Chelerythrine Chloride - CAS 3895-92-9
Catalog number: 3895-92-9
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H19NO4
Molecular Weight:
383.82
COA:
Inquire
Targets:
PKC
Description:
Chelerythrine is a cell-permeable inhibitor of protein kinase C (IC50 = 660 nM) with a wide range of biological activities.
Purity:
≥98%
Appearance:
Yellow to Orange Solid
Synonyms:
1,2-dimethoxy-12-methyl-[1,3]benzodioxolo[5,6-c]phenanthridin-12-ium;chloride;
Solubility:
Soluble in DMSO
Storage:
Store at 2-8 °C
MSDS:
Inquire
Application:
A cell permeable protein kinase C (PKC) inhibitor.
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Melting Point:
172 - 180 °C
InChIKey:
WEEFNMFMNMASJY-UHFFFAOYSA-M
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
Canonical SMILES:
C[N+]1=C2C(=C3C=CC(=C(C3=C1)OC)OC)C=CC4=CC5=C(C=C42)OCO5.[Cl-]
1.[ATP release mechanism from the supporting cells in the Kölliker organ in vitro in the cochlea of newborn rat].
He Y;Yang J Zhonghua Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2015 Jan;50(1):43-9.
OBJECTIVE: ;The specific mechanism underlying in the Adenosine triphosphate (ATP) release from the Kölliker's organ is still unknown. The present study was designed to investigate whether the supporting cells in the Kölliker organ in vitro release ATP and to explore the mechanism of ATP releasing from these cells.;METHODS: ;Supporting cells in the Kölliker organ from P1 rats were isolated, purified and cultured with a combinatorial approach of enzymatic digestion and mechanical separation. Quinacrine staining was used to observe the cochlear membranous labyrinth and supporting cells. the bioluminescence assay was chosen to explore the release ATP from supporting cells in the Kölliker organ, when the ATP metabolism of the cells was influenced, the intracellular or extracellular Ca(2)+ concentration changed, the hemichannels blocked, and the phospholipase signaling pathways inhibited.;RESULTS: ;There were intensely numerous star-like green spots of quinacrine staining in the cytoplasm of supporting cells. There was a strong log-linear relationship in the ATP standard curve generated by the bioluminescence assay. With increasing concentrations of bafilomycin A1, the ATP concentration in the culture medium of the supporting cells in the Kölliker organ decreased, while with adipic acid didecyl, it increased.
2.Potentiation of NMDA and AMPA responses by the specific mGluR5 agonist CHPG in spinal cord motoneurons.
Ugolini A;Corsi M;Bordi F Neuropharmacology. 1999 Oct;38(10):1569-76.
The specific metabotropic glutamate receptor (mGluR)5 agonist (RS)-2-chloro-5-hydroxyphenylglycine (CHPG) is able to potentiate NMDA and AMPA responses recorded from ventral roots of the isolated hemisected baby rat spinal cord. Previously we have demonstrated that activation of group I mGluRs (mGluR1 and mGluR5) with the broad spectrum mGluR agonist 1S,3R-1-amino-1,3-cyclopentanedicarboxylate (ACPD) produced potentiation of ionotropic glutamate responses. In contrast to ACPD-induced potentiation, however, no evidence for an involvement of protein kinase C (PKC) is found in the CHPG-induced potentiation of both NMDA and AMPA depolarization because the PKC blockers chelerythrine chloride or calphostin C did not antagonize this effect. Moreover, in the absence of Ca2+ in the perfusing medium or depleting intracellular Ca2+ stores with thapsigargin or dantrolene did not modify the CHPG-induced enhancement of NMDA depolarizations. Phorbol-12,13-diacetate (PDA), on the other hand, was able to attenuate this effect, which was reversed by chelerythrine chloride. These results suggest that both mGluR5 and mGluR1 may act to enhance ionotropic glutamate responses but the two types of mGluRs may have different intracellular mechanisms of action.
3.Gender differences in cardioprotection against ischemia/reperfusion injury in adult rat hearts: focus on Akt and protein kinase C signaling.
Bae S;Zhang L J Pharmacol Exp Ther. 2005 Dec;315(3):1125-35. Epub 2005 Aug 11.
Previous studies have reported the sex differences in heart susceptibility to ischemia/reperfusion (I/R) injury, but the mechanisms are not understood. The present study tested the hypothesis that Akt and protein kinase C (PKC)epsilon play an important role in the sexual dimorphism of heart susceptibility to I/R injury. Isolated hearts from 2-month-old male and female rats were subjected to I/R in the Langendorff preparation. The postischemic recovery of left ventricular function was significantly better, and infarct size was significantly smaller in female (37.1 +/- 1.9%) than in male (48.3 +/- 2.3%) hearts after 25-min ischemia followed by 2-h reperfusion. Inhibition of phosphatidylinositol 3-kinase/Akt pathway by wortmannin or PKC by chelerythrine chloride before ischemia significantly reduced postischemic recovery and increased infarct size in female but not male hearts. There were no differences in myocardial protein levels of heat shock protein 70, Akt, and PKCepsilon, respectively, between male and female rats. However, the ratio of phosphorylated (p)-Akt/Akt (0.58 +/- 0.05 versus 0.22 +/- 0.04; P < 0.05) and p-PKCepsilon/PKCepsilon (0.35 +/- 0.03 versus 0.22 +/- 0.02; P < 0.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related PKC Products


CAS 102649-78-5 SC-9

SC-9
(CAS: 102649-78-5)

SC-9 is a potent activator of protein kinase C in the presence of Ca2+.

CAS 137592-45-1 Bisindolylmaleimide II

Bisindolylmaleimide II
(CAS: 137592-45-1)

Bisindolylmaleimide II is a potent and ATP-competitive inhibitor of protein kinase C (PKC) (IC50 = 0.01 μM). It also displays an antagonistic effect on nicotini...

CAS 37558-16-0 Phorbol 12,13-dibutyrate

Phorbol 12,13-dibutyrate
(CAS: 37558-16-0)

Phorbol 12,13-dibutyrate, a protein kinase C activator, stimulates the phosphorylation of Na+,K+- ATPase, thereby inhibiting its activity.

CAS 151342-35-7 Ro 32-0432 hydrochloride

Ro 32-0432 hydrochloride
(CAS: 151342-35-7)

Ro 32-0432 hydrochloride is a selective and orally active inhibitor of PKC displaying a 10-fold greater selectivity for PKC-&alpha (IC50 = 9.3 nM); and a 4-fold...

CAS 192050-59-2 LY 333531 mesylate

LY 333531 mesylate
(CAS: 192050-59-2)

LY 333531 mesylate is an orally-available protein kinase C β (PKC-β) specific inhibitor used for the treatment of diabetic nephropathy and diabetic macular edem...

CAS 169939-94-0 Ruboxistaurin

Ruboxistaurin
(CAS: 169939-94-0)

Ruboxistaurin, also called as LY 333531, initially developed for the treatment of diabetic retinopathy, inhibits isolated enzymes PKCβI and PKCβII with a half-m...

CAS 30220-46-3 Ingenol

Ingenol
(CAS: 30220-46-3)

Ingenol, the analogue of Ingenol 3-Angelate found in the seeds of Euphorbia lathyris L, is an extremely weak PKC (protein kinase C) activator ( Ki=30 μM, ED50=2...

CAS 1874276-76-2 LXS196

LXS196
(CAS: 1874276-76-2)

LXS196 is a potent and orally active protein kinase C (PKC) inhibitor under clinical trials for the treatment of uveal melanoma, the most common cancer of the e...

Chemical Structure

CAS 3895-92-9 Chelerythrine Chloride

Quick Inquiry

Verification code

Featured Items