Histone Acetyltransferase Inhibitor

XP-524 is a potent BET and EP300 inhibitor. XP-524 shows great tumoricidal activity in vivo. XP-524 prevents KRAS-induced, neoplastic transformation in vivo and extends survival in two transgenic mouse models of aggressive PDAC. XP-524 also enhances the presentation of self-peptide and tumor recruitment of cytotoxic T lymphocytes. XP-524 has the potential for the research of pancreatic ductal adenocarcinoma (PDAC).

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d of 2.2 nM and an IC₅₀ of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.

CHI-KAT8i5 is a selective and orally active KAT8 inhibitor with a K_D value of 19.72 μM. CHI-KAT8i5 does not bind to other proteins in HAT family (KAT2A, KAT2B, KAT5, and KAT7). CHI-KAT8i5 induces cancer cell apoptosis. CHI-KAT8i5 suppresses esophageal squamous cell carcinoma (ESCC) growth through targeting KAT8/c-Myc signaling pathway.

NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC₅₀ value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer.

Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (K_d:8.6 μM), blocks the interaction between the KIX domain and the KID domain of CREB with IC₅₀ of 2.26 μM. Naphthol AS-E can be used for cancer research.

Omvitrastat (OP-3136) is an orally active, highly selective inhibitor of KAT6A and KAT6B. Omvitrastat inhibits the proliferation of prostate cancer, ovarian cancer and non-small cell lung cancer cells that express or overexpress KAT6A. Omvitrastat reduces the proliferative capacity of cancer cells and suppresses cell growth in ER⁺ breast cancer cell models with KAT6 overexpression. Omvitrastat induces tumor regression and inhibits tumor growth in an ovarian cancer xenograft model in immunodeficient mice. Omvitrastat inhibits tumor growth in a non-small cell lung cancer xenograft model in immunodeficient mice. Omvitrastat can be used in research related to HR⁺/HER^2- breast cancer, prostate cancer, ovarian cancer and non-small cell lung cancer (NSCLC).

CBP/p300-IN-8 is a potent inhibitor of the CBP/P300 family of bromodomains. CBP/p300-IN-8 inhibits CBP (IC₅₀=0.01-0.1 µΜ) and BRD4 (IC₅₀=1-1000 µΜ) activity.

CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC₅₀ of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC₅₀ of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.

UMB298 is a potent and selective CBP/P300 bromodomain inhibitor.

PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.

MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC₅₀ of 125 μM.

Pocenbrodib is a P300/CBP inhibitor. Pocenbrodib blocks the function of P300/CBP and inhibits the acetylation of histones and non-histone proteins. Pocenbrodib may be used in research related to castration-resistant prostate cancer and other cancers.

CPTH2-Alkyne is a cell active analog of CPTH2 (HY-W013274). CPTH2-Alkyne specifically accumulates in nucleoli and locates in nuclear periphery and in cytoplasma. CPTH2-Alkyne inhibits N-acetyltransferase 10 (NAT10). CPTH2-Alkyne is used in study of nuclear architecture and application in laminopathy.

CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC₅₀s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity.

KAT6A/KAT7-IN-4 is a KAT6A and KAT7 inhibitor. KAT6A/KAT7-IN-4 has IC₅₀ values of both ≤ 1 nM for KAT6A and KAT7. KAT6A/KAT7-IN-4 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-4 also inhibits tumor cell proliferation, with an IC₅₀ of ≤ 100 nM for CAMA-1. KAT6A/KAT7-IN-4 can be used in the study of breast cancer.

Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC₅₀ value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia).

SYY-B029-2 is a potent histone acetyltransferase (HAT) inhibitor with an IC₅₀ of 1.4 nM. SYY-B029-2 cell growth of human mantle cell lymphoma (MCL) cell line MAVER-1 and human castration resistant prostate cancer cell line LNCaP clone FGC, with IC₅₀ values of 15 nM and 13 nM, respectively.

CBP/p300-IN-10 is a highly potent histone acetyltransferase EP300 and CREBBP with IC₅₀ values of 26 nM and 39 nM, respectively. CBP/p300-IN-10 can be used to research anticancer.

EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC₅₀s of 2.9 and 1.1 μM, respectively.

Snail IN-1 is an orally active Snail inhibitor with a Ka of 0.36 μM.Snail IN-1 disrupts Snail-CBP interaction, accelerates Snail protein degradation, reduces Snail acetylation, increases Snail polyubiquitination, and selectively downregulates Snail protein without altering other EMT transcription factors.Snail IN-1 reduces atherosclerotic plaque burden, modulates inflammation and plaque stability factors, downregulates CCL5, CXCL10, MMP2, and MMP9, and upregulates α-smooth muscle actin.Snail IN-1 exerts anti-inflammatory and plaque-stabilizing properties.Snail IN-1 can be used for the research of atherosclerosis.