Kinase Inhibitor Library
From the Halo Fan Fiction Wikia, writing 12,604 fan fiction articles
|
This article, Kinase Inhibitor Library, was written by RelentlessRecusant. Please do not edit this fiction without the writer's permission. |
.jpg)
The Kinase Inhibitor Library, colloquially referred to as the "Kinase Library", is a commercially-available collection of small-molecule chemical compounds that saturate the entire human kinome, providing at least one specific inhibitor for each of the five hundred human kinases as well as general and promiscuous kinase inhibitors.[1] Inhibitors of protein kinases generally function through three general modalities on the structural level: by binding to the active ATP-binding site, stabilization of the kinase in an inactive conformation, or at a kinase-unique allosteric binding site.[2]
A comprehensive kinase inhibitor collection is available from Acumen Science Laboratories; the library spans eight 96-well plates, and each small-molecule compound is cheminformatically documented and indexed with an exclusive and accurate plate map, and each compound is solubilized stably in DMSO at a 10 mM concentration for thousandfold dilution into an approximate active concentration.
[edit] References
- ↑ Bilanges et. al (2008). Killing two kinase families with one stone. Nature Chemical Biology (4): 648-649.
- ↑ Adrián et. al (2006). Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nature Chemical Biology (2): 93-102.
| Chemical Biology: Small-Molecule Control of Biological Systems (RelentlessRecusant) | ||
|---|---|---|
| | ||
| 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 | ||
