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Merck

529627

PPIase-Parvulin Inhibitor - CAS 64005-90-9 - Calbiochem

The PPIase-Parvulin Inhibitor, also referenced under CAS 64005-90-9, controls the biological activity of PPIase-Parvulin.

Synonim(y):

PPIase-Parvulin Inhibitor - CAS 64005-90-9 - Calbiochem, PiB, Diethyl-1,3,6,8-tetrahydro-1,3,6,8-tetraoxobenzo[lmn][3,8]phenanthroline-2,7-diacetate

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Informacje o tej pozycji

Wzór empiryczny (zapis Hilla):
C22H18N2O8
Numer CAS:
Masa cząsteczkowa:
438.39
UNSPSC Code:
12352200
MDL number:
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Quality Segment

assay

≥95% (NMR)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

brownish

solubility

chloroform: 1 mg/mL, ethanol: 250 μg/mL, cloudy (suspension)

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C22H18N2O8/c1-3-31-15(25)9-23-19(27)11-5-7-13-18-14(8-6-12(17(11)18)20(23)28)22(30)24(21(13)29)10-16(26)32-4-2/h5-8H,3-4,9-10H2,1-2H3

InChI key

WNKQGFNIIHNGQM-UHFFFAOYSA-N

General description

A cell-permeable napthalenetetracarboxylic-bisimide compound that displays anti-proliferative properties (IC50<5 µM against a panel of human cancer cell lines). Causes cell cycle arrest and acts as a potent, selective, reversible, competitive, active site binding inhibitor of Pin1/Par14 PPIase (peptidyl prolyl cis-trans isomerase) activity (IC50 = ~ 1.5 µM). Does not bind to DNA or functions as a topoisomerase I inhibitor.
A cell-permeable, napthalenetetracarboxylic-bismide compound that displays anti-proliferative properties (IC50<5 µM against a panel of human cancer cell lines). Causes cell cycle arrest and acts as a potent, selective, reversible, competitive, active site-binding inhibitor of Pin1/Par14 peptidylprolyl cis-trans isomerase (PPIase) activity (IC50 ~ 1.5 µM). Does not bind to DNA or function as a topoisomerase I inhibitor.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Pin1/Par14 PPIase (peptidyl prolyl cis-trans isomerase) activity
Product competes with ATP.
Reversible: yes
Target IC50: <5 µM for anti-proliferative properties against a panel of human cancer cell lines; ~ 1.5 µM inhibiting Pin1/Par14 PPIase (peptidyl prolyl cis-trans isomerase) activity

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.

Other Notes

Uchida, T., et al. 2003. Chem. Biol.10, 15.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)
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Klasa składowania

10-13 - German Storage Class 10 to 13



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Francesco Napoletano et al.
Cell reports, 36(11), 109694-109694 (2021-09-16)
Chromatin organization plays a crucial role in tissue homeostasis. Heterochromatin relaxation and consequent unscheduled mobilization of transposable elements (TEs) are emerging as key contributors of aging and aging-related pathologies, including Alzheimer's disease (AD) and cancer. However, the mechanisms governing heterochromatin