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.

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₂H₁₈N₂O₈
• CAS Number: 64005-90-9
• Molecular Weight: 438.39
• MDL number: MFCD00333607
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 10-13 - German Storage Class 10 to 13