CHELERYTHRINE CHLORIDE Property

Melting point:

195-205 °C

storage temp. 

Inert atmosphere,Store in freezer, under -20°C

solubility 

DMSO: ≥10 mg/mL

form 

powder

color 

yellow to orange

Stability:

Hygroscopic

InChIKey

WEEFNMFMNMASJY-UHFFFAOYSA-M

Safety

Hazard Codes 

Xn,Xi

Risk Statements 

20/21/22-36/37/38-36/37

Safety Statements 

26-36-36/37

RIDADR 

UN 1544PSN1 6.1 / PGII

WGK Germany 

3

RTECS 

FL9200000

HS Code 

29349990

Toxicity

mouse,LD50,intravenous,18500ug/kg (18.5mg/kg),Planta Medica. Vol. 43, Pg. 161, 1981.

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

CHELERYTHRINE CHLORIDE Chemical Properties,Usage,Production

Description

Chelerythrine is a potent, cell permeable inhibitor of protein kinase C (IC₅₀ = 660 nM) that does not inhibit tyrosine protein kinases, cAMP-dependent protein kinase, or calcium/calmodulin-dependent protein kinase. Chelerythrine also inhibits Bcl-xL function (IC₅₀ = 1.5 μM) by displacing Bax binding, inducing apoptosis in several cancer cell lines. Chelerythrine can also have PKC-independent effects, activate p38 MAP kinase and JUNK signaling pathways, and induce apoptosis in cancer cells both in vitro and in vivo.

Chemical Properties

yellow to orange solid

Uses

Chelerythrine Chloride is a cell permeable protein kinase C (PKC) inhibitor.

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.

Biochem/physiol Actions

Cell permeable: yes

storage

-20°C (desiccate)

References

1. j. m. herbert, j. m. augereau, j. gleye and j. p. maffrand, biochem biophys res commun 1990, 172, 993-999. 2. w. d. jarvis, a. j. turner, l. f. povirk, r. s. traylor and s. grant, cancer res 1994, 54, 1707-1714. 3. j. vrba, p. dolezel, j. vicar, m. modriansky and j. ulrichova, toxicol in vitro 2008, 22, 1008-1017. 4. m. vogler, k. weber, d. dinsdale, i. schmitz, k. schulze-osthoff, m. j. dyer and g. m. cohen, cell death differ 2009, 16, 1030-1039. 5. r. yu, s. mandlekar, t. h. tan and a. n. kong, j biol chem 2000, 275, 9612-9619. 6. s. yamamoto, k. seta, c. morisco, s. f. vatner and j. sadoshima, j mol cell cardiol 2001, 33, 1829-1848.