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QS 11

Catalog No.
B7364
ARFGAP1 inhibitor,Wnt/beta-catenin pathway modulator
Grouped product items
SizePriceStock Qty
5mg
$135.00
Ship with 10-15 days
10mg
$240.00
Ship with 10-15 days
25mg
$540.00
Ship with 10-15 days
50mg
$1,000.00
Ship with 10-15 days
100mg
$1,645.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

EC50: 1.5 μM for ARFGAP1 enzymatic assay [1] and 0.5 μM for Wnt synergist [2]

Purine derivative QS11 is a Wnt synergistic agonist by inhibiting the GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1). ARFGAP1 promotes hydrolysis of ARF1-bound GTP and is required in membrane trafficking and /or vesicle transport.

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]..

Clinical trial: So far, no clinical study has been conducted.

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.

Chemical Properties

Physical AppearanceOff White solid
StorageStore at -20°C
M.Wt567.68
Cas No.944328-88-5
FormulaC36H33N5O2
SolubilitySoluble in DMSO
Chemical Name(S)-2-((9-([1,1'-biphenyl]-4-ylmethyl)-2-((2,3-dihydro-1H-inden-5-yl)oxy)-9H-purin-6-yl)amino)-3-phenylpropan-1-ol
SDFDownload SDF
Canonical SMILESOC[C@H](CC1=CC=CC=C1)NC2=NC(OC3=CC=C4CCCC4=C3)=NC5=C2N=CN5CC6=CC=C(C7=CC=CC=C7)C=C6
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

QS 11