A reactivator of p53
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Roslin-2

Item No. 21985

Technical Information
Formal Name
1-(phenylmethyl)-3,5,7-triaza-1-azoniatricyclo[3.3.1.13,7]decane, monobromide
CAS Number
29574-21-8
Molecular Formula
C13H19N4 • Br
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
SMILES
[N@@]12C[N+](C[N@](C2)C3)(CC4=CC=CC=C4)C[N@]3C1.[Br-]
InChi Code
InChI=1S/C13H19N4.BrH/c1-2-4-13(5-3-1)6-17-10-14-7-15(11-17)9-16(8-14)12-17;/h1-5H,6-12H2;1H/q+1;/p-1
InChi Key
YJMKPGPWDHCYCD-UHFFFAOYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Roslin-2 is a reactivator of p53.1 Roslin-2 (111, 333, and 1000 µM) impairs the interaction between focal adhesion kinase (FAK) and p53 and restores p53 transcriptional activity. It reverses FAK-mediated suppression of the expression of p53-dependent p21, MDM2, and Bax in wild-type p53 HCT116 colon and MCF-7 breast cancer cells, but not in p53 mutant SW620 colon cancer cells, when used at concentrations ranging from 1 to 50 µM. Roslin-2 (10 µM) potentiates the pro-apoptotic effect of doxorubicin (Item No. 15007) and 5-fluorouracil (Item No. 14416) in p53+/+, but not p53-/-, HCT116 cells. It reduces tumor growth and activates p21 in p53+/+, but not p53-/- tumors, in HCT116 mouse xenograft models when administered at a dose of 60 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Golubovskaya, V.M., Ho, B., Zheng, M., et alDisruption of focal adhesion kinase and p53 interaction with small molecule compound R2 reactivated p53 and blocked tumor growth. BMC Cancer 13:342, (2013).