220285

Chelerythrine Chloride

Naturally-occurring alkaloid.

• Sinonimo/i: Chelerythrine Chloride
• Formula empirica (notazione di Hill): C₂₁H₁₈ClNO₄
• Numero CAS: 3895-92-9
• Peso molecolare: 383.82
• Numero MDL: MFCD00060717
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Descrizione: Merck USA index - 14, 2051
• Livello qualitativo: 100
• Saggio: ≥97% (HPLC)
• Stato: solid
• Potenza: 660 nM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: light yellow to yellow
• Solubilità: water: 1 mg/mL; DMSO: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C
• Stringa SMILE: [Cl-].[n+]1(c2c(c5c(c1)c(c(cc5)OC)OC)ccc3c2cc4c(c3)OCO4)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; WEEFNMFMNMASJY-UHFFFAOYSA-M

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
PKC

Product does not compete with ATP.

Reversible: no

Attenzione

Toxicity: Harmful (C)

Nota sulla preparazione

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

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Pittogrammi: GHS07
• Avvertenze: Warning
• Indicazioni di pericolo: H302 + H312 + H332,H315,H319,H335
• Consigli di prudenza: P261 - P280 - P301 + P312 - P302 + P352 + P312 - P304 + P340 + P312 - P305 + P351 + P338
• Classi di pericolo: Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organi bersaglio: Respiratory system
• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable