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The safety and efficacy of this agent(s), or use in this setting, has not been established or is subject to confirmation. For an agent(s) whose safety and efficacy has not been established or confirmed, future regulatory approval or commercial availability is not guaranteed.

KAT2 Inhibitor

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KAT2 Inhibitor

PF-07994525 | KAT2 is an investigational compound.  Its safety and efficacy have not been established.

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Overview + Rationale

Rationale for Cancer Target

  • KAT2A and KAT2B are transcriptional coactivators that acetylate histone H3 at lysine 9 (H3K9ac),2,3 promoting expression of genes involved in proliferation, differentiation, apoptosis, and immune responses.4
  • Through the SAGA complex, they recruit transcription factors like MYC, E2F, and MAF to activate gene expression.5,6

 

Overview1,6-7

  • PF-07994525 is a small molecule lysine acetyltransferase catalytic inhibitor targeting the KAT2 enzymes1
  • Preclinical data show that PF-07994525 selectively binds to KAT2A/2B inhibiting the acetylation of H3K9Ac6
  • In preclinical models, KAT2A/2B inhibition by PF-07994525 disrupts oncogenic transcriptional programs, e.g., MYC, E2F, and MAF6

Mechanism of Action

Stage of Development

Other

Advanced Malignancies

Phase 1 Monotherapy
This information is current as of August 4th 2026.

Ac=acetyl; HAT, histone acetyltransferase; H3K9ac, histone H3 lysine 9 acetylation; KAT, lysine acetyltransferase; MYC, family of regulator genes and proto-oncogenes that code for transcription factors; SAGA, Spt-Ada-Gcn5 acetyltransferase; TF, transcription factor.; TRRAP, transformation/transcription domain associated protein.

REFERENCES:  1. Pfizer Data on File; 2. Arede L et al. Blood Adv. 2022;6(1):165-180; 3.Jin, Q., et al., EMBO J, 2011. 30(2): p. 249-62; 4. Chen, Y.C. Dent, S.Y.R. Epigenetics Chromatin, 2021.14:26; 5. Ramberger, E., et al., Nat Cancer, 2024. 5(8): p. 1267-1284; 6. Chen, Y.C., et al. Genes Dev, 2024.38(15-16): p. 738-754; 7. Jensen-Pergakes K et al. Cancer Res 2026;86(7 Suppl):Abstract nr 6781; 8. NCT07426757. https://clinicaltrials.gov/study/NCT07426757 updated April 7, 2026. Accessed July 16, 2026