CC=C(C=C1)OC(=O)CCCCCN=C(N)N.CS(=O)(=O)O,
InChi:InChI=1S/C16H23N3O4.CH4O3S/c1-2-22-15(21)12-7-9-13(10-8-12)23-14(20)6-4-3-5-11-19-16(17)18;1-5(2,3)4/h7-10H,2-6,11H2,1H3,(H4,17,18,19);1H3,(H,2,3,4),
InChiKey:DNTNDFLIKUKKOC-UHFFFAOYSA-N,
IUPAC Name:ethyl 4-[6-(diaminomethylideneamino)hexanoyloxy]benzoate;methanesulfonic acid

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-Ambient, Appropriate long-term storage conditions-Ambient, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Estrogen receptor also known as ER functions as a ligand-activated transcription factor. This receptor binds estrogens such as estradiol and regulates gene expression by interacting with specific DNA sequences. It weighs approximately 66 kilodaltons and is mainly expressed in reproductive tissues like the ovaries and uterus as well as in breast tissue. CYP2D6 is a cytochrome P450 enzyme part of a superfamily involved in the metabolism of medications. Weighing around 55 kilodaltons CYP2D6 shows expression mostly in the liver and small intestine. Kallikrein 7 or KLK7 acts as a serine protease that plays a role in skin desquamation with a mass of about 29 kilodaltons and expression found in the skin and other epithelial tissues.
Biological function summary
The estrogen receptor influences the growth and function of reproductive tissues and also plays a role in bone density maintenance. It can form complexes with co-activators for transcriptional activity. CYP2D6 is responsible for metabolizing approximately 25% of clinical drugs including antidepressants and opioids. It requires electron transfer from NADPH-cytochrome P450 reductase for its catalytic cycle. KLK7 breaks down corneodesmosomal proteins in the outer skin layers making it important for normal skin shedding. This protease does not act alone but rather as part of the kallikrein-related peptidase family.
Pathways
We see the estrogen receptor participating in the estrogen signaling pathway which is critical for sexual development and reproductive function. It interacts with co-regulators like steroid receptor coactivator-1 (SRC-1). CYP2D6 integrates into the drug metabolism pathway involving others like cytochrome P450 oxidoreductase to transform drugs into their active forms or prepare them for elimination. KLK7 participates in skin barrier formation and regulation pathways often interacting with other kallikrein-related peptidases in maintaining skin homeostasis and regulating inflammation.
Estrogen receptor's malfunction or aberrant expression links to breast cancer with overexpression often noted in hormone-receptor-positive types influencing tumor growth alongside HER2. CYP2D6 genetic polymorphisms can lead to altered drug metabolism affecting conditions like depression due to differential drug responses. KLK7 relates to atopic dermatitis where its increased activity may contribute to the disease's skin barrier dysfunction often alongside other proteases like KLK5. These associations highlight the importance of these targets in maintaining health or contributing to disease states.