An inhibitor of c-Myc/Max dimerization
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Product Categories

Product Type

Biochemicals
Small Molecule Modulators
Small Molecule Inhibitors

Research Area

10074-G5

Item No. 17408

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[1,1'-biphenyl]-2-yl-7-nitro-2,1,3-benzoxadiazol-4-amine
CAS Number
413611-93-5
Molecular Formula
C18H12N4O3
Formula Weight
332.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS(pH 7.2) (1:4): 0.2 mg/mlEthanol: 2 mg/ml
λmax
232, 327, 467 nm
SMILES
O=[N+](C(C1=NON=C12)=CC=C2NC3=CC=CC=C3C4=CC=CC=C4)[O-]
InChi Code
InChI=1S/C18H12N4O3/c23-22(24)16-11-10-15(17-18(16)21-25-20-17)19-14-9-5-4-8-13(14)12-6-2-1-3-7-12/h1-11,19H
InChi Key
KMJPYSQOCBYMCF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $77

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    10 mg

    $120

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    25 mg

    $219

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    Product Description

    10074-G5 is a c-Myc inhibitor that binds to and distorts the bHLH-ZIP domain of c-Myc (Kd = 2.8 µM), thereby inhibiting c-Myc/Max heterodimer formation and inhibiting its transcriptional activity (IC50 = 146 µM).1,2,3 10074-G5 is cytotoxic to c-Myc-overexpressing cells lines with IC50 values of 15.6 and 13.5 µM for Daudi Burkitt lymphoma cells and HL60 promyelocytic leukemia cells, respectively.4 10074-G5 can also interfere with N-Myc/Max interactions (Kd = 19.2 µM for binding the bHLH-Zip of N-Myc), inducing apoptosis in N-Myc amplified neuroblastoma Kelly cells (IC50 = 22.5 µM).5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Follis, A.V., Hammoudeh, D.I., Wang, J., et al. Structural rationale for the coupled binding and unfolding of the c-Myc oncoprotein by small molecules. Chem. Biol. 15(11), 1149-1155 (2008).

    2. Hammoudeh, D.I., Follis, A.V., Prochownik, E.V., et al. Multiple independent binding sites for small-molecule inhibitors on the oncoprotein c-Myc. J. Am. Chem. Soc. 131(21), 7391-7401 (2009).

    3. Yap, J.L., Wang, H., Hu, A., et al. Pharmacophore identification of c-Myc inhibitor 10074-G5. Bioorg. Med. Chem. Lett. 23(1), 370-374 (2013).

    4. Clausen, D.M., Guo, J., Parise, R.A., et al. In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization. J. Pharmacol. Exp. Ther. 335(3), 715-727 (2010).

    5. Müller, I., Larsson, K., Frenzel, A., et al. Targeting of the MYCN protein with small molecule c-MYC inhibitors. PLoS One 9(5), (2014).