Activators & Inhibitors

Activity: γ-secretase inhibitor . Function/Pharmacology: Inhibitor of γ-secretase (IC50 in human primary neurons = 115 nM for total Aβ or 200 nM for Aβ42 specifically)1. Oral administration of DAPT has been shown to reduce levels of Aβ in brain extract, cerebrospinal fluid and plasma from mice and rats.2,3 DAPT blocks Notch signaling which promotes neuronal differentiation of precur-sor cells.4 Enhances iPS cells without oncogenes KLF4 and CMYC5. Cell permeable. Chemical Name: N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester

Activity: ALK2 / ALK3 inhibitor . Function/Pharmacology: LDN-193189 HCl is a potent and selective inhibitor of ALK2 (IC50 = 5 nM) and ALK3 (IC50 = 30 nM), thereby inhibiting SMAD1/5/8 phosphorylation.1 Only weak inhibition of ALK4, ALK5, and ALK7 is observed. Promotes neuronal differentiation of human pluripotent stem cells.2-3 LDN-193189 HCl has also been used to examine the role of osteogenesis in prostate tumor metastases in bone.4 Chemical Name: 4-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline hydrochloride

Roxadustat (FG-4592) is an orally bioavailable, hypoxia-inducible factor prolyl hydroxylase inhibitor (HIF-PHI), with potential anti-anemic activity.

Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.

Pseudouridine is the most abundant modified nucleoside in non-coding RNAs. It enhances the function of transfer RNA and ribosomal RNA by stabilizing RNA structure.

Uridine (Uridin) is a nucleoside compound, one of the four bases that make up RNA, that replaces thymine in DNA during transcription and pairs with adenine.

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

Guanosine (DL-Guanosine) is a purine nucleoside formed from a beta-N9-glycosidic bond between guanine and a ribose ring, and is essential for metabolism.