Histone Acetyltransferase Inhibitor

NSC 228155 (Standard) is the analytical standard of NSC 228155 (HY-101084). This product is intended for research and analytical applications. NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.

L002 (Standard) is the analytical standard of L002 (HY-100671). This product is intended for research and analytical applications. 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.

HAT-IN-11 is a Histone acetyltransferase (HAT) inhibitor. HAT-IN-11 is used for research on lymphoma and castration-resistant prostate cancer.

Acetaminophen-d₅ is deuterated-labeled Acetaminophen (HY-66005). Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.

CPI-637 (Standard) is the analytical standard of CPI-637 (HY-100482). This product is intended for research and analytical applications. CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.

I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (K_ds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.

SGC-CBP30 (Standard) is the analytical standard of SGC-CBP30 (HY-15826). This product is intended for research and analytical applications. SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (K_ds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.

Naphthol AS-E (Standard) is the analytical standard of Naphthol AS-E (HY-104068). This product is intended for research and analytical applications. 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 (Kd: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.

GNE-781 (Standard) is the analytical standard of GNE-781 (HY-108696). This product is intended for research and analytical applications. 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.

Curcumin-d₃ (Diferuloylmethane-d₃ ) 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.

GNE-049 (Standard) is the analytical standard of GNE-049 (HY-108435). This product is intended for research and analytical applications. GNE-049 is a highly potent and selective CBP inhibitor with an IC₅₀ of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC₅₀s of 12 nM and 4200 nM, respectively.

WM-3835 (Standard) is the analytical standard of WM-3835 (HY-134901). This product is intended for research and analytical applications. WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.

XDM-CBP is a CBP/p300 inhibitor. XDM-CBP can be used in the study of malignant melanoma, breast cancer and leukemia.

EML 425 (Standard) is the analytical standard of EML 425 (HY-110263). This product is intended for research and analytical applications. EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC₅₀s of 2.9 and 1.1 μM, respectively.

Garcinol (Standard) is the analytical standard of Garcinol. This product is intended for research and analytical applications. Garcinol, a polyisoprenylated benzophenone harvested from Garcinia indica, exerts anti-cholinesterase properties towards acetyl cholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50s of 0.66 μM and 7.39 μM, respectively. Garcinol also inhibits histone acetyltransferases (HATs, IC50= 7 μM) and p300/CPB-associated factor (PCAF, IC50 = 5 μM). Garcinol has anti-inflammatory and anti-cancer activity.

GNE-272 (Standard) is the analytical standard of GNE-272 (HY-100726). This product is intended for research and analytical applications. GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.

NU9056 (Standard) is the analytical standard of NU9056 (HY-110127). This product is intended for research and analytical applications. 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.

WM-1119 (Standard) is the analytical standard of WM-1119 (HY-102058). This product is intended for research and analytical applications. WM-1119, a chemical probe, is a highly potent and selective KAT6A inhibitor, with an IC₅₀ of 0.25 μM for KAT6A in lymphoma cells, the binding K_d values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.

Histone Acetyltransferase Inhibitor II (Standard) is the analytical standard of Histone Acetyltransferase Inhibitor II (HY-100734). This product is intended for research and analytical applications. 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.

EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC₅₀s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells.