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

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Showing 621 - 630 of 1679 results

PD168393 is potent, cell-permeable, irreversible and selective inhibitor of EGF receptor (EGFR) tyrosine kinase and ErbB2. PD168393 has an IC50 value of 0.70 nM for EGFR, and is inactive against insulin, PDGFR, FGFR and PKC. PD168393 induced cytostatic responses in preclinical models of non-small cell lung cancer, squamous carcinoma, malignant peripheral nerve sheath tumors. Locally administred PD168393 ameliorated excessive reactive astrogliosis and facilitated a more favorable environment for axonal regeneration in the model of spinal cord injury.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Psoralidin (1) was first isolated from seeds of Psoralea corylifolia Linn. It was found to be an active ingredient of many Indian and Chinese traditional herbal medicines. Psoralidin exhibits a variety of biological activities like antineoplastic, antioxidant, antibacterial, antidepressant activities. Psoralidin inhibits protein tyrosine phosphatase 1B activity. Psoralidin may act as a estrogen receptor agonist. In addition psoralidin showed potent and noncompetitive inhibition against UDP- glucuronosyltransferase (UGT) or cytochrome p450 (CYP450) enzymes.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


L-alloisoleucine (2S, 3R), a diastereomer of L-isoleucine (2S, 3S), is a normal constituent of human plasma. It was shown, that the plasma L-alloisoleucine above the cutoff value of 5 micromol/L is the most specific and most sensitive diagnostic marker for all forms of maple syrup urine disease (MSUD). The precise mechanism of L-alloisoleucine formation is unclear, but existed suggestions, that R-3-methyl-2-oxopentanoate is an immediate and inevitable byproduct of L-isoleucine transamination and that alloisoleucine is primarily formed via transamination of 3-methyl-2-oxopenanoate in vivo.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)



BMS-509744 is a potent interleukin-2 inducible T cell kinase (ITK) inhibitor (IC50 = 19 nM). It displays 200-fold selectivity over Tec family kinases and 55-fold selectivity over other kinases tested. BMS-509744 reduces HIV infection of primary CD4+ T cells and attenuates the establishment of HIV infection in vitro. BMS-509744 also reduces T cell proliferation and IL-2 production in vitro. BMS-509744 reduces TCR-induced functions including PLCgamma1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-509744 suppresses the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma.
BAY 61-3606 is a potent inhibitor of spleen tyrosine kinase (Syk) which is playing essential roles in receptors for Fc portion of immunoglobulins and B cell receptor complex signaling in various inflammatory cells. In addition, BAY61-3606 could inhibit the inhibitor of nuclear factor kappa B kinase (IKK-alpha) kinase activity. The compound is able to inhibit neoplastic phenotype of leukemia cells as well as of colon and breast cancer cells in vitro. BAY 61-3606 also exrets antiinflammatory and antiallergic properties in animal models.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

LDC1267 preferentially inhibits TAM tyrosine kinase receptors Tyro3, Axl and Mer at low nanomolarity. LDC1267 conferred therapeutic potential, efficiently enhancing anti-metastatic natural killer (NK) cells activity. In vivo the compound markedly reduced murine mammary cancer and melanoma metastases dependent on NK cells.