220285

Chelerythrine Chloride

Naturally-occurring alkaloid.

• Synonyme(s) : Chelerythrine Chloride
• Formule empirique (notation de Hill): C₂₁H₁₈ClNO₄
• Numéro CAS: 3895-92-9
• Poids moléculaire : 383.82
• Numéro MDL: MFCD00060717
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥97% (HPLC)
• Forme: solid
• Puissance: 660 nM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: light yellow to yellow
• Solubilité: water: 1 mg/mL; DMSO: 10 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: −20°C
• InChI: 1S/C21H18NO4.ClH/c1-22-10-16-13(6-7-17(23-2)21(16)24-3)14-5-4-12-8-18-19(26-11-25-18)9-15(12)20(14)22;/h4-10H,11H2,1-3H3;1H/q+1;/p-1
• Clé InChI: WEEFNMFMNMASJY-UHFFFAOYSA-M

Description

Description générale

Naturally occurring alkaloid. Cell-permeable, selective inhibitor of protein kinase C (IC₅₀ = 660 nM). Acts on the catalytic domain irrespective of the attachment of the regulatory domain. Material is a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.

Naturally-occurring alkaloid. Potent, selective, and cell-permeable inhibitor of protein kinase C (IC₅₀ = 660 nM). Acts on the catalytic domain of PKC. A competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Avertissement

Toxicity: Harmful (C)

Notes préparatoires

Heating to 40-50°C with gentle agitation may be necessary to achieve complete solubilization. Further dilute with buffer just prior to use.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Autres remarques

Kandasamy, R.A., et al. 1995. J. Biol. Chem.270 29209.
Jarvis, W.D., et al. 1994. Cancer Res.54, 1707.
Barg, J., et al. 1992. J. Neurochem.59, 1145.
Herbert, J.M., et al. 1990. Biochem. Biophys. Res. Commun.172, 993.
Ko, F., et al. 1990. Biochim. Biophys. Acta1052, 360.
Walterova, D., et al. J. Med. Chem.24, 1100.

Informations légales

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

Informations sur la sécurité

• Pictogrammes: GHS07
• Mention d'avertissement: Warning
• Mentions de danger: H302 + H312 + H332,H315,H319,H335
• Conseils de prudence: P261 - P280 - P301 + P312 - P302 + P352 + P312 - P304 + P340 + P312 - P305 + P351 + P338
• Classification des risques: Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organes cibles: Respiratory system
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable