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Oncrasin-1

CAS No. : 75629-57-1

Biological Activity：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.
IC50 value: 1.0 μM(A549, K-ras 12H and p53 Wt) [1]
Target: human lung cancer cells with K-Ras mutation; K-Ras/PKCiota pathway inhibitor
in vitro: effectively kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. The cytotoxic effects correlated with apoptosis inductionas was evidenced by increase of apoptotic cells and activation of caspase-3 and caspase-8 upon the treatment of oncrasin-1 in sensitive cells.
Treatment with oncrasin-1 also led to abnormal aggregation
of PKCι in nucleus of sensitive cells but not in resistant cells. Furthermore, oncrasin-1 induced apoptosis was blocked by siRNA of K-Ras or PKCι suggesting that oncrasin-1 is targeted to a novel K-Ras/PKCι pathway [1]. 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 [2].
in vivo: The in vivo administration of oncrasin-1 suppressed the growth of K-ras mutant human lung tumor xenografts by >70% and prolonged the survival of nude mice bearing these tumors, without causing detectable toxicity [1].

Research Area：Cancer

Targets：Apoptosis|Ras

Related Screening Libraries:Covalent Screening Library Plus;Bioactive Compound Library Plus;Apoptosis Compound Library;GPCR/G Protein Compound Library;Kinase Inhibitor Library;Anti-Cancer Compound Library;Covalent Screening Library;Ferroptosis Compound Library;Glutamine Metabolism Compound Library;Anti-Lung Cancer Compound Library;Anti-Pancreatic Cancer Compound Library;Anti-Blood Cancer Compound Library;Angiogenesis-Related Compound Library;Anti-Liver Cancer Compound Library ;Anti-Colorectal Cancer Compound Library ;

Related Small Molecules:Physalin A;Bomedemstat ditosylate;Enpp/Carbonic anhydrase-IN-1;GK563;Calpeptin;Lobetyolin;BJE6-106;Dinaciclib;Ecteinascidin 770;MDM2-p53-IN-15;AT9283;Staurosporine;SNS-032;C188-9;ZLDI-8;Topoisomerase I/II inhibitor 3;Xevinapant;Mangiferin;Cambinol;Antioxidant agent-5;Apoptosis inducer 9;Bafetinib;Cyclovirobuxine D;STAT3-IN-10;Rigosertib sodium

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