Histone Acetyltransferases

SYY-B029-2 is a potent inhibitor of histone acetyltransferases (HATs), exhibiting an IC50 of 1.4 nM. This compound demonstrates significant anti-proliferative effects on human mantle cell lymphoma (MCL) cell line MAVER-1 and human castration-resistant prostate cancer cell line LNCaP clone FGC, with IC50 values of 15 nM and 13 nM, respectively. SYY-B029-2 serves as a valuable tool for research into epigenetic regulation and cancer therapy.

B026 is a selective and potent inhibitor of the p300/CBP histone acetyltransferase (HAT) with IC50 values of 1.8 nM for p300 and 9.5 nM for CBP. This compound exhibits significant anticancer activity against androgen receptor-positive (AR+) prostate cancer cell lines, making it a valuable tool for research in cancer biology and epigenetic regulation. Its oral bioavailability enables easy administration for in vivo studies targeting p300/CBP-mediated pathways.

CBP/p300-IN-18 is a potent inhibitor of the EP300 and CBP histone acetyltransferases (HATs), exhibiting IC50 values of 0.056 µM and 0.46 µM for EP300 and LK2 H3K27, respectively. This compound serves as a valuable tool for investigating the role of histone acetylation in various biological processes and disease states. It is particularly useful in studies focused on chromatin remodeling, gene expression, and potential therapeutic applications in cancer and other disorders associated with dysregulated acetylation.

CBP/p300-IN-21 is a selective inhibitor of the CBP/p300 transcriptional co-activators, exhibiting IC50 values of 0.07 μM for p300 and 1.755 μM for CBP. This compound effectively reduces the acetylation level of histone H3 at lysine 18 (H3K18Ac), implicating a potential role in modulating gene expression. Furthermore, CBP/p300-IN-21 has demonstrated efficacy in inhibiting the growth of 4T1 tumors in murine models, highlighting its relevance in cancer research and therapeutic applications.

CBP/p300-IN-15 is a potent inhibitor of the CBP/p300 coactivators, exhibiting IC50 values of 2.50 nM for p300 and 28.0 nM for CBP. This compound demonstrates significant biological activity in ovarian cancer cell lines, with EC50 values of 0.865 μM for OVCAR-3 and 2.71 μM for A2780. CBP/p300-IN-15 is a valuable tool for investigating the role of CBP/p300 in ovarian cancer research and could provide insights into therapeutic strategies targeting these coactivators.

Ep300/CREBBP-IN-3 is a potent inhibitor of the Ep300 and CREBBP enzymes, demonstrating IC50 values of 0.056 μM and 0.095 μM, respectively. This compound is primarily utilized in cancer research, facilitating investigations into the role of histone acetylation in tumor progression and therapy resistance. Its ability to selectively inhibit these acetyltransferases makes it a valuable tool for understanding the epigenetic regulation of gene expression in oncology.

PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor that specifically targets Gcn5, p300/CBP-associated factor (PCAF), CREB-binding protein (CBP), and p300. This compound demonstrates inhibitory activity with IC50 values of 8.39 μM, 9.74 μM, 2.49 μM, and 5.35 μM for each respective HAT. PU139 is valuable for research applications exploring histone acetylation and its roles in gene regulation, cellular signaling, and cancer biology.

CTB is a potent activator of the p300 histone acetyltransferase, known for its role in regulating gene expression through histone acetylation. This compound has demonstrated the ability to induce apoptosis in MCF-7 breast cancer cells, making it a valuable tool for research into cancer biology and therapeutic approaches targeting acetylation pathways. Its specificity for p300 highlights its potential in studies of transcriptional regulation and chromatin dynamics.

TH1834 is a selective inhibitor of the Tip60 (KAT5) histone acetyltransferase (HAT). This compound has demonstrated the ability to induce apoptosis and enhance DNA damage in breast cancer cells. Notably, TH1834 does not interfere with the activity of the related MOF HAT, making it a valuable tool for investigating the role of Tip60 in cancer biology and exploring potential therapeutic applications.

TH1834 dihydrochloride is a selective inhibitor of Tip60 (KAT5), a histone acetyltransferase involved in the regulation of gene expression and DNA repair. This compound has been shown to induce apoptosis and enhance DNA damage in breast cancer cells, demonstrating its potential as a therapeutic agent in cancer research. Importantly, TH1834 dihydrochloride does not inhibit the activity of the structurally related histone acetyltransferase MOF, suggesting a targeted approach in modulating histone acetylation and cellular responses.

RU-SKI 43 hydrochloride is a selective inhibitor of Hedgehog acyltransferase (Hhat) with an IC50 of 850 nM. This compound effectively reduces Gli-1 activation via Smoothened-independent, non-canonical signaling pathways and inhibits Akt and mTOR pathway activity. RU-SKI 43 hydrochloride demonstrates promising anti-cancer effects, making it a valuable tool for research in cancer biology and targeted therapy.

RUSKI-201 dihydrochloride is a potent and selective inhibitor of Hedgehog acyltransferase (Hhat), demonstrating an IC50 of 0.20 μM. This compound effectively blocks Hedgehog signaling in cells overexpressing Sonic Hedgehog (Shh) and inhibits the palmitoylation process essential for Hh function. RUSKI-201 dihydrochloride serves as a valuable chemical probe for investigating Hhat catalytic activity in cellular studies, providing insights into the mechanisms of Hedgehog signaling.

IMP-1575 is a potent inhibitor of Hedgehog acyltransferase (HHAT), demonstrating an IC50 value of 0.75 μM against purified HHAT. This compound is valuable for research focused on cancer, particularly in studies exploring the role of the Hedgehog signaling pathway in tumorigenesis. Its specificity and efficacy make it a significant tool for investigating HHAT-related biological processes and potential therapeutic applications.

RUSKI-201 is a specific inhibitor of Hedgehog acyltransferase (Hhat), exhibiting an IC50 of 0.20 μM. This compound effectively disrupts Hedgehog (Hh) signaling in cells that overexpress Sonic Hedgehog (Shh) and inhibits the palmitoylation of Hh. RUSKI-201 serves as a valuable chemical probe for investigating Hhat catalytic function and its role in cellular signaling pathways.