Histone Acetyltransferase Inhibitor

NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC₅₀ value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.

BT-O2C is a p300 PROTAC degrader. BT-O2C induces p300 degradation via proteasome- and ubiquitin-like modification-dependent pathways, downregulates the expression of CIC::DUX4 sarcoma target genes, and exerts cytotoxicity against such sarcoma cells. BT-O2C can be used in CIC::DUX4 sarcoma-related studies.

KAT6A/KAT7-IN-3 is a KAT6A and KAT7 inhibitor. KAT6A/KAT7-IN-3 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-3 also inhibits tumor cell proliferation and can be used in the study of cancer.

JYZ3032 is an orally active super inhibitor of androgen receptor (AR) and p300/CBP. JYZ3032 redirects the catalytic activity of p300 and locks the complex in a transcriptionally inactive state, thereby inhibiting AR-driven transcription and proliferation. JYZ3032 induces deep and durable tumor regression in castration-resistant and patient-derived xenograft models, and exhibits good tolerability. JYZ3032 can be used in research related to metastatic castration-resistant prostate cancer and prostate cancer.

P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC₅₀ of 18.8 nM.

B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC₅₀ values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.

CBP/p300-IN-20 is a potent and selective p300/CBP inhibitor, with a pIC₅₀ of 10.1 for p300. CBP/p300-IN-20 can be used for the research of cancer.

CTX-0124143 is a KAT6A inhibitor with a sulfonyl hydrazine skeleton.

KAT7 Human Pre-designed siRNA Set A contains three designed siRNAs for KAT7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

DC-CPin711 is a potent and selective inhibitor of CREB-binding protein (CBP) bromodomain with an IC₅₀ of 0.0626 μM. DC-CPin711 arrests cell cycle at G1 phase and induces apoptosis.

CAY10669 (compound 6d) is an anacardic acid (HY-N2020) derivative that inhibits histone acetyltransferase PCAF with an IC₅₀ of 662 μM. CAY10669 enhances the SAHA-induced acetylation in HEPG2 cells, exhibits cytotoxicity in zebrafish embryo, promotes transgene expression in CHO-K1 cells.

Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site.

NAT2-IN-1 (APA) is an inhibitor of agent metabolic enzyme N-acetyltransferase 2 (NAT2). NAT2-IN-1 can selectively kill slow NAT2 cells.

Acetylethylcholine mustard hydrochloride (Acetyl-AF64) is an inhibitor of choline acetyl-transferase that reduces the contraction frequency of the myotubes by inhibiting the synthesis of acetylethylcholine (Ach) with the half-maximal inhibitory concentration (IC₅₀) of 1.22 mM. Acetylethylcholine mustard hydrochloride is an irreversible ligand for the high affinity choline transport system. Acetylethylcholine mustard hydrochloride is also a cholinotoxin. Acetylethylcholine mustard hydrochloride is a precursor for ethylcholine mustard aziridinium ion.

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

A-485 (Standard) is the analytical standard of A-485 (HY-107455). This product is intended for research and analytical applications. A-485, a chemical probe, is a potent and selective catalytic inhibitor of p300/CBP with IC₅₀s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively.

CBP/EP300-IN-2 is an inhibitor of CBP/EP300 with IC₅₀ values of 1.07 nM and 5.96 nM for CBP/HTRF and Myc, respectively. CBP/EP300-IN-2, example 25, is extracted from patent WO2017205538A1.

CZL-105 is a highly potent, selective, and orally active p300/CBP inhibitor, with IC₅₀ values of 0.09 μM and 0.08 μM against p300 and CBP bromodomains, respectively. CZL-105 inhibits the proliferation of OPM-2 multiple myeloma cells with an IC₅₀ of 57 nM, and induces G0/G1 cell cycle arrest and apoptosis. CZL-105 is applicable for research related to multiple myeloma.

P300-IN-1 (cpd205) is a Histone acetylase p300 inhibitor.

CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).