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

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Showing 221 - 230 of 609 results

IMD-0354 is an inhibitor of IκB kinase-β (IKKβ) that blocks NF-κB nuclear translocation. Attenuates myocardial ischemia/reperfusion injury by decreasing expression of adhesion molecules ICAM-1 and P-selectin and inhibiting cytokine and chemokine production in cardiomyocytes. Induces G0/G1 cell cycle arrest and apoptosis in HMC-1 and breast cancer cells. IMD-0354 had been in phase I clinical trials for the treatment of atopic dermatitis.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Asparanin B is a steroidal saponin from the roots of Asparagus racemosus. It has being shown to exhibit significant anticancer activity in both in vitro and in vivo experimental models.
Lobelanidine is one of lobelia alkaloids that are the constituents of Lobelia inflata. Lobelia Chinensis Lour. (L. chinensis) is a plant of the Campanulaceae family that is commonly known as "xi-mi-cao", and "she-she-cao". It has been widely used as an antidote, diuretic, and hemostat in traditional Chinese medicine for decades. Lobelanidine is known for its emetic and anticancer activity.
(-)-Gallocatechin gallate is a polyphenol, which occurs naturally in various plants, including green tea leaves. The compound was shown to have anti-cancer activity in vitro, with breast cancer, lung cancer, and colon cancer cells. It is supposed that the drug may act by inhibiting Bcl family of proteins. It has been reported to inhibit HIV-1 replication by targeting several steps in HIV-1 life cycle. (-)-Gallocatechin gallate (in combination with other catechins) caused the hypocholesterolemic effect in rats.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

5-Amino-1,3,4-thiadiazole-2-thiol is a thiadiazole derivative with antibacterial activity used in the preparation of herbicides as well as carbonic anhydrase inhibitors.
Olomoucine acts as a competitive inhibitor of ATP in cyclin-dependent kinase 1/2/5, and mitogen-activated protein kinase 1. Olomoucine is an anti-mitotic compound that induces cell death preferentially in cancer cell lines, but also at a slower rate in non-cancer cells. It has been studied pre-clinically in a number of cancer models but has not been reported in any human trials. Olomoucine has also seen some preliminary investigation in mouse models of Herpes Simplex Viral Encephalitis.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Cupric selenide (Cu2S) is a semiconductor, which is able to form nanocrystals. The nanocrystals were shown to be an effective photothermal material for the photothermal therapy application in cancer. In vitro photothermal heating of Cu2-xSe nanocrystals in the presence of human colorectal cancer cell (HCT-116) led to cell destruction after 5 min of laser irradiation at 33 W/cm2
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

N-(4-((1,2,4)TRIAZOLO(1,5-A)PYRIDIN-7-YLOXY)-3-METHYLPHENYL)-6-(5-(((2-(METHYLSULFONYL)ETHYL)AMINO)METHYL)FURAN-2-YL)QUINAZOLIN-4-AMINE is an inhibitor of ErbB family of tyrosine kinases which was developed by Array Biopharma for the treatment of hyperproliferative diseases (cancer). The compound is marketed as Arry-380 analog, and should not be confused with Arry-380 (Tucatinib), which has a different, albeit largely similar structure.
(-)-Sesamin is a lignan present in sesam oil and a number of medicinal plants. It exerts various pharmacological effects, such as prevention of hyperlipidemia, hypertension, and carcinogenesis. Moreover, (-)-sesamin has chemopreventive and anticancer activity in vitro and in vivo. (-)-Sesamin is an inhibitor of human mitochondrial Lon protease and DNA damage agents to activate the DNA damage checkpoints as well induce apoptosis in NSCLC cells. (-)-Sesamin is an antioxidant, showing effective 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



AM-966 is a potent antagonist of LPA(1) receptors, with selectivity for this receptor over the other LPA receptors. In vitro, AM-966 inhibited LPA-stimulated intracellular calcium release (IC(50)= 17 nM) from Chinese hamster ovary cells stably expressing human LPA(1) receptors and inhibited LPA-induced chemotaxis (IC(50)= 181 nM) of human IMR-90 lung fibroblasts expressing LPA(1) receptors. AM-966 demonstrated a good pharmacokinetic profile following oral dosing in mice. In the mouse, AM-966 reduced lung injury, vascular leakage, inflammation and fibrosis at multiple time points following intratracheal bleomycin instillation. AM-966 also decreased lactate dehydrogenase activity and tissue inhibitor of metalloproteinase-1, transforming growth factor beta1, hyaluronan and matrix metalloproteinase-7, in bronchoalveolar lavage fluid. AM-966 as a potent, selective, orally bioavailable LPA(1) receptor antagonist that may be beneficial in treating lung injury and fibrosis, as well as other diseases that are characterized by pathological inflammation, oedema and fibrosis.

Showing 221 - 230 of 609 results