at6

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

KAT681 is a liver selective thyromimetic.

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.

STAT6-IN-8 is a highly selective STAT6 inhibitor (IC50=0.25 μM)that exerts potent anti-inflammatory and anti-allergic effects by blocking STAT6’s DNA-binding activity and its dimerization process. STAT6-IN-8 can be used in research on STAT6-related diseases such as atopic dermatitis, bronchial asthma, and allergic rhinitis.

STAT6-IN-9 is a highly potent STAT6 inhibitor with an EC₅₀ of 4 nM. It markedly blocks STAT6 activation mediated by the IL-13/IL-13 receptor/IL-4 receptor pathway and inhibits CCL17 secretion with an IC₅₀ of 4.6 nM. STAT6-IN-9 is suitable for studying various chronic inflammatory diseases related to the STAT6 signaling pathway, including allergic diseases, asthma, and chronic obstructive pulmonary disease.

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.

STAT6-IN-10 is a highly active signal transducer and activator of transcription 6 (STAT6) inhibitor with an EC₅₀ of 0.002 μM. It inhibits the secretion of CCL17 in human peripheral whole blood with an IC₅₀ of 0.095 μM and can be used in research on skin diseases and respiratory disorders.

STAT6-IN-11 is a STAT6 inhibitor with an EC₅₀ of 6 nM. It inhibits the secretion of CCL17 in human peripheral whole blood with an IC₅₀ of 83 nM through the IL-13–IL-13 receptor/IL-4 receptor pathway and can be used in research on skin diseases and respiratory diseases.

KAT6-IN-4 (Compound Example 2) is a selective inhibitor of lysine acetyltransferase 6 (KAT6). It inhibits the transcription of oncogenes such as ERα. In ER+/HER2- breast cancer xenograft models, KAT6-IN-4 demonstrates strong antitumor activity. This compound holds promise for research into KAT6-driven malignancies, such as breast cancer and non-small cell lung cancer.

(trans)-STAT6 modulator-5 (Compound 95) is a modulator of the STAT6 protein, inhibiting the STAT6 signaling pathway. This compound holds potential for the research of inflammatory diseases and allergic reactions.

PROTACSTAT6 degrader-1 (Compound I-2) is a STAT6 PROTAC degrader with a DC50 of less than 1 nM. This compound is utilized in the study of inflammation and cancer.

STAT6ligand-1 is a ligand for STAT6. It can be utilized in the synthesis of PROTACs, such as STAT6degrader-2.

STAT6ligand-1 is a ligand for STAT6. It can be used in the synthesis of PROTACs, such as Compound 22.

PROTACSTAT6 degrader-2 is a potent PROTAC degrader targeting STAT6. It exhibits a DC50 of 1-10 nM for STAT6 in human peripheral blood mononuclear cells (PBMC) and a DC50 of less than 100 nM in HEK293-HIBiT-STAT6 cells. PROTACSTAT6 degrader-2 is applicable for the treatment of diseases mediated by STAT6.

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.