Histone Acetyltransferase Inhibitor

NU9056 is a potent and selective Tip60 (KAT5) histone acetyltransferase inhibitor with an of 2 µM. NU9056 shows >16-fold selectivity for Tip60 over PCAF, p300 and GCN5. NU9056 induces apoptosis of prostate cancer cells.

Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.

GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC₅₀ of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC₅₀s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.

Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.

Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. 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.

E-7386 is an orally active CBP/beta-catenin modulator.

JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1) with an IC₅₀ of 14.8 μM. JG-2016 can inhibit the growth of multiple tumor cells and has anti-tumor activity.

PLX51107 is a potent and selective BET inhibitor, with K_ds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (K_d, in the 100 nM range).

SGF29-IN-1 (Compound Cpd_DC60) is a selective inhibitor for Spt-Ada-Gcn5 acetyltransferase (SAGA)–associated factor 29 (SGF29)-Tudor domain. SGF29-IN-1 exhibits activity against leukemia.

MC4033 shows IC₅₀s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively.
MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells.

MC4171 (compound 34) is a selective KAT8 inhibitor (IC₅₀=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer.

Naa50-IN-1 is an N-alpha-acetyltransferase 50 (Naa50) inhibitor with an IC₅₀ of 7 nM against the human protein. Naa50-IN-1 exhibits selectivity toward the related enzymes Naa10 and Naa60. Naa50-IN-1 binds to the substrate-binding pocket of Naa50, and its binding affinity is enhanced by AcCoA.

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.

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.

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.

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.

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.

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.