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].
References:
- [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 Related Products (316)
Related Products (316)
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Antibodies (1)
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HDAC-IN-27
0 ImagesHDAC-IN-27 (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC50 values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 can be used for research in acute myeloid leukemia (AML).
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JPS014
0 ImagesCat. No.: HY-145815CAS No.: 2669785-76-4JPS014 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 can be used for the research of colon cancer.
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CM-444
0 ImagesCat. No.: HY-163803CAS No.: 2256079-52-2CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.
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HDAC1/6-IN-1
0 ImagesCat. No.: HY-144725CAS No.: 2630989-02-3HDAC1/6-IN-1 (compound D7) is a potent multitarget inhibitor of GLP, HDAC6 and HDAC1, with IC50 values of 1.3, 13, and 89 nM, respectively. HDAC1/6-IN-1 can inhibit the methylation and deacetylation of H3K9 on protein level. HDAC1/6-IN-1 induces cancer cell apoptosis, G0/G1 cell cycle arrest, and blocks migration and invasion.
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HDAC6-IN-49
0 ImagesCat. No.: HY-169156HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC50 of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models.
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HDAC6-IN-74
0 ImagesCat. No.: HY-181579HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.
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M122
0 ImagesCat. No.: HY-125645CAS No.: 2127411-50-9
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HDAC1-IN-15
0 ImagesCat. No.: HY-187346CAS No.: 3055432-86-2HDAC1-IN-15 is a HDAC1 inhibitor with activity against hHDAC1, PfHDAC1 and HDAC8. HDAC1-IN-15 inhibits the proliferation of asexual blood-stage Plasmodium falciparum and reduces the survival rate of stage IV-V gametocytes of Plasmodium falciparum. HDAC1-IN-15 is applicable to malaria-related research.
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HDAC1-IN-12
0 ImagesCat. No.: HY-181010HDAC1-IN-12 is a Plasmodium falciparum HDAC1 (PfHDAC1) inhibitor with an IC50 of 4.1 nM against Pf3D7. HDAC1-IN-12 inhibits PfHDAC1, upregulates histone H3 acetylation in P. falciparum parasites, downregulates malaria invasion-related gene expression, and exhibits favorable safety profiles, improved physicochemical properties, and potent in vivo antimalarial activity. HDAC1-IN-12 can be used for the research of malaria.
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Azumamide E
0 ImagesCat. No.: HY-P2044CAS No.: 585535-37-1Azumamide E is a HDAC inhibitor, with an IC50 of 0.064 μM against HDAC, 1.22 μM against HDAC1, and 2.28 μM against HDAC4. Azumamide E inhibits HDAC activity in nuclear extracts of leukemia cells and cervical adenocarcinoma cells. Azumamide E suppresses angiogenesis. Azumamide E is applicable for research on leukemia, cervical adenocarcinoma, and anti-angiogenesis.
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β-Hydroxymethyl chalcone
0 ImagesCat. No.: HY-118394CAS No.: 1613310-15-8β-Hydroxymethyl chalcone is a time-dependent selective HDAC2 inhibitor, with IC50 values of 0.17 μM (24 h) and 9.19 μM (1 h). After binding to the catalytic zinc ion in the active pocket of HDAC2, β-Hydroxymethyl chalcone undergoes an intramolecular nucleophilic attack to form a cyclic product, resulting in time-dependent tight binding. β-Hydroxymethyl chalcone can be used for the study of HDAC2 selective inhibition and related epigenetic targets[1].
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BG47
0 ImagesCat. No.: HY-117583ACAS No.: 1628784-54-2BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. BG47 can be used for neurological disease research.
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CRA-026440
0 ImagesCat. No.: HY-19754CAS No.: 847460-34-8CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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TW9
0 ImagesCat. No.: HY-155222CAS No.: 2614417-90-0TW9 is a potent dual inhibitor simultaneously targeting BET and HDAC proteins with KDs of 0.069 μM, 0.231 μM for BRD4(1), BRD4(2), and an IC50 of 0.29 μM for HDAC1, respectively. TW9 is a newly generated adduct of the BET inhibitor (+)-JQ1 (HY-13030) and class I HDAC inhibitor CI994 (HY-50934). TW9 shows high potency in suppressing tumor growth in pancreatic ductal adenocarcinoma (PDAC). TW9 improves the efficacy of the chemotherapeutic agent Gemcitabine (HY-17026).
