Histone Acetyltransferases

NSC 694623 is a potent inhibitor of histone acetyltransferases (HATs), with an IC50 value of 15.9 μM for recombinant p300/CBP-associated factor (PCAF). This compound exhibits antiproliferative effects on various cancer cell lines, making it a valuable tool for cancer research. Its capacity to modulate histone acetylation offers potential insights into epigenetic regulation and therapeutic strategies in oncology.

CBP/p300-IN-19 hydrochloride is a selective inhibitor of the histone acetyltransferases (HAT) p300 and CBP, exhibiting IC50 values of 1.4 µM and 2.2 µM, respectively. It demonstrates significant antitumor activity, making it a valuable tool for cancer research. This compound can be applied in studies investigating the roles of acetylation in gene regulation and cell proliferation, as well as in the development of targeted therapies.

NiCur is a potent and selective inhibitor of CBP histone acetyltransferase (HAT) with an IC50 value of 0.35 μM. By targeting CBP HAT activity, NiCur effectively downregulates p53 activation in response to genotoxic stress. This compound is suitable for mechanistic studies, allowing researchers to investigate pathways involving histone acetylation without altering the expression of target proteins.

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.

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.

Naa50-IN-1 is a potent inhibitor of N-alpha-acetyltransferase 50 (Naa50), exhibiting an IC50 of 7 nM against the human enzyme. This compound shows selectivity for related acetyltransferases, Naa10 and Naa60. Naa50-IN-1 interacts with the substrate-binding pocket of Naa50, with its binding affinity augmented by the presence of AcCoA, making it a valuable tool for investigating the biological roles of protein acetylation. Research applications include studies on gene regulation and enzyme activity related to Naa50 and its substrates.