Chelerythrine has a wide range of biological activities, including antiplatelet, anti-inflammatory, antibacterial and antitumor effects. Activates MAPK pathways, independent of PKC inhibition. Inhibits binding of BclXL to Bak (IC50 = 1.5 μM) or Bad proteins and stimulates apoptosis.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||≥ 3.9 mg/mL in DMSO|
Chelerythrine inhibits the sarco/endoplasmic reticulum Ca(2+)-ATPase and results in cell Ca(2+) imbalance.
Vieira SM, et al. Arch Biochem Biophys. 2015 Mar 15;570:58-65. PMID: 25721495.
Recognition of chelerythrine to human telomeric DNA and RNA G-quadruplexes.
Bai LP, et al. Sci Rep. 2014 Oct 24;4:6767. PMID: 25341562.
|Related PKC Products|
Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor, it could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
VTX-27 is a novel potent and selective PKCθ inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
PKCβ inhibitor is a potent and selective inhibitor of PKCβ isozymes (IC50 = 5 nM and 21 nM for human PKCβII and βI).
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
|Zoledronic acid monohydrate
Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
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