Histone Acetyltransferase Inhibitor

Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.

Y08262 is a potent and selective CBP bromodomain inhibitor. Y08262 selectively inhibits the CBP bromodomain with an IC₅₀ value of 73.1 nM. Y08262 can be used for the research of acute myeloid leukemia (AML).

P300-IN-2 is a p300 inhibitor (IC₅₀=3.6 μM) that inhibits histone acetyltransferase p300 activity. P300-IN-2 shows weak inhibitory activity against CWR22RV1 cell proliferation. P300-IN-2 can be used for research on p300-mediated diseases, such as cancer.

CPTH2-d₄ is the deuterated-labeled CPTH2 (HY-W013274). CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B).

KCN1 is a p300/HIF-1α interaction inhibitor with a K_d value of 345 nM for p300-CH1. KCN1 binds to the CH1 domain of p300, blocks the assembly of the p300/HIF-1α complex, and disrupts the HIF-1α-p300/CBP interaction. KCN1 inhibits cancer cell growth, induces cancer cell cycle arrest and apoptosis. KCN1 inhibits β-galactosidase activity and downregulates the expression of VEGF, Glut1, CA9 and CAIX. KCN1 exerts anticancer activity in mouse tumor xenograft models. KCN1 can be used in research related to malignant glioma, pancreatic cancer and metastatic uveal melanoma.

Antitumor agent-130 (Compound 7b) is a p300 histone acetyltransferases (HAT) inhibitor with an IC₅₀ of 1.51 μM. Antitumor agent-130 combinates with doxorubicin (HY-15142A) can significantly inhibit tumor growth and invasion in vitro and in vivo.

KAT6A-IN-1 is a KAT6A inhibitor with an IC₅₀ of <10 μM. KAT6A-IN-1 can be used for the research of cancer.

Y16524 is a potent inhibitor of CBP/p300 bromodomain , with the IC₅₀ of 0.01 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).

KAT6A/B-IN-1 is a KAT6A/KAT6B inhibitor (IC₅₀ = 3.2 nM and 25.2 nM) that inhibits lysine acetyltransferase activity. KAT6A/B-IN-1 inhibits cancer cell proliferation and tumor growth in xenograft models. KAT6A/B-IN-1 exhibits chemical and physical stability, low hygroscopicity, and reduced sensitivity to heat, humidity, and light. KAT6A/B-IN-1 is used in the study of breast cancer.

ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer.

Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC₅₀s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer.

CoA-C2-SGRGK-cCPP is a NatD (NAA40) bisubstrate inhibitor with an IC₅₀ of 78 nM and a K_i of 39 nM. CoA-C2-SGRGK-cCPP competitively targets the peptide substrate binding site and noncompetitively targets the CoA binding site of NatD to block acetyltransferase activity. CoA-C2-SGRGK-cCPP reduces cellular Nα-acetylation on histone H4, modulates EMT marker expression. CoA-C2-SGRGK-cCPP can be used for the research of non-small cell lung cancer.

CBP/p300-IN-17 (compound 7) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.18, 0.69 µM for HAT EP300 and LK2 H3K27, respectively.

ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G₂/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach.

BAY-7728 is an orally active and selective dual inhibitor of KAT6A (IC₅₀: 45 nM)/KAT6B (IC₅₀: 95 nM). BAY-7728 can effectively inhibit tumor growth and regulate the acetylation level of histone H3K23. BAY-7728 can be used for tumor research.

NSC 698600 is a potent PCAF inhibitor, with IC₅₀ of 6.51 µM (PCAF/H3_1-21). NSC 698600 exhibits good activity of inhibiting the proliferation of cancer cells.

DC-CPin7 is a potent inhibitor of CREB-binding protein (CBP) bromodomain with an IC₅₀ of 2.5 μM.

P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC₅₀ values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma.

iP300w (Compound 9) is a Histone acetyltransferase p300 (KAT3B) inhibitor. iP300w can be used for synthesis of PROTAC BT-O2C (HY-174866).

Y16526 is a potent inhibitor of CBP/p300 bromodomain , with the IC₅₀ of 0.03 μM. Y16524 has the potential for the research of acute myeloid leukemia (AML).