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

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Showing 291 - 300 of 609 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Hypocrellin B (HB), a natural perylenequinone pigment, has been successfully employed in the photodynamic therapy (PDT) in a variety of human cancer cells due to its high singlet oxygen yield. Hypocrellin B exhibits antibacterial, anti-metastatic, and anticancer chemotherapeutic activities. Hypocrellin B inhibits proliferation of Staphylococcus by increasing ROS levels and damaging cell walls. In ovarian cancer cells, this compound induces apoptosis and inhibits cell migration and adhesion under photodynamic stimulation; it also induces tumor regression in animal models of lymphoma. In vitro, hypocrellin B induces DNA strand breakage.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

NSC-207895 (XI-006) is a derivative of nitrobenzofuroxan and an anticancer agent with an EC50 of 1 μM. NSC-207895 also upregulated the expression of p53 in MCF-7 cells that led to increased expression of proapoptotic genes including PUMA, BAX, as well as PIG3. Notably, NSC-207895, also called a small-molecule p53 activator, gives rise to MCF-7 cells to experience apoptosis and decrease the viability of cancer cells along with nutlin-3a, which dissociated the MDM2-p53 complex. NSC-207895 is an electrophilic compound that has antitumor and mutagenic activities. NSC-207895 may lead to the damage of DNA that inhibits the growth of tumors.
Trihydroxychalcone (Isoliquiritigenin, ISL) is a flavonoid found in licorice root and several other plants that displays antioxidant,anti-inflammatory,and antitumor activities as well as hepatoprotection against steatosis-induced oxidative stress. Trihydroxychalcone is a potent antimetastatic agent, which can markedly inhibit the metastatic and invasive capacity of prostate cancer cells. The inhibition of JNK/AP-1 signaling may be one of the mechanisms by which ISL inhibits cancer cell invasion and migration. Trihydroxychalcone has been shown to be a BACE1 inhibitor, which could ameliorate memory impairment in mice, and is expected to be potentially used as a lead compound for further anti-AD reagent development.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Acacetin is an O-methylated flavone that exhibits anti-inflammatory, anti-nociceptive, neuroprotective, and anti-aromatase properties. It is a naturally occurring plant metabolite which can be found in Robinia pseudoacacia, Turnera diffusa, Betula pendula, and Asplenium normale. Acacetin has been investigated in a number of in-vitro and animal models for various cancers, and neurological disorders including Alzheimer's disease.
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.
Okadaic acid (OA) is a naturally occurring polyether toxin that was originally derived from marine dinoflagellates, Prorocentrium spp.. It is a reversible, potent and selective inhibitor of two serine threonine protein phosphatases: PP2A-C (PP2A) which is inhibited completely at 1 nM and PP1 which is inhibited at higher concentrations (IC50= 10-15 nM). PP2B is much less sensitive to okadaic acid than PP1, while PP2C is not inhibited. This selectivity is the basis for an improved identification and quantification procedure for these enzymes. The hydrophobic backbone of okadaic acid enables it to enter cells where it stimulates intracellular protein phosphorylation. It mimics the effects of insulin, enhances transmitter release at neuromuscular junctions, causes vasodilation and is a very potent tumor promoter. Okadaic acid is an extremely useful tool for studying cellular processes that are regulated by phosphorylation. Okadaic Acid is an activator of PKC.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Patchouli alcohol is a sesquiterpene with tricyclic structure and has been extracted from the whole plant of traditional Chinese medicine Guang-huo-xiang, which is also called Pogostemon cablin(Blanco) Benth. Patchouli alcohol is the nominal ingredient which standing for the typical aromatic odor and also used as the chemical reference for the quality control of P. cablin in Chinese Pharmacopoeia. Patchouli alcohol has exhibited various pharmacological activities, such as protecting against the neurotoxicity of beta-amyloid peptide fragment 25–35 (Aβ25–35), enhancing cognition in memory impairment mice induced by scopolamine, anti-inflammatory activities in RAW 264.7 cells and rats models, anti-influenza virus activities in vitro and in vivo. However, Patchouli alcohol easily evaporates even at room temperature due to its volatile nature, which can cause the bioactivity decrease in the processing and storage. In addition, the development of Patchouli alcohol as medicine is greatly limited due to its low water solubility and poor bioavailability. Patchoulol is also used in the synthesis of the chemotherapy drug Taxol.
Laurotetanine is an alkaloid isolated from the leaves of Peumus boldus and other plants. It was demonstrated that laurotetanine from Beilschmiedia species possess an anti-acetylcholinesterase (AChE), anti-α-glucosidase, anti-leishmanial and anti-fungal activities. Laurotetanine exhibits antiplasmodial activity and good antioxidant activities also. It relaxed the rat thoracic aorta mainly by suppressing the Ca2+ influx through both voltage- and receptor-operated calcium channels. It showed significant anti-tumor metastatic activities.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

2-Fluoroadenosine (F-Ado) was developed at Southern Research Institute in 1957 as a potential anticancer drug. 2-Fluoroadenosine is not deaminated by adenosine deaminase but metabolized to triphosphate as shown in vitro. The drug was also shown to be a potent inhibitor of lymphocyte-mediated cytolysis.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

Pyronin Y is an intercalating dye with a specificity towards RNA. It has been shown to accumulate in the mitochondria of viable cells. Pyronin Y has been used to measure RNA in flow cytometry. Pyronin Y possesses some anti-cancer properties: it causes cell cycle arrest and increases lifespan in a mouse model of sarcoma.

Showing 291 - 300 of 609 results