histoneacetyltransferase

A-485 is a potent and selective catalytic p300 CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP.

Acetaminophen (APAP) is a COX inhibitor that inhibits COX-1 and COX-2 (IC50=113.7 25.8 μM). Acetaminophen has antipyretic and analgesic activity as well as weak anti-inflammatory activity.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300 CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

NU 9056 is an effective and selective inhibitor of KAT5 histone acetyltransferase with an IC50 of 2 µM. NU 9056 blocks DNA damage response and inhibits protein acetylation in prostate cancer cell lines.

Remodelin is an effective and specific inhibitor of the acetyl-transferase protein NAT10.

CPI-637 is a selective and cell-active benzodiazepinone CBP EP300 bromodomain inhibitor.

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. 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.

C646, a histone acetyltransferase inhibitor, inhibits p300 (Ki: 400 nM, in a cell-free assay).

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor targeting the CBP p300 bromodomains.

Remodelin hydrobromide (Remodelin HBR) is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.

MOZ-IN-3 (Compound 6j), a potent KAT6A (MOZ) acetyltransferase inhibitor with an IC50 of 30 nM, exhibits antitumor activity against multiple myeloid leukemia cell lines, including HL-60, U937, SKNO-1, and K562. This compound also demonstrates favorable metabolic stability and pharmacokinetics [1].

KAT modulator-1 (Compound 3), an epigenetics research tool, selectively interacts with the full-length p300 protein but not its catalytic domain [1].

CPTH2 is a histone acetyltransferase inhibitor modulating Gcn5 network.

CTX-0124143 is a histone acetyltransferase inhibitor with an IC50 value of 1.0 μM for KAT6A.CTX-0124143 can be used to study cellular senescence.

NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 of 15.9 μM against recombinant HAT p300 CBP-associated factor (PCAF) and exhibits anti-proliferative activity against certain cancer cells, making it useful for anti-cancer research.

dWIZ-1 ((rac)-dWIZ-1) is a potent WIZ molecular gel degrader that recruits WIZ (ZF7) to the cereblon thereby inducing degradation and thus induction of haemoglobin fetalis (HbF) in erythroblasts, which can be used to study sickle cell disease (SCD).

KAT6A-IN-2 (compound 7) is an inhibitor of KAT6A.

KAT6A-IN-1 (compound 5) is an inhibitor of KAT6A.

WIZ degrader 8 (compound 10) is a potent and selective molecular glue degrader of the transcription factor WIZ, effectively inducing HbF expression. It promotes WIZ degradation and HbF induction, suggesting its potential use as an inhibitor for sickle cell disease.

AUR1545 is a compound that selectively degrades KAT2A and KAT2B. It is applicable in cancer research, including studies on AML, SCLC, and NEPC.

NSC 228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulating EGFR tyrosine phosphorylation.

CCT077791 is a potent inhibitor of p300 and PCAF histone acetyltransferase activity for cancer research.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.