A KDM2/7 inhibitor
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TC-E 5002

Item No. 17717

Technical Information
Formal Name
N-(9-cyclopropyl-1-oxononyl)-N-hydroxy-β-alanine
CAS Number
1453071-47-0
Molecular Formula
C15H27NO4
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 10 mg/mlDMSO: 30 mg/mlEthanol: 50 mg/mlPBS (pH 7.2): 0.25 mg/ml
SMILES
O=C(O)CCN(C(CCCCCCCCC1CC1)=O)O
InChi Code
InChI=1S/C15H27NO4/c17-14(16(20)12-11-15(18)19)8-6-4-2-1-3-5-7-13-9-10-13/h13,20H,1-12H2,(H,18,19)
InChi Key
NEHSERYKENINRH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TC-E 5002 is an inhibitor of the histone lysine demethylase (KDM) subfamily KDM2/7 (IC50s = 6.8, 0.2, and 1.2 µM for KDM2A, KDM7A, and KDM7B, respectively).1 It is selective for the KDM2/7 subfamily over KDM4A, KDM4C, KDM5A, and KDM6A/UTX (IC50s = >120, 83, 55, and 100 µM, respectively). It inhibits the growth of N2a, KYSE150, and HeLa cells with GI50 values of 86, 16, and 40 µM, respectively, which are in the range where it increases H3K27me2 levels in KYSE150 and HeLa cells. TC-E 5002 decreases gene expression of E2F1, a transcription factor activated by KDM7B that leads to progression of the cell cycle. In addition, TC-E 5002 treatment leads to cell cycle arrest at the G0/G1 phase in KYSE150 and HeLa cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Suzuki, T., Ozasa, H., Itoh, Y., et alIdentification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. J. Med. Chem. 56(18), 7222-7231 (2013).