Histone acetyltransferases (HATs) are epigenetic proteins that attach acetyl groups to lysine residues in cellular proteins like histones, transcription factors, nuclear receptors, and enzymes. In eukaryotic cells, HATs are essential for chromatin remodeling and transcriptional control. Through the acetylation of both histone and non-histone proteins, HATs have been shown to play a role in diseases ranging from cancer and inflammatory disorders to neurological disorders.
At least five different subfamilies of HATs (HAT1, Gcn5/PCAF, MYST, p300/CBP, and Rtt109) can be distinguished. HATs mediate a wide range of biological functions, such as hormone signaling, dosage adjustment, DNA damage repair, and cell cycle progression. A number of human diseases, such as solid tumors, leukemias, inflammatory lung disease, viral infection, diabetes, fungus infection, and drug addiction, are associated with abnormal HAT function.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V88875 | (E/Z)-NiCur | 63476-70-0 | (E/Z)-NiCur is the active isomer of NiCur. |
|
V107451 | 3,5-DMA hydrochloride | 24973-29-3 | |
|
V9859 | A-485 | 1889279-16-6 | A-485 (A485) is a potent, drug-like and selective HAT (histone acetyltransferase) inhibitor of p300/CBP with potential antitumor activity. |
|
V84850 | Antitumor agent-130 | ||
|
V103705 | BAY-184 | 2520347-03-7 | |
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V2519 | C646 | 328968-36-1 | C646 is a potent, selective and competitive inhibitor for histone acetyltransferase p300. |
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V88873 | CAY10669 | 1243583-88-1 | CAY10669 (compound 6d) is an Anacardic Acid derivative that inhibits histone acetyltransferase (PCAF) with IC50 of 662 μM. |
|
V52296 | CBP/p300-IN-10 | 2259641-71-7 | CBP/p300-IN-10 is a potent inhibitor of histone acetyltransferases EP300 and CREBBP, with IC50s of 26 nM and 39 nM respectively. |
|
V41054 | CBP/p300-IN-5 | 1889284-33-6 | P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase with IC50 of 18.8 nM. |
|
V88866 | CBPD-268 | CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with a DC50 value of ≤ 0.03 nM. | |
|
V88871 | CPTH2-Alkyne | 1613116-16-7 | CPTH2-Alkyne is a cell-active analog of CPTH2. |
|
V97364 | dCE-2 | dCE-2 (compound 5) is a PROTAC targeting CREB binding protein (CBP) and E1A-related protein (EP300) and was developed based on the crystal structure of a bromodomain (BRD) inhibitor. | |
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V52155 | DS-9300 | 2259641-46-6 | DS-9300 is a potent, orally bioactive and selective EP300/CBP HAT inhibitor (antagonist) with IC50 of 28 nM. |
|
V52120 | Ep300/CREBBP-IN-2 | 2259641-59-1 | Ep300/CREBBP-IN-2 (Example 73) is a potent and orally bioactive inhibitor of Ep300 and CREBBP with IC50 of 0.052 μM and 0.148 μM, respectively. |
|
V52119 | Ep300/CREBBP-IN-3 | 2259641-47-7 | Ep300/CREBBP-IN-3 (Example 61) is a potent Ep300 and CREBBP inhibitor (antagonist) with IC50 of 0.056 μM and 0.095 μM, respectively. |
|
V52118 | Ep300/CREBBP-IN-4 | 2259641-42-2 | Ep300/CREBBP-IN-4 (Example 56) is a potent inhibitor of Ep300 and CREBBP with IC50 of 0.024 μM and 0.064 μM, respectively. |
|
V52117 | Ep300/CREBBP-IN-8 | 2259641-24-0 | Ep300/CREBBP-IN-8 (Example 37) is a potent and orally bioactive inhibitor of Ep300 and CREBBP with IC50 of 0.014 μM and 0.018 μM, respectively. |
|
V2998 | I-CBP112 | 1640282-31-0 | I-CBP112 (I-CBP-112) is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor (PPI) with anticancer activity. |
|
V75851 | JG-2016 | 2887480-87-5 | JG-2016 is a potent inhibitor of histone acetyltransferase 1 (HAT1) with IC50 of 14.8 μM in HAT1 acetylation assay[1]. |
|
V51910 | KAT modulator-1 | 1314006-43-3 | KAT modulator-1 (Compound 3) is a KAT modulator. |
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