220285

Chelerythrine Chloride

Naturally-occurring alkaloid.

• Synonim(y): Chelerythrine Chloride
• Wzór empiryczny (zapis Hilla): C₂₁H₁₈ClNO₄
• Numer CAS: 3895-92-9
• Masa cząsteczkowa: 383.82
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD00060717
• Assay: ≥97% (HPLC)
• Form: solid
• Storage condition: OK to freeze

Właściwości

• description: Merck USA index - 14, 2051
• Quality Segment: 100
• assay: ≥97% (HPLC)
• form: solid
• potency: 660 nM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: light yellow to yellow
• solubility: water: 1 mg/mL, DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• SMILES string: [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
• InChI key: WEEFNMFMNMASJY-UHFFFAOYSA-M

Opis

General description

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.

Biochem/physiol Actions

Product does not compete with ATP.

Reversible: no

Primary Target
PKC

Cell permeable: yes

Preparation Note

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

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

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Harmful (C)

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Informacja o środkach bezpieczeństwa

• Piktogramy: GHS07
• Słowo ostrzegawcze: Warning
• Kody zagrożeń: H302 + H312 + H332,H315,H319,H335
• Ostrzeżenia: P261 - P280 - P301 + P312 - P302 + P352 + P312 - P304 + P340 + P312 - P305 + P351 + P338
• Hazard Classifications: Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Narządy docelowe: Respiratory system
• Klasa składowania: 11 - Combustible Solids
• Co się dzieje?: WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable