U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 541 - 550 of 609 results

Chelerythrine is a kind of benzo[c] phenanthridine alkaloids, which is widely found in plant of Fumariaceae, Papaveraceae, Ranunculaceae and Rutaceae families. Chelerythrine is a potent and specific inhibitor of protein kinase C. In addition chelerythrine inhibits pro-survival protein Bcl(XL) thereby inducing apoptosis. It exerts antitumor properties.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Piperic Acid is a metabolite of Piperine. Piperic acid is found in herbs and spices. Piperic acid is obtained from black pepper (Piper nigrum), from Minthostachys verticillata, peppermint (Mentha piperita) and others. Piperic acid is an intermediate in the synthesis of other compounds such as piperonal, and as-such may be used to produce fragrances, perfumes flavorants and drugs as well as other useful compounds. The cytotoxic effects of piperic acid in prostate cancer cells (PC-3) and breast cancer cells (MDA-MB-231) were studied. The drug treatment experiments clearly indicated that maximum cytotoxicity was achieved at 48 hours and at 100uM concentration of piperic acid in both the cell lines. It is proposed that piperine might get metabolized into piperonylic acid, piperic acid, and piperonal in human as evidenced in rats. Hence, the three derivatives of piperine presented above shall be of therapeutic significance. Piperic Acid has revealed Lipoxygenase (LOX) inhibitory activity. The possibility of exploiting the higher LOX inhibitory activity and lower IC50 values of piperine derivatives, piperonal, and piperonylic acid, in various ways for therapeutic applications, especially with fermented herbal drugs containing materials with piperine as a constituent has being suggested.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Piperic Acid is a metabolite of Piperine. Piperic acid is found in herbs and spices. Piperic acid is obtained from black pepper (Piper nigrum), from Minthostachys verticillata, peppermint (Mentha piperita) and others. Piperic acid is an intermediate in the synthesis of other compounds such as piperonal, and as-such may be used to produce fragrances, perfumes flavorants and drugs as well as other useful compounds. The cytotoxic effects of piperic acid in prostate cancer cells (PC-3) and breast cancer cells (MDA-MB-231) were studied. The drug treatment experiments clearly indicated that maximum cytotoxicity was achieved at 48 hours and at 100uM concentration of piperic acid in both the cell lines. It is proposed that piperine might get metabolized into piperonylic acid, piperic acid, and piperonal in human as evidenced in rats. Hence, the three derivatives of piperine presented above shall be of therapeutic significance. Piperic Acid has revealed Lipoxygenase (LOX) inhibitory activity. The possibility of exploiting the higher LOX inhibitory activity and lower IC50 values of piperine derivatives, piperonal, and piperonylic acid, in various ways for therapeutic applications, especially with fermented herbal drugs containing materials with piperine as a constituent has being suggested.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bisbenzimide ethoxide is a fluorescent nucleic acid stain useful for DNA labeling in fluorescence microscopy and flow cytometry. It appears to bind to AT-rich regions containing at least four such basepairs. Bisbenzimide ethoxide seems to bind relatively poorly to nucleotide sequences containing the alternating step TpA. Bisbenzimide ethoxide induced apoptosis in the HL-60 cells in a time- and dose-dependent manner. Endogenous nuclear topoisomerase I activity in HL-60 cells was inhibited by treatment with Bisbenzimide ethoxide.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Harmaline is a fluorescent psychoactive indole alkaloid from the group of harmala alkaloids and beta-carbolines. It is a partially hydrogenated form of harmine. Harmaline is produced by various plants including Peganum harmala aswell as Banisteriopsis caapi. Harmaline has been investigated as an anti-cancer agent and for the treatment of dementia in rats. However, Harmaline is known to induce tremors in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Harmaline is a fluorescent psychoactive indole alkaloid from the group of harmala alkaloids and beta-carbolines. It is a partially hydrogenated form of harmine. Harmaline is produced by various plants including Peganum harmala aswell as Banisteriopsis caapi. Harmaline has been investigated as an anti-cancer agent and for the treatment of dementia in rats. However, Harmaline is known to induce tremors in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Jervine (11-Ketocyclopamine) is a naturally occuring steroidal alkaloid is derived from the Veratrum plant species. Jervine is a teratogen implicated in birth defects when consumed by animals during a certain period of their gestation. Over the Hedgehog signaling pathway Jervine effectively inhibit the tumor growth using three human tumor xenograft models including lung cancer, pancreatic cancer and basal cell carcinoma. Jervine has the potential to advance to a treatment for different tumors.
Staurosporine is an alkaloid isolated from the culture broth of Streptomyces staurosporesa. It exerts antimicrobial, hypotensive, and cytotoxic activity. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity, though with little selectivity. It is a potent, cell permeable protein kinase C inhibitor with an IC50 of 0.7 nM. At higher concentration (1-20 nM), staurosporine also inhibits other kinases such as PKA, PKG, CAMKII and Myosin light chain kinase (MLCK). At 50-100 nM, it is a functional neurotrophin agonist, promoting neurite outgrowth in neuroblastoma, pheochromocytoma and brain primary neuronal cultures. At 0.2- 1 uM, staurosporine induces cell apoptosis. Staurosporine is also a potent GSK-3β inhibitor with a reported IC50 value of 15 nM. In research, staurosporine is used to induce apoptosis. It has been found that one way in which staurosporine induces apoptosis is by activating caspase-3. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The interest in these activities resulted in a large investigative effort in chemistry and biology and the discovery of the potential for anti-cancer treatment. Staurosporine induces apoptosis by multiple pathways and that the inhibition of more than one kinase is responsible for its potent activity. Because the mechanism of action of staurosporine is distinct from traditional anticancer drugs, this may warrant further preclinical evaluations of the antitumor potential of new staurosporine derivatives either alone or in combination with death ligands or conventional chemotherapeutic drugs.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Anisomycin (2-p-methoxyphenylmethyl-3-acetoxy-4-hydroxypyrrolidine) is an antibiotic isolated from cultures of various Streptomyces. Anisomycin is a potent, structurally specific, and reversible inhibitor of protein biosynthesis in certain yeast and mammalian cells. The inhibition occurs subsequent to the formation of aminoacyl transfer ribonucleic acid but prior to the release of polypeptides from the polyribosome. Anisomycin has unspecified effects that can produce temporary amnesia for a reactivated memory and they also could be responsible for any permanent effects that anisomycin produces. Anisomycin is known to cause apoptosis by activation of MAPK cascade.

Showing 541 - 550 of 609 results