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Merck

219372

Cathepsin G Inhibitor I

≥98% (HPLC), solid, cathepsin G inhibitor, Calbiochem®

Synonyme(s) :

Cathepsin G Inhibitor I

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A propos de cet article

Formule empirique (notation de Hill) :
C36H33N2O6P
Numéro CAS:
Poids moléculaire :
620.63
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze
protect from light
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Nom du produit

Cathepsin G Inhibitor I, The Cathepsin G Inhibitor I, also referenced under CAS 429676-93-7, controls the biological activity of Cathepsin G. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

SMILES string

[P](=O)(O)(O)C(c5c6c(ccc5)cccc6)C(=O)c1cc2c(cc1C(=O)N(C3CCN(CC3)C(=O)c4ccccc4)C)cccc2

InChI

1S/C36H33N2O6P/c1-37(28-18-20-38(21-19-28)35(40)25-11-3-2-4-12-25)36(41)32-23-27-14-6-5-13-26(27)22-31(32)33(39)34(45(42,43)44)30-17-9-15-24-10-7-8-16-29(24)30/h2-17,22-23,28,34H,18-21H2,1H3,(H2,42,43,44)

InChI key

GNOZQRKYZJSIPZ-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

potency

53 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 5 mg/mL
methanol: soluble

shipped in

ambient

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

Cell permeable: no
Primary Target
cathepsin G
Product does not compete with ATP.
Reversible: yes
Target Ki: 63 nM for cathepsin G

Disclaimer

Toxicity: Standard Handling (A)

General description

A potent, selective, reversible, and competitive non-peptide inhibitor of cathepsin G (IC50 = 53 nM and Ki = 63 nM). Weakly inhibits chymotrypsin (Ki = 1.5 µM) and does not have any significant inhibitory effect on thrombin, factor Xa, factor IXa, plasmin, trypsin, tryptase, proteinase 3, and human leukocyte elastase (IC50 >100 µM).
A potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G [IC50 = 53 nM and Ki = 63 nM]. Weakly inhibits chymotrypsin (Ki = 1.5 µM) and poorly inhibits thrombin, factor Xa, factor IXa, plasmin, trypsin, tryptase, proteinase 3, and human leukocyte elastase (IC50 >100 µM).

Other Notes

Greco, M.N., et al. 2002. J. Am. Chem. Soc.124, 3810.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Classe de stockage

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Stefan J Schunk et al.
Circulation, 144(11), 893-908 (2021-07-02)
Cardiovascular diseases and chronic kidney disease (CKD) are highly prevalent, aggravate each other, and account for substantial mortality. Both conditions are characterized by activation of the innate immune system. The alarmin interleukin-1α (IL-1α) is expressed in a variety of cell
Mira Tohmé et al.
Methods in molecular biology (Clifton, N.J.), 960, 509-515 (2013-01-19)
Proteases generate peptides that bind to MHC class II molecules to interact with a wide diversity of CD4(+) T cells. They are expressed in dedicated organelles: endosomes and lysosomes of professional antigen presenting cells (pAPCs) such as B cells, macrophages
Akmaral Assylbekova et al.
Pharmaceuticals (Basel, Switzerland), 15(5) (2022-05-29)
Coronavirus disease 2019 (COVID-19) can lead to multi-organ failure influenced by comorbidities and age. Binding of the severe acute respiratory syndrome coronavirus 2 spike protein (SARS-CoV-2 S protein) to angiotensin-converting enzyme 2 (ACE2), along with proteolytic digestion of the S
Fabian Gärtner et al.
ACS omega, 5(43), 28233-28238 (2020-11-10)
During an immune response, cathepsin G (CatG) takes on the role of adaptive and innate immunity and the outcome depends on the localization of CatG. Soluble, cell surface-bound, or intracellular CatG is also responsible for pathophysiology conditions. We applied the
Hui Yang et al.
EMBO reports, 24(10), e57032-e57032 (2023-08-31)
Bromodomain-containing protein 4 (BRD4) is overexpressed and functionally implicated in various myeloid malignancies. However, the role of BRD4 in normal hematopoiesis remains largely unknown. Here, utilizing an inducible Brd4 knockout mouse model, we find that deletion of Brd4 (Brd4Δ/Δ )

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