at 6

AT6 is a PROTAC AT1 analog which is a highly selective bromodomain (Brd4) degrader.

KAT6-IN-2 is a potent inhibitor of KAT6, showing promise for use in cancer research.

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

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

KAT6-IN-3 (compound 10) competitively targets and binds to KAT6A and KAT6B.

KAT6A/KAT7-IN-3 (Example 191) is an inhibitor of KAT6A and KAT7. It exhibits an IC50 of 10-50 nM for KAT6A and 1 nM or less for KAT7. This compound inhibits acetylation of H3K14 and H3K23 and suppresses tumor cell proliferation, with an IC50 of 2-5 μM for CAMA-1. KAT6A/KAT7-IN-3 is applicable in cancer research.

STAT6-IN-7 (Compound 178) is a STAT6 inhibitor with an IC50 of 0.28 μM for inhibiting the binding of human STAT6/pIL-4Rα. It is utilized in research related to inflammation and allergic diseases.

KAT6A/KAT7-IN-2 (Example 177) is an inhibitor targeting KAT6A and KAT7, with an IC50 of 1 nM or less for both enzymes. It inhibits acetylation of H3K14 and H3K23 and also suppresses tumor cell proliferation, demonstrating an IC50 of 100 nM or less for CAMA-1 cells. This compound is applicable in cancer research.

KAT6A/KAT7-IN-4 (Example 230) is an inhibitor targeting KAT6A and KAT7, with an IC50 of less than or equal to 1 nM for both enzymes. It inhibits acetylation of H3K14 and H3K23 and suppresses tumor cell proliferation, specifically showing an IC50 of less than or equal to 100 nM for CAMA-1. This compound is useful in cancer research.

KAT6A/KAT7-IN-1 (Example 113) is an inhibitor targeting both KAT6A and KAT7. It shows an IC50 for KAT6A of greater than 1 nM and up to 10 nM, while for KAT7, the IC50 is 1 nM or less. This compound suppresses acetylation of H3K14 and H3K23. Additionally, KAT6A/KAT7-IN-1 inhibits tumor cell proliferation with an IC50 for CAMA-1 of more than 2 μM but no greater than 5 μM. It is applicable in tumor research.

NAT6-297775 is a SHP2 inhibitor with IC50 =2.47uM.

STAT6-IN-1, a STAT6 inhibitor, exhibits high affinity for the SH2 domain of STAT6 (IC 50 = 0.028 µM), making it suitable for research on allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease, or cancer.

KAT6-IN-1 (compound E) is a selective, orally available inhibitor of histone acetyltransferases KAT6A and KAT6B, exhibiting antitumour activity for cancer research.

STAT6-IN-2 (Comp R-84) is a STAT6 inhibitor that effectively reduces the secretion of the chemokine eotaxin-3, which induces eosinophil infiltration. This compound is valuable for studying immune diseases [1].

STAT6-IN-3 (Compound 18a) is an inhibitor of STAT6, targeting the Src Homology 2 (SH2) domain with an IC50 value of 44 nM. It is used in research on inflammatory disorders, such as asthma [1].

STAT6-IN-5 (example 84) is an inhibitor of STAT6 (IC50 = 0.24 μM), applicable for investigating inflammation and allergies such as atopic dermatitis.

STAT6-IN-4 (compound 78) is a STAT6 inhibitor with an IC₅₀ of 0.34 μM, suitable for investigating inflammatory and allergic diseases.

ESAT6 Epitope is a known CD4+ T cell epitope within the Early Secretory Antigenic Target 6 (ESAT6), demonstrating nanoscale affinity (IC50=180 nM) for Major Histocompatibility Complex MHC class I. Additionally, ESAT6 Epitope can enhance the anti-tuberculosis cellular immunity initiated by the Bacille Calmette-Guérin vaccine.

6PPD-Q (6PPD-Quinone) is an environmental pollutant that can target CNR2, CNR1, AA2AR, LCAT and TRPA1. Among them, CNR2 has the highest binding affinity and may act as a CNR2 receptor agonist to activate cannabinoid receptors. 6PPD-Q can damage the sperm quality and induce the impairment of male reproductive ability in mice. 6PPD-Q can induce intestinal inflammation and barrier damage by disrupting mitochondrial function, reducing neuronal glycolytic metabolites and TCA cycle intermediates, and exacerbating α-synuclein (α-syn) aggregation.

6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine) is a glutaminase antagonist (Ki: 6 μM) and an antineoplastic antibiotic produced by an unidentified Streptomyces species from Peruvian soil.

INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor that disrupts CN-NFAT signaling by targeting the NFAT(P) substrate at the calcineurin (CN) phosphatase site.

6-Chloromelatonin is a potent melatonin receptor agonist, a 5-methoxyindole compound that competes for presynaptic melatonin receptor sites in the rabbit retina, inhibiting the calcium-dependent release of [3H]dopamine with higher metabolic stability than melatonin. Chloromelatonin competitively binds to [3H]melatonin at MT2 receptors (pKi=9.77) and may be used to study insomnia and sleep disorders associated with depression.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

6-Methyl-5-azacytidine is a potent DNMT (DNA methyltransferase) inhibitor.