QS11

From the Halo Fan Fiction Wikia, writing 13,088 fan fiction articles

QS11 Chemical information IUPAC Nomenclature (S)-2-(9-(biphenyl-4-ylmethyl)-2-(2,3-dihydro-1H-inden-5-yloxy)-9H-purin-6-ylamino)-3-phenylpropan-1-ol Chemical Formula C36H33N5O2 Molecular Weight 567.26 g/mol Clinical information Clinical Usage Wnt/β-catenin agonist Mechanism of Action Inhibitor of ADP-ribosylation factor 1 (ARFGAP1) Known Side Effects Carcinogenic; significantly elevated incidence of colorectal cancer[1] Legal Status Not approved by the UNSC Medical Corps for in vivo clinical usage Pregnancy Status Contraindicated (embryonic gastrulation and cardiogenesis) Marketed by Acumen Science Laboratories Pharmacokinetic information Elimination Half-Life High

[Source]

QS11, IUPAC name (S)-2-(9-(biphenyl-4-ylmethyl)-2-(2,3-dihydro-1H-inden-5-yloxy)-9H-purin-6-ylamino)-3-phenylpropan-1-ol, is a small-molecule chemical inhibitor of GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) that synergizes with recombinant Wnt3a in the activation of the canonical Wnt/β-catenin signaling pathway.^[2]. It was originally concieved from the high-throughput screening of a 100,000 compound library of heterocycles against a low-content luciferase-based assay analysis system, where 2,6,9-trisubstituted purine derivatives were identified through chemical hierarchical clustering of compound hits. Focused structure-activity relation (SAR) studies resulted in the synthesis of a derivative, QS11, which demonstrated the most potent activity.

QS11 was originally synthesized and characterized by Zhang et. al in 2006 at the Scripps Research Institute in California, United States of America.

[edit] References

1. ↑ Lepourcelet et. al (2004). Small-molecule antagonists of the oncogenic Tcf/β-catenin protein complex. Cancer Cell (5): 91-102.
2. ↑ Zhang et. al (2006). Small-molecule synergist of the Wnt/β-catenin signaling pathway. Proceedings of the National Academy of Sciences (104): 7444–7448.

Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant)
Biological Targets		Compound Names
Receptor Tyrosine Kinases		A-83-01 (TGFβ/Activin) · BPIQ-II (EGFR) · Dorsomorphin/LDN-193189 (TGFβ/BMP) · SU5402 (FGFR)
Signaling Kinases		A-769662 (AMPK) · BMS-354825 (BCR-ABL, Src)· BIO-Acetoxime (GSK3) · CHIR99021 (GSK3) · GO 6976 (PKC) · IMD-0354 (IκBa) · PD184352 (MAPK) · SB203580 (MAPK) · Y-27632 (ROCK)
G Protein-Coupled Receptor		(+)-WIN-55212 (CB1/CB2) · ±-Sulpride (D2) · A 841720 (mGluR1) · BP-554 (5-HT1A) · Hh-Ag1.5 (Smo) · Cyclopamine/KAAD-Cyclopamine (Smo) · SANT1 (Smo) · SB-277011 (D3)
Ion Channels		BAY K8644 (Cav1.2) · Bicuculline (GABAAR) · Cymarin (Na+/H+) · G-strophanthin (Na+/H+) · L-AP4 (Na+/H+) · Oxcarbazepine (Na+) · Resiniferatoxin (TRPV1) · Sarmentogenin (Na+/H+) · Theanine (AMPAR, NMDAR)
Transporters		O-1783 (DAT) · WF-23 (DAT, SERT)
Nuclear Receptor		All-trans retinoic acid (RAR/RXR) · GW501516 (PPARδ) · RU-486 (Nr3c1, Nr3c3)
Protein Phosphatases		Endothall (PP2A)
Polypharmacological		Phosphoserine (mGluR4) · PK115-584 (Tcf4/β-catenin, PKC) · Pluripotin · Reversine
Other		2C-E (DAT) · 4-methoxyphenyl-HTI-286 (α/β-tubulin) · Compound E/DAPT (presenilin-1) · D-cysteine · D-phenylalanine · Flurbiprofen (COX) · JZL184 (MAGL) · QS11 (RAFGAP1) · RO-28-1675 (glucokinase) · Robotnikinin (Shh) · Selegiline (MAOB)
Uncharacterized		Neuropathiazol
Libraries		Kinase Inhibitor Library
Publications
Small molecule-mediated manipulation of the adult human induces selective and reversible control of physiological and psychological phenotype (Rubin et. al, 2590. Nature Medicine)
Source · Edit