QS11 Property

Boiling point:

852.2±75.0 °C(Predicted)

Density 

1.27

storage temp. 

Keep in dark place,Sealed in dry,2-8°C

solubility 

Soluble in DMSO

form 

Pale amber solid

pka

14.46±0.10(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H317May cause an allergic skin reaction

H319Causes serious eye irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

QS11 Chemical Properties,Usage,Production

Description

QS11 is an inhibitor of GTPase activating protein of ADP-ribosylation factors (ARFGAPs) that increases activity of ARFs in NIH3T3 cells at a concentration of 1 μM. It activates Wnt/β-catenin activity in a reporter assay using HEK293 cells (EC₅₀ = 0.5 μM). QS11 exhibits synergy with Wnt-3a ligand-conditioned media, inducing a 200-fold increase in reporter activity compared to 40- and 2-fold increases observed with Wnt-3a ligand-conditioned media alone or QS11 treatment alone, respectively. It inhibits ARFGAP1 with an EC₅₀ value of 1.5 μM in an enzyme assay and inhibits the migration of MDA-MB-231 breast cancer cells that overexpress AMAP1, an ARFGAP essential to cellular invasiveness.

Uses

QS 11 is a small molecule Wnt synergistic agonist.

Definition

ChEBI: (2S)-2-[[2-(2,3-dihydro-1H-inden-5-yloxy)-9-[(4-phenylphenyl)methyl]-6-purinyl]amino]-3-phenyl-1-propanol is a member of biphenyls.

in vitro

qs11 showed potent wnt synergist activity with little cytotoxicity in hek293 cells (ec50 = 0.5 μm) and human primary fibroblast cells (ec50 ≥ 10 μm). qs11 at 2.5 μm activated the super(8x)topflash reporter ~200-fold in the presence of wnt-3a conditioned medium. synergistic effect was also observed when qs11 was combined with recombinant wnt-3a protein (10–200 ng/ml) [2].

in vivo

in wnt signaling test model, embryos were injected with qs11, xwnt-8 rna or a combination of qs11and xwnt-8 rna. compared with qs11 alone and xwnt-8 rna alone, injection of a combination of xwnt-8 rna and qs11 induced significantly more full (20.9%) and partial (30.2%) double axis formation [2]..

storage

Store at +4°C

References

[1] singh mk1, gao h1, sun w1, song z1, schmalzigaug r2, premont rt2, zhang q3. structure-activity relationship studies of qs11, a small molecule wnt synergistic agonist. bioorg med chem lett. 2015 nov 1;25(21):4838-42.
[2] zhang q1, major mb, takanashi s, camp nd, nishiya n, peters ec, ginsberg mh, jian x, randazzo pa, schultz pg, moon rt, ding s. small-molecule synergist of the wnt/beta-catenin signaling pathway. proc natl acad sci u s a. 2007 may 1;104(18):7444-8. epub 2007 apr 25.