Oncrasin 1

Proapoptotic agent CAS# 75629-57-1

Oncrasin 1

Catalog No. BCC2390----Order now to get a substantial discount!

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Chemical structure

Oncrasin 1

3D structure

Chemical Properties of Oncrasin 1

Cas No. 75629-57-1 SDF Download SDF
PubChem ID 872445 Appearance Powder
Formula C16H12CINO M.Wt 373.2
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 43 mg/mL (159.42 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 1-[(4-chlorophenyl)methyl]indole-3-carbaldehyde
SMILES C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C=O
Standard InChIKey ZDRQMXCSSAPUMM-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H12ClNO/c17-14-7-5-12(6-8-14)9-18-10-13(11-19)15-3-1-2-4-16(15)18/h1-8,10-11H,9H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Oncrasin 1

DescriptionProapoptotic 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 Dilution Calculator

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Oncrasin 1 Molarity Calculator

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Preparing Stock Solutions of Oncrasin 1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6795 mL 13.3976 mL 26.7953 mL 53.5906 mL 66.9882 mL
5 mM 0.5359 mL 2.6795 mL 5.3591 mL 10.7181 mL 13.3976 mL
10 mM 0.268 mL 1.3398 mL 2.6795 mL 5.3591 mL 6.6988 mL
50 mM 0.0536 mL 0.268 mL 0.5359 mL 1.0718 mL 1.3398 mL
100 mM 0.0268 mL 0.134 mL 0.268 mL 0.5359 mL 0.6699 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Oncrasin 1

Oncrasin 1 is a small molecule antitumor agent with IC50 value of 4.81 μM [1].
The activated mutations of Ras genes (K-Ras, N-Ras and H-Ras) play important roles in tumorigenesis and maintenance of malignant phenotypes. The mutations make Ras constitutively be in the activated state with GTP-bound. Among the three Ras genes, the mutations of K-Ras are the most frequently found in tumors and are associated with resistance to radio therapy, chemotherapy and poor prognosis. Thus, mutant K-Ras is important target for antitumor treatment. Oncrasin 1 is a small-molecule compound that found by a synthetic lethality screening. It effectively killed tumor cells with K-Ras mutation but not normal isogenic cells through inducing cell apoptosis. Besides that, Oncrasin 1 caused abnormal aggregation of PKCι of those sensitive cells [1].
In a sulforhodamine B (SRB) assay, treatment of Oncrasin 1 at final concentration of 5 μg/ml killed more than 50% of cells. Oncrasin 1 was highly selective against K-Ras mutation, it showed dose-dependent cytotoxicity in T29Kt1 (K-Ras mutant) cells with IC50 value of 4.81 μM. For T29Ht1 (H-Ras mutant) cells and T29 (wild-type Ras) cells, Oncrasin 1 showed no cytotoxicity even at concentration of 33 μM. For the other K-Ras-mutant tumor cells such as A549, H2122 and H460, Oncrasin 1 all showed cytotoxicity with IC50 value of ≤ 3 μM. It was found that induction of apoptosis was a major mechanism of Oncrasin 1 treatment [1].
In mice injected with H460 cells, administration of Oncrasin 1 at dose of 100 mg/kg resulted in significant tumor growth suppression by 75.4%. In addition, the survival time was prolonged by the Oncrasin 1 treatment [1].
Reference:
[1] Guo W, Wu S, Liu J, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer research, 2008, 68(18): 7403-7408.

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References on Oncrasin 1

Analogues and derivatives of oncrasin-1, a novel inhibitor of the C-terminal domain of RNA polymerase II and their antitumor activities.[Pubmed:21443218]

J Med Chem. 2011 Apr 28;54(8):2668-79.

To optimize the antitumor activity of oncrasin-1, a small molecule RNA polymerase II inhibitor, we evaluated 69 oncrasin-1 analogues for their cytotoxic activity against normal human epithelial cells and K-Ras mutant tumor cells. About 40 of those compounds were as potent as or more potent than oncrasin-1 in tumor cells and had a minimal cytotoxic effect on normal cells. Structure-activity relationship analysis revealed that most of the active compounds contained either a hydroxymethyl group or an aldehyde group as a substitute at the 3-position of the indole. Both electron-donating and electron-withdrawing groups in the benzene ring were well tolerated. The hydroxymethyl compounds ranged from equipotent with to 100 times as potent as the corresponding aldehyde compounds. We tested three active analogues' effect on RNA polymerase phosphorylation and found that they all inhibited phosphorylation of the C-terminal domain of RNA polymerase II, suggesting that the active compounds might act through the same mechanisms as oncrasin-1.

Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1).[Pubmed:19208825]

Mol Cancer Ther. 2009 Feb;8(2):441-8.

Protein kinase Ciota (PKCiota) is activated by oncogenic Ras proteins and is required for K-Ras-induced transformation and colonic carcinogenesis in vivo. However, the role of PKCiota in signal transduction and oncogenesis is not clear. We recently identified a small molecule, designated 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1), that can selectively kill K-Ras mutant cancer cells and induce abnormal nuclear aggregation of PKCiota in sensitive cells but not in resistant cells. To determine the causes and biological consequences of PKCiota aggregates in the nucleus, we analyzed the effect of oncrasin-1 on proteins involved in DNA repair and RNA processing. Our results showed that oncrasin-1 treatment led to coaggregation of PKCiota and splicing factors into megaspliceosomes but had no obvious effects on the DNA repair molecule Rad51. Moreover, oncrasin-1 treatment suppressed the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells but not in resistant cells, suggesting that suppression of RNA transcription is a major effect of oncrasin-1 treatment. Studies with cultured cells or with recombinant proteins showed that oncrasin-1 can disrupt the interaction of PKCiota and cyclin-dependent protein kinase 9/cyclin T1 complex, which is known to phosphorylate the largest subunit of RNA polymerase II and is required for RNA transcription. Together, our results suggest that oncrasin-1 suppresses the function of RNA processing machinery and that PKCiota might be involved in the biological function of RNA processing complexes.

Description

Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.

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