HDAC1
HDAC1 is a class I histone deacetylase that supports transcriptional repression through histone deacetylase activity[1]. Mechanistically, HDAC1/2 form core catalytic components of corepressor complexes that modulate gene expression, linking chromatin regulation to proliferation and stem-cell self-renewal[2]. In human tumor cells, HDAC1 knockdown causes G1 or G2/M arrest, growth inhibition, loss of mitotic cells, and increased apoptosis[3]. In embryonic stem cells, HDAC1, but not HDAC2, is required for optimal corepressor-complex activity and cell-fate determination during differentiation[4]. Compared with HDAC2, HDAC1 shows nonredundant disease relevance in glioma stem cells, where its loss is not compensated by HDAC2 and affects the glioma stem-cell phenotype in a p53-dependent manner[5]. For experimental applications, selective HDAC1/2 inhibition suppresses colorectal cancer cells through apoptosis induction and cell-cycle regulation, supporting inhibitor use in pathway-focused cancer models[6].
Verweise:
- [1]. Hassig CA, et al. A role for histone deacetylase activity in HDAC1-mediated transcriptional repression. Proc Natl Acad Sci U S A. 1998 Mar 31;95(7):3519-24. [Content Brief]
- [2]. Jamaladdin S, et al. Histone deacetylase (HDAC) 1 and 2 are essential for accurate cell division and the pluripotency of embryonic stem cells. Proc Natl Acad Sci U S A. 2014 Jul 8;111(27):9840-5. [Content Brief]
- [3]. Senese S, et al. Role for histone deacetylase 1 in human tumor cell proliferation. Mol Cell Biol. 2007 Jul;27(13):4784-95. [Content Brief]
- [4]. Dovey OM, et al. Histone deacetylase 1 (HDAC1), but not HDAC2, controls embryonic stem cell differentiation. Proc Natl Acad Sci U S A. 2010 May 4;107(18):8242-7. [Content Brief]
- [5]. Lo Cascio C, et al. Nonredundant, isoform-specific roles of HDAC1 in glioma stem cells. JCI Insight. 2021 Sep 8;6(17):e149232. [Content Brief]
- [6]. Lee HY, et al. A novel HDAC1/2 inhibitor suppresses colorectal cancer through apoptosis induction and cell cycle regulation. Chem Biol Interact. 2022 Jan 25;352:109778. [Content Brief]
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HDAC1 Verwandte Produkte (317)
Verwandte Produkte (317)
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Antibodies (1)
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HDAC6-IN-31
0 ImagesArt. -Nr.: HY-161155HDAC6-IN-31 (compound 8m) is a selective HDAC6 inhibitor, with the IC50 value of 0.026 μM, that significantly inhibits the production and release of pro-inflammatory cytokines. While HDAC6 is critically involved in the activation of inflammasomes, HDAC6-IN-31 has the potential to inhibit NLRP3 inflammasome-driven inflammatory diseases. HDAC6-IN-31 also inhibits glioblastoma cell migration.
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HDAC-IN-42
0 ImagesArt. -Nr.: HY-147892CAS. Nr.: 2454024-18-9HDAC-IN-42 (compound 14f) is a potent and selective HDAC inhibitor with IC50 values of 0.19 and 4.98 µM for HDAC1 and HDAC6, respectively. HDAC-IN-42 shows anticancer and anti-proliferative activity. HDAC-IN-42 induces apoptosis and cell cycle arrest at G2/M phase.
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HDAC6-IN-87
0 ImagesArt. -Nr.: HY-189296CAS. Nr.: 3122437-17-3HDAC6-IN-87 is a selective HDAC6 inhibitor (IC50 = 4.29 nM). HDAC6-IN-87 weakly inhibits HDAC1 (IC50 = 749.59 nM), HDAC3 (IC50 = 813.09 nM), and HDAC10 (IC50 = 679.25 nM). HDAC6-IN-87 exhibits broad-spectrum antitumor activity, elevates α-tubulin acetylation levels without affecting histone H3 acetylation, and induces cell cycle arrest and apoptosis. HDAC6-IN-87 can be used for cancer-related research.
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Top/HDAC-IN-2
0 ImagesArt. -Nr.: HY-145852CAS. Nr.: 2775446-64-3
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KZL-064
0 ImagesArt. -Nr.: HY-189233CAS. Nr.: 2773345-67-6KZL-064 is an orally active HDAC1 ligand that directly binds to HDAC1. KZL-064 inhibits the proliferation, migration, and invasion of hepatocellular carcinoma cells, and induces apoptosis and G2/M phase cell cycle arrest. The antiproliferative, proapoptotic, and cell cycle regulatory effects of KZL-064 are partially dependent on HDAC1, while its inhibitory effects on migration and invasion also involve HDAC1-independent mechanisms. KZL-064 is applicable to hepatocellular carcinoma research.
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HDAC3-IN-8
0 ImagesArt. -Nr.: HY-181768CAS. Nr.: 2763368-90-5HDAC3-IN-8 is a selective inhibitor targeting HDAC1, HDAC2 and HDAC3, with IC50 values of 3.52 nM for HDAC1, 15.14 nM for HDAC2 and 0.38 nM for HDAC3. HDAC3-IN-8 shows high selectivity for HDAC3 and exerts its effect by inhibiting histone deacetylase activity. HDAC3-IN-8 can be used to construct HDAC3-targeted PROTAC degrader (HY-181767) and is suitable for the research of acute myeloid leukemia (AML).
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HDAC6-IN-45
0 ImagesArt. -Nr.: HY-161783CAS. Nr.: 3048532-05-1HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability.
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sEH/HDAC6-IN-1
0 ImagesArt. -Nr.: HY-163207CAS. Nr.: 2847838-67-7
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HDAC6-IN-38
0 ImagesArt. -Nr.: HY-163503CAS. Nr.: 3030872-95-5HDAC6-IN-38 (Compound Z-7) is an inhibitor for histone deacetylase 6 (HDAC6), with an IC50 of 3.25 nM. HDAC6-IN-38 inhibits proliferation of cells MGC 803.
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SH-17
0 ImagesArt. -Nr.: HY-187212SH-17 is a STAT3 and HDAC inhibitor, with a Kd of 0.87 μM for STAT3, and IC50 values of 115.2 nM and 9.8 nM for HDAC1 and HDAC6, respectively. SH-17 blocks intracellular ATP production and mitochondrial oxidative phosphorylation, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. SH-17 is applicable to colon cancer research.
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HDAC/Top-IN-1
0 ImagesArt. -Nr.: HY-144654CAS. Nr.: 2411379-14-9HDAC/Top-IN-1 is an orally active and pan HDAC/Top dual inhibitor with IC50s of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8. HDAC/Top-IN-1 efficiently induces apoptosis with S cell-cycle arrest in HEL cells. HDAC/Top-IN-1 has exhibits excellent in vivo antitumor efficacy.
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FLT3/HDAC-IN-3
0 ImagesArt. -Nr.: HY-181086CAS. Nr.: 2864394-30-7FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3D853Y (IC50 = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies.
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Andrographidine E
0 ImagesArt. -Nr.: HY-N16881CAS. Nr.: 113963-41-0Andrographidine E is a COX-2 (IC50 = 19 μM) and HDAC inhibitor, with high affinity for HDAC1 and HDAC3. Andrographidine E can specifically bind to macrophages and has potential immunotargeting properties. Andrographidine E can be used for studying inflammation.
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sEH/HDAC6-IN-2
0 ImagesArt. -Nr.: HY-159171CAS. Nr.: 3009011-58-6sEH/HDAC6-IN-2 is a potent dual soluble epoxide hydrolase (sEH) and HDAC6 inhibitor with IC50s of 0.9 nM, 46.8 nM, and 8 nM for human sEH, mouse sEH, and HDAC6, respectively. sEH/HDAC6-IN-2 can be used for the study of inflammatory pain.
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AMC-3-030
0 ImagesArt. -Nr.: HY-180934CAS. Nr.: 2926656-07-5AMC-3-030 is a selective and potent dual inhibitor targeting HDAC6 and chymotrypsin-like proteasome with IC50 values of 884 and 4.17 nM. AMC-3-030 has a proliferation inhibitory effect. AMC-3-030 can reduce α-tubulin and β-actin levels. AMC-3-030 can be used for research of multiple myeloma.
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HDAC1/6-IN-3
0 ImagesArt. -Nr.: HY-175176CAS. Nr.: 3038691-85-6HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.
