A KAT8 inhibitor
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KAT8 Inhibitor 19

Item No. 38977

Technical Information
Formal Name
4-[4,5-dihydro-3-methyl-5-oxo-4-(1H-pyrrol-2-ylmethylene)-1H-pyrazol-1-yl]-benzoic acid
CAS Number
28532-21-0
Synonyms
  • Lysine Acetyltransferase 8 Inhibitor 19
Molecular Formula
C16H13N3O3
Formula Weight
Purity
≥98%
Formulation
A solid
Acetonitrile: SolubleDMSO: Soluble
SMILES
CC(C1=CC2=CC=CN2)=NN(C3=CC=C(C(O)=O)C=C3)C1=O
InChi Code
InChI=1S/C16H13N3O3/c1-10-14(9-12-3-2-8-17-12)15(20)19(18-10)13-6-4-11(5-7-13)16(21)22/h2-9,17H,1H3,(H,21,22)
InChi Key
WBHVGUYXAZIVHV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    KAT8 inhibitor 19 is an inhibitor of lysine acetyltransferase 8 (KAT8; IC50 = 12.1 µM).1 It is selective for KAT8 over KAT2A, KAT2B, KAT3B, KAT6A, and KAT7 at 200 µM. KAT8 (50 µM) reduces histone 4 lysine 16 acetylation (H4K16Ac) in HT-29 colorectal carcinoma cells. It reduces the viability of HCT116, H1299, A549, and U937 cancer cells (IC50s = 39.4, 52.1, 41, and 30.1 µM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fiorentino, F., Sementilli, S., Menna, M., et alFirst-in-class selective inhibitors of the lysine acetyltransferase KAT8. J. Med. Chem. 66(10), 6591-6616 (2023).