An ALKBH5 inhibitor
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ALKBH5-IN-5

Item No. 46498

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-(2-methoxyphenyl)ethyl]-1H-pyrrole-2,5-dione
CAS Number
140481-05-6
Synonyms
  • ALKBH5 Inhibitor 5
  • Alpha-ketoglutarate-dependent Dioxygenase alkB Homolog 5-IN-5
  • Alpha-ketoglutarate-dependent Dioxygenase alkB Homolog 5 Inhibitor 5
Molecular Formula
C13H13NO3
Formula Weight
231.3
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
COC1=C(C=CC=C1)CCN(C(C=C2)=O)C2=O
InChi Code
InChI=1S/C13H13NO3/c1-17-11-5-3-2-4-10(11)8-9-14-12(15)6-7-13(14)16/h2-7H,8-9H2,1H3
InChi Key
HIXVCNYFZONNJH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $29

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    10 mg

    $38

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    50 mg

    $131

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    100 mg

    $203

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    Cayman Chemical
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    Product Description

    ALKBH5-IN-5 is an inhibitor of the mRNA N6-methyladenosine (m6A) demethylase activity of alpha-ketoglutarate-dependent dioxygenase alkB homolog 5 (ALKBH5; IC50 = 0.62 µM.1 It is selective for ALKBH5 over the m6A demethylase fat mass and obesity-associated protein (FTO) at 50 µM and a panel of 14 proteases at 10 µM. ALKBH5-IN-5 increases m6A levels in NB4 leukemia cells and reduces the proliferation of MOLM-13, MV4-11, NOMO-1, and NB4 leukemia cells (IC50s = 0.63-2.99 µM). It reduces tumor volume in an NB4 mouse xenograft model and inhibits tumor growth and metastasis in a 143B osteosarcoma mouse xenograft model overexpressing the long non-coding RNA (lncRNA) ZMIZ1-AS1, an effect that is enhanced when co-administered with the FGFR inhibitor BGJ398 (Item No. 19157).1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wu, H., Lai, G.Q., Cheng, R., et al. Discovery of covalent and cell-active alkbh5 inhibitors with potent antileukemia effects in vivo. Angew. Chem. Int. Ed. Engl. 64(18), e202424928 (2025).

    2. Zhang, Y., Xu, Y., Bao, Y., et al. ALKBH5 demethylation modification of SE-lncRNA ZMIZ1-AS1 promotes FGFR1-mediated proliferation and invasive metastasis in osteosarcoma. Cell Mol. Life Sci. 83(1), 33 (2025).