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Inhibitor Report for: Propidium

The most common use of propidium is because it is a membrane impermeable DNA intercalator. Has red fluorescence at 488 nm. Has the following spectral properties: extinction coefficient: 5,900 M -1 cm -1 (493 nm); 55,700 M -1 cm -1 (287 nm) 13,800 M -1 cm -1 (252.5 nm); excitation maximum: 536 nm; emission maximum: 617 nm


General
Type Phenanthridinium, Fluorescent Probe
Chemical_Nomenclature 3,8-diamino-5[3-(diethylmethylammonio)propyl]-6-phenylphenanthridinium diiodide
Canonical SMILES CC[N+](C)(CC)CCC[N+]1=C2C=C(C=CC2=C3C=CC(=CC3=C1C4=CC=CC=C4)N)N
InChI InChI=1S/C27H33N4/c1-4-31(3,5-2)17-9-16-30-26-19-22(29)13-15-24(26)23-14-12-21(28)18-25(23)27(30)20-10-7-6-8-11-20/h6-8,10-15,18-19,29H,4-5,9,16-17,28H2,1-3H3/q+1/p+1
InChIKey ZDWVWKDAWBGPDN-UHFFFAOYSA-O
Other name(s) 36015-30-2 ; UNII-74NX23J96Y ; CHEBI:51246 ; 74NX23J96Y ; CHEMBL345124 ; SCHEMBL55279 ; ZINC622264 ; PRM
________________________________________________________________________________________________
MW|668.4
Formula|C27H34N4I2
CAS_number|25535-16-4
PubChem|4939
UniChem|ZDWVWKDAWBGPDN-UHFFFAOYSA-O
IUPHAR|
Wikipedia|Propidium_iodide

Target
Families | Propidium ligand of proteins in family: ACHE, BCHE
Stucture | 2 structures: 6ESJ, 1N5R
Protein | human-BCHE, mouse-ACHE

References:
Search PubMed for references concerning: Propidium

14 more
    Title: Cloning and expression of acetylcholinesterase from Bungarus fasciatus venom. A new type of cooh-terminal domain; involvement of a positively charged residue in the peripheral site
    Cousin X, Bon S, Duval N, Massoulie J, Bon C
    Ref: Journal of Biological Chemistry, 271:15099, 1996 : PubMed

            

    Title: Different effects of two peripheral anionic site-binding ligands on acetylcholinesterase active-site gorge topography revealed by electron paramagnetic resonance
    Grubic Z, Stalc A, Sentjurc M, Pecar S, Gentry MK, Doctor BP
    Ref: Biochimica & Biophysica Acta, 1249:155, 1995 : PubMed

            

    Title: Characterization of monoclonal antibodies that strongly inhibit Electrophorus electricus acetylcholinesterase
    Remy MH, Frobert Y, Grassi J
    Ref: European Journal of Biochemistry, 231:651, 1995 : PubMed

            


bunfa-ACHE
MutationKiKsiIc50SubstrateConditionPaper
K285D 4.6 & 0.8 uM 27.9 & 5.0 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
M70Y 1.6 & 0.0 uM 2.3 & 0.4 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
M70Y/K285D 0.6 & 0.1 uM 1.0 & 0.2 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
WT 46.0 & 3.6 uM 250.0 & 60.0 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099

chick-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT >1000 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335

human-ACHE
MutationKiKsiIc50SubstrateConditionPaper
> Mutations for human-ACHE (29)

mouse-ACHE
MutationKiKsiIc50SubstrateConditionPaper
> Mutations for mouse-ACHE (12)

mouse-BCHE
MutationKiKsiIc50SubstrateConditionPaper
WT 5.3 & 1.8 uM 26 & 18 uM - Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074

torma-ACHE
MutationKiKsiIc50SubstrateConditionPaper
WT 2.8 uM - - Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
WT 2.0 & 0.2 uM 3.6 & 0.4 uM - Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099

WT Kinetics
Kinetic parametersKiKsiIc50SubstrateConditionsPapers
bunfa-ACHE46.0 & 3.6 uM250.0 & 60.0 uM- Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099
chick-ACHE>1000 uM-- Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
human-ACHE0.6 uM0.9 uM- Acetylthiocholine 5 or 50mM Na Phosphate pH8 T27C Ordentlich_1995_J.Biol.Chem_270_2082
human-ACHE1.4 uM-- Acetylthiocholine 50mM Na phosphate pH8 Barak_1994_J.Biol.Chem_269_6296
human-ACHE--1.5 uM Acetylthiocholine pH8 T27C 50mM Na phosphate Shafferman_1992_EMBO.J_11_3561
mouse-ACHE2.2 & 0.7 uM5.3 & 1.8 uM- Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
mouse-BCHE5.3 & 1.8 uM26 & 18 uM- Acetylthiocholine 100mM NaP pH7.0 T22C eq3.gif sch3.gif Radic_1993_Biochemistry_32_12074
torma-ACHE2.8 uM-- Acetylthiocholine 100mM NaCl 50mM Tris pH7.4 Eichler_1994_Mol.Pharmacol_45_335
torma-ACHE2.0 & 0.2 uM3.6 & 0.4 uM- Acetylthiocholine T25C IS 50 mM phosphate Cousin_1996_J.Biol.Chem_271_15099