Oncrasin-1 is a proapoptotic agent that induces abnormal nuclear aggregation of PKCι and suppresses RNA transcription. Exhibits antiproliferative effects against various human tumor cell lines with K-Ras mutations (IC50 ≤ 3 μM) with minimal effects on normal epithelial cells and inhibits human xenograft growth by 75% in vivo. Oncrasin-1 induces aggregation of PKCL in the nuclei and is proapoptotic. oncrasin-1 or its active analogues could be a novel class of anticancer agents, which effectively kill K-Ras mutant cancer cells.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 40 mg/mL|
Analogues and derivatives of oncrasin-1, a novel inhibitor of the C-terminal domain of RNA polymerase II and their antitumor activities.
Wu S, et al. J Med Chem. 2011 Apr 28;54(8):2668-79. PMID: 21443218.
Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1).
Guo W, et al. Mol Cancer Ther. 2009 Feb;8(2):441-8. PMID: 19208825.
Identification of a Small Molecule with Synthetic Lethality for K-Ras and Protein Kinase C Iota.
Guo W, et al. Cancer Res. 2008 Sep 15;68(18):7403-8. PMID: 18794128.
|Related PKC Products|
Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
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.
Ingenol Mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.