A KAT6A/MOZ and KAT6B/MORF inhibitor
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PF-9363

Item No. 37778

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,6-dimethoxy-N-[4-methoxy-6-(1H-pyrazol-1-ylmethyl)-1,2-benzisoxazol-3-yl]-benzenesulfonamide
CAS Number
2569009-58-9
Synonyms
  • CTx-648
Molecular Formula
C20H20N4O6S
Formula Weight
444.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
SMILES
O=S(NC1=NOC2=CC(CN3C=CC=N3)=CC(OC)=C21)(C4=C(OC)C=CC=C4OC)=O
InChi Code
InChI=1S/C20H20N4O6S/c1-27-14-6-4-7-15(28-2)19(14)31(25,26)23-20-18-16(29-3)10-13(11-17(18)30-22-20)12-24-9-5-8-21-24/h4-11H,12H2,1-3H3,(H,22,23)
InChi Key
VNSQFPFWUAZOTQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

    $198

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    10 mg

    $351

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    25 mg

    $767

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    Product Description

    PF-9363 is an inhibitor of lysine acetyltransferase 6A (KAT6A), also known as monocytic leukemia zinc finger protein (MOZ) and KAT6B, also known as MOZ-related factor (MORF; Kis = 0.27 and 2.4 nM, respectively).1 It is selective for KAT6A and KAT6B over KAT7, KAT5, and KAT8 (Kis = 70, 420, and 670 nM, respectively). PF-9363 reduces the proliferation of, and the levels of acetylation of histone 3 lysine 23 (H3K23Ac) and lysine 14 (H3K14Ac) in, ZR-75-1 breast epithelial carcinoma cells (IC50s = 0.37, 0.85, and 120 nM, respectively). It reduces tumor levels of H3K23Ac and tumor volume without affecting body weight in a ZR-75-1 breast cancer mouse xenograft model when administered at doses of 0.03, 03, or 5 mg/kg per day. PF-9363 (1 mg/kg per day) reduces tumor volume and increases survival in a patient-derived xenograft (PDX) mouse model of breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sharma, S., Chung, C.-Y., Uryu, S., et al. Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer. Cell Chem. Biol. 30, (2023).