Chromatin/Epigenetics

Anemonin, a furanone dimer from Buttercups, may help manage melanocytes and osteoarthritis.

EZH2-IN-5, potent EZH2 inhibitor; IC50: 1.52 nM (wild-type), 4.07 nM (Tyr641 mutant).

4-PivO-NMT chloride is an indole derivative-based regulator of the AMPK signaling pathway. It modulates neurogenesis or neurite outgrowth by influencing AMPK activity and holds potential for research in neurological disorders, pain, and inflammation.

MAK683-CH2CH2COOH, an EED binder, was key in crafting PROTAC EED degrader-1 and -2 targeting VHL-E3 ligase.

HDAC-IN-80 (compound 5) is a selective inhibitor of class I HDAC.

PROTAC BRD4 Degrader-8: BRD4 inhibitor with IC50s of 1.1/1.4 nM for BD1/BD2, degrades BRD4 in PC3 cells.

GSK9311 hydrochloride is a less active GSK6853 analog, serving as a negative control, inhibiting BRPF1/2 (pIC50: 6.0/4.3).

PF-3166 (compound PF-3166) is a cell-active inhibitor of PAD2.

NUCC-0226272, a potent PROTAC, induces the degradation of EZH2 and exhibits anti-proliferative effects. It holds promise for application in cancer research [1].

Fluorescein NAD+ is a non-radioactive PARP assay substrate, enabling direct enzyme measurement by fluorescence. Comes as 81μg in 250μl water.

PROTAC BRD9 binder moiety 5 selectively binds BRD9 with IC50 4.20μM, used in PROTAC synthesis, shows cancer cell antiproliferative activity.

PROTAC BRD4 Degrader-5-CO-PEG3-N3 is a PROTAC-linker conjugate for PAC. PROTAC BRD4 Degrader-5-CO-PEG3-N3 comprises the BRD4 degrader GNE-987 linked through a PEG-based spacer to enable modular bioconjugation. PROTAC BRD4 Degrader-5-CO-PEG3-N3 functions as a click-chemistry reagent containing an azide group capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-bearing molecules. PROTAC BRD4 Degrader-5-CO-PEG3-N3 can also react through strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO- or BCN-containing compounds, thereby supporting targeted PROTAC assembly and bioconjugation for chemical biology and drug-discovery applications.

A compound inhibits EZH2, overexpressed in cancers, affecting Treg activity and innate immunity.

Ethyl 2-amino-4-methyl-5-thiophene carboxylate is a SETD7 inhibitor (IC50=4.59μM) with anticancer properties.

PROTAC SMARCA2/4-degrader-28 (PROTAC 1) functions as a partial degrader of SMARCA2 and SMARCA4 through the PROTAC-based mechanism.

CBP/p300-IN-14, patent WO2021213521A1's compound 27, inhibits CBP/EP300 with 3.3 nM IC50.

RBN012811 is a PROTAC specifically targeting PARP14.

CEM114 is a potent chemical compound known as a chemical epigenetic modifier (CEM).

Curcuphenol in concentrations in the range of 29-116 μg/ml inhibited cell proliferation and DNA replication and induced cell death in a dose-dependent manner.

AUR1545 is a selective KAT2A/KAT2B degradator, inhibitory against AML, SCLC, and NEPC, and suppressing tumour growth in the NCI-H1048 xenograft model.