kat6a

WM-1119 is a highly potent, selective KAT6A/B inhibitor

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.

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.

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.

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

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

PF-9363 (CTX-3648) is a potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer.

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

BAY-184 is a selective oral inhibitor of KAT6A and KAT6B with IC50 values of 71 nM and 83 nM, respectively. This compound suppresses estrogen receptor α (ERα) transcriptional activity and impedes cell proliferation across various breast cancer subtypes as well as tumor growth.

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

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].

MW-2474 is an inhibitor of the lysine acetyltransferase KAT6A.