Results for Activators & Inhibitors ( 70846 )
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PK14105 (Legacy Tebubio ref. 282T16547). PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit receptor ligands, calcium channel ligands, and co-transporters in all salivary glands.
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Ambrisentan (Legacy Tebubio ref. 282T1655). Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury.
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PKR-IN-C16 (Legacy Tebubio ref. 282T16550). PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.
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Pladienolide B (Legacy Tebubio ref. 282T16551). Pladienolide B is a potent spliceosome inhibitor, a macrolide isolated from Streptomyces obtusususus Mer-12, which targets the SF3B1 subunit of the spliceosome.Pladienolide B exerts its antitumor effects by inhibiting pre-mRNA splicing and inducing necrosis.Pladienolide B possesses antitumor activity and can be used to study leukemia and lymphoid tumors. Pladienolide B has antitumor activity and can be used to study leukemia and lymphoid tumors.