8 products were found matching "Cay16261"!

The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations...

Apoptosis signal-regulating kinase 1 (ASK1) is the ubiquitously expressed mitogen-activated protein kinase kinase kinase 5 involved in a wide range of biological functions that are dependent on cell survival or death. NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 µM, Ki = 500 nM) that demonstrates potent...

NMDA receptors are neuroreceptors that have binding sites for glycine or D-serine as well as L-glutamate. MDL 29951 is an antagonist of NMDA receptors with high affinity for the glycine binding site (Ki = 140 nM). It is functional both in vitro and in vivo. MDL 29951 blocks NMDA receptor-dependent convulsions in...

While class I HDACs are localized predominantly within the nucleus, class II HDACs shuttle into and out of the nucleus in response to intracellular signaling. Class IIa HDACs, which includes HDAC4, 5, 7, and 9, commonly act as corepressors and play diverse roles in cell biology. MC 1568 is a selective inhibitor of...

ONX 0912 is an orally bioavailable proteasome inhibitor. It potently targets the chymotrypsin-like activity of the 20S proteasome subunits beta5 and LMP7 (IC50s = 36 and 82 nM, respectively). ONX 0912 inhibits the growth of multiple myeloma cells at nanomolar concentrations while not decreasing the viability of...

LDE225 is a smoothened (Smo) antagonist (IC50s = 1.3 and 2.5 nM for mouse and human Smo, respectively). In vivo, LDE225 (20 mg/kg per day) inhibits Gli1 mRNA expression and prevents tumor growth in an orthotopic Ptch+/- p53-/- medulloblastoma mouse allograft model. Formulations containing LDE225 have been used in...

LY2940680 is a smoothened (Smo) antagonist. It inhibits [35S]GTPgammaS binding in CHO cells expressing wild-type Smo (IC50 = 294 nM) and reduces production of GLI1 mRNA induced by sonic hedgehog (Shh) in Daoy cells (IC50 = 5.49 nM). Topical application of LY2940680 (2% w/v) decreases skin GLI1 and PTCH1 mRNA...

Dolastatin 10 is a natural antimitotic and antineoplastic agent that binds to tubulin and inhibits tubulin polymerization. Monomethyl Auristatin E (MMAE) is a synthetic analog of dolastatin 10 that similarly inhibits tubulin polymerization and exhibits potent cytotoxicity. It is commonly conjugated with monoclonal...