Histone Acetyltransferase Inhibitor

KAT6A-IN-2 (compund 7) is a KAT6A inhibitor.

SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor extracted from patent WO2019201291A1.

KAT6-IN-3 (compund 10) competitively targets KAT6A and KAT6B.

Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity.

Y08175 is a potent CBP bromodomain inhibitor. Y08175 exhibits considerable inhibitory effect with IC₅₀s of 37 and 178.15 nM against CBP bromodomain in AlphaScreen assay and HTRF assay, respectively. Y08175 can be used for the research of prostate cancer.

ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC₅₀ value of 0.035 nM and a CBP DC₅₀ value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.

KAT6-IN-2 (Compound 25) is a potent KAT6 inhibitor. KAT6-IN-2 is promising for research of cancers.

CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC₅₀ = 0.034 μM, CBP IC₅₀ = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC₅₀ values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.

CZL-046 (compund 29) is an oral p300 bromodomain inhibitor.

PRMT/HKMT-IN-1 is an epigenetic multi-target protein arginine methyltransferases (PRMTs) and histone lysine methyltransferases (HKMTs) inhibitor. PRMT/HKMT-IN-1 inhibits Aspergillus nidulans RmtA with an IC₅₀ of 29 μM. PRMT/HKMT-IN-1 inhibits human PRMT1, p300/CBP HAT, CARM1, SET7, SIRT1 and SIRT2. PRMT/HKMT-IN-1 inhibits methylation of histone H3K4, H4R3, and H3R17 residues. CBP/p300-IN-23 induces apoptosis, arrests cell cycle in S phase, and triggers granulocytic differentiation in leukemia cells. PRMT/HKMT-IN-1 can be used for the research of leukemia.

Anacardic Acid (Standard) is the analytical standard of Anacardic Acid. This product is intended for research and analytical applications. Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC₅₀s of ～8.5 μM and ～5 μM, respectively.

KAT6-IN-4 (Compound Example 2) is a selective lysine acetyltransferase 6 (KAT6) inhibitor. KAT6-IN-4 suppresses transcription of oncogenes like ERα. KAT6-IN-4 demonstrates potent antitumor efficacy in ER⁺/HER2^- breast cancer xenografts. KAT6-IN-4 is promising for research of KAT6-driven malignancies (e.g., breast cancer, NSCLC).

HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.

Ep300/CREBBP-IN-8 (Example 37) is a potent and orally active Ep300 and CREBBP inhibitor with IC₅₀s of 0.014 and 0.018 μM, respectively. Ep300/CREBBP-IN-8 can be used for the research of cancer.

P300-IN-4 (compound 6) is a (p300) inhibitor with the IC₅₀ of 12.2 μM.

CCT077791 is a PCAF (IC₅₀: 7.3 μM (FlashPlate); 2.2 μM (Filter assay)) and p300 histone acetyltransferase inhibitor. CCT077791 reduces total acetylation of histones H3 and H4, levels of specific acetylated lysine marks, and acetylation of α-tubulin. CCT077791 can be used in the research of colorectal cancer.

CBP/p300-IN-22 is a selective CBP/EP300-BRD inhibitor with an IC₅₀ of 4 nM. CBP/p300-IN-22 is highly selective over BRD4(1). CBP/p300-IN-22 reduces TNF-α-induced cytokine expression and subsequent immune cell recruitment by inhibiting NF-κB signaling, and has anticancer activity. CBP/p300-IN-22 can be used for the research of rheumatoid arthritis (RA) and other TNF-α-mediated inflammatory conditions.

KAT5 Human Pre-designed siRNA Set A contains three designed siRNAs for KAT5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC₅₀s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity.

Remodelin (Standard) is the analytical standard of Remodelin (HY-16706). This product is intended for research and analytical applications. Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.