An LSD1 inhibitor
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GSK2879552

Item No. 19403

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-benzoic acid
CAS Number
1401966-69-5
Molecular Formula
C23H28N2O2
Formula Weight
364.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 20 mg/mlPBS (pH 7.2): 5 mg/ml
λmax
224 nm
SMILES
OC(C1=CC=C(CN2CCC(CN[C@@H]3C[C@H]3C4=CC=CC=C4)CC2)C=C1)=O
InChi Code
InChI=1S/C23H28N2O2/c26-23(27)20-8-6-18(7-9-20)16-25-12-10-17(11-13-25)15-24-22-14-21(22)19-4-2-1-3-5-19/h1-9,17,21-22,24H,10-16H2,(H,26,27)/t21-,22+/m0/s1
InChi Key
LRULVYSBRWUVGR-FCHUYYIVSA-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

    $120

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    10 mg

    $203

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    25 mg

    $294

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    Cayman Chemical
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    Product Description

    GSK2879552 is a selective, orally bioavailable, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor for element-1-silencing transcription factor (CoREST) activity.1 Inhibition of LSD1 via GSK2879552 has been shown to enhance H3K4 methylation and to increase the expression of tumor-suppressor genes.1,2 GSK2879552 demonstrates anti-proliferative growth effects (EC50s = 2-240 nM) in AML cell lines and is currently under clinical evaluation for cancer treatment.1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Mohammad, H.P., Smitheman, K.N., Kamat, C.D., et al. A DNA hypomethylation signature predicts antitumor activity of LSD1 inhibitors in SCLC. Cancer Cell 28(1), 57-69 (2015).

    2. Maes, T., Mascaró, C., Ortega, A., et al. KDM1 histone lysine demethylases as targets for treatments of oncological and neurodegenerative disease. Epigenomics 7(4), 609-626 (2015).

    3. Zheng, Y.C., Yu, B., Jiang, G.Z., et al. Irreversible LSD1 inhibitors: Application of tranylcypromine and its derivatives in cancer treatment. Curr. Top. Med. Chem. 16(19), 2179-2188 (2016).