Histone Acetyltransferase Inhibitor

Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.

BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC₅₀ of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth.

L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC₅₀ of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.

TCIP3 is a bivalent molecular glue degrader that binds dually to p300/CBP and BCL6. TCIP3 redirects p300 and CBP, thereby activating programmed cell death genes that are normally repressed by the oncogenic driver gene BCL6. TCIP3 induces acetylation of BCL6 and histone tails, inhibits c-MYC transcription. TCIP3 can be used for the research of diffuse large B-cell lymphoma (DLBCL).

PCAF-IN-1 is a highly selective PCAF inhibitor. PCAF-IN-1 is a antitumor agents, which can be used in tumor research research.

Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC₅₀ of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.

DS-9300 is a potent, orally active, selective EP300/CBP HAT inhibitor with an IC₅₀ value of 28 nM. DS-9300 has anticancer activity and can be used in prostate cancer disease research.

KI-TOX-A3 is a TOX protein-protein interaction inhibitor that blocks the TOX-KAT7 protein-protein interaction with an IC₅₀ of 0.51 μM. KI-TOX-A3 induces proteasomal degradation of TOX, restores KAT7-mediated H3K14 acetylation, reverses exhaustion of CD8⁺ T cells, and inhibits the proliferation of T cell acute lymphoblastic leukemia (T-ALL) cells. KI-TOX-A3 shows promise for use in studies of hematological malignancies such as T-ALL.

Curcumin-d₆ (Diferuloylmethane-d₆ ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.

PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC₅₀ value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase.

XX-650-23 is a potent CREB inhibitor. XX-650-23inhibits CREB function through disruption of CBP-CREB interaction. XX-650-23 can be used for AML research.

Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC₅₀=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC₅₀=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.

CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.

NSC 694621 is a potent PCAF inhibitor, with an IC₅₀ of 5.71 µM (PCAF/H3_1-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells.

MOZ-IN-3 is an orally active KAT6A (MOZ) inhibitor with an IC₅₀ of 0.03 μM against human targets, and it exhibits high selectivity over other MYST family histone acetyltransferases. MOZ-IN-3 modulates monocyte function, exerts anti-tumor effects, increases the nucleocytoplasmic ratio, and enhances cellular resistance to chemotherapeutic drug-induced cell death. MOZ-IN-3 is applicable to leukemia-related research.

NAT1-IN-1 (compound 350) is a potent N-acetyltransferase 1 (NAT1)-targeted inhibitor, with an IC₅₀ of 44 nM. NAT1-IN-1 can be used for the research of hypermetabolic diseases such as amyotrophic lateral sclerosis, cancer cachexia, and sepsis.

Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP.

TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K_d values of 134 nM and 5.02 μM for CBP and BRD4.

CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.

DCH36_06 is a potent and selective p300/CBP inhibitor with IC₅₀s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.