An ARFGAP inhibitor
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QS11

Item No. 21247

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
βS-[[9-([1,1'-biphenyl]-4-ylmethyl)-2-[(2,3-dihydro-1H-inden-5-yl)oxy]-9H-purin-6-yl]amino]-benzenepropanol
CAS Number
944328-88-5
Molecular Formula
C36H33N5O2
Formula Weight
567.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: <100 mMEthanol: <100 mM
λmax
272 nm
SMILES
OC[C@H](CC1=CC=CC=C1)NC2=C3C(N(CC4=CC=C(C5=CC=CC=C5)C=C4)C=N3)=NC(OC6=CC=C(CCC7)C7=C6)=N2
InChi Code
InChI=1S/C36H33N5O2/c42-23-31(20-25-8-3-1-4-9-25)38-34-33-35(40-36(39-34)43-32-19-18-28-12-7-13-30(28)21-32)41(24-37-33)22-26-14-16-29(17-15-26)27-10-5-2-6-11-27/h1-6,8-11,14-19,21,24,31,42H,7,12-13,20,22-23H2,(H,38,39,40)/t31-/m0/s1
InChi Key
DOKZLKDGUQWMSX-HKBQPEDESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $253

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    25 mg

    $587

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    Cayman Chemical
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    Product 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.1 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.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhang, Q., Major, M.B., Takanashi, S., et al. Small-molecule synergist of the Wnt/β-catenin signaling pathway. Proc. Natl. Acad. Sci. USA 104(18), 7444-7448 (2007).

    2. Singh, M.K., Gao, H., Sun, W., et al. Structure-activity relationship studies of QS11, a small molecule Wnt synergistic agonist. Bioorg. Med. Chem. Lett. 25(21), 4838-4842 (2015).