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 (317)
Related Products (317)
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Antibodies (1)
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HDAC-IN-98
0 ImagesHDAC-IN-98 is a HDAC1, HDAC2, HDAC3 inhibitor (one of the most selective class I HDAC inhibitors) with human IC50 values of 41.2 nM, 52.5 nM, and 74.3 nM respectively. HDAC-IN-98 induces H3K9 acetylation, p21 upregulation, G2/M arrest, cell apoptosis, has strong antiproliferative effects in colorectal cancer cells, low toxicity in healthy colon epithelium, modulates short-term in vitro effects via autophagy, and shows strong antitumor efficacy in vivo in the chorioallantoic membrane model (CAM) assay. HDAC-IN-98 can be used for the research of colorectal cancer.
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KH-259
0 ImagesCat. No.: HY-150503CAS No.: 3023019-93-1
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PIM-1/HDAC-IN-2
0 ImagesCat. No.: HY-174302CAS No.: 3103925-33-0PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
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NN-390
0 ImagesCat. No.: HY-143877CAS No.: 2490284-25-6NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
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HDAC-IN-104
0 ImagesCat. No.: HY-184574HDAC-IN-104 is a potent and selective class I Histone deacetylases (HDAC) inhibitor with an IC50 of 25 nM. HDAC-IN-104 exerts potent antiproliferative and antitumor effects by inhibiting glycolysis and OXPHOS via blockade of the PI3K/AKT signaling pathway, and these effects are synergistically enhanced when combined with the FMS-like tyrosine kinase 3 (FLT3) inhibitor Quizartinib (AC220) (HY-13001). HDAC-IN-104 induces significant early and late apoptosis. HDAC-IN-104 can be used for acute myeloid leukemia (AML) research.
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G4/HDAC-IN-1
0 ImagesCat. No.: HY-151263CAS No.: 3031784-60-5G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer.
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HDAC8-IN-17
0 ImagesCat. No.: HY-187382HDAC8-IN-17 is a histone deacetylase 8 inhibitor with human IC50 values of 0.08 μM, 0.44 μM, and 1.9 μM, and high selectivity over HDAC1, HDAC2, HDAC3, and HDAC6. HDAC8-IN-17 exhibits slow-binding, reversible uncompetitive inhibition via allosteric binding to the enzyme-substrate complex. HDAC8-IN-17 induces selective hyperacetylation of SMC3. HDAC8-IN-17 can be used for the research of cancer.
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HDAC6/HSP90-IN-1
0 ImagesCat. No.: HY-146293CAS No.: 2411955-43-4HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice.
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HDAC6-IN-63
0 ImagesCat. No.: HY-178022HDAC6-IN-63 (Compound 7) is an orally active HDAC6 inhibitor with an IC50 of 145 nM. HDAC6-IN-63 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC6-IN-63 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC6-IN-63 can be used for chemotherapy of cancers like NSCLC research.
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IMPDH II/HDAC1-IN-1
0 ImagesCat. No.: HY-174221IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active, selective dual IMPDH II/HDAC1 inhibitor, with an IC50 of 84.69 nM against hIMPDH II and an IC50 of 81.75 nM against HDAC1. IMPDH II/HDAC1-IN-1 inhibits the proliferation of chronic myeloid leukemia cells. IMPDH II/HDAC1-IN-1 can be used for the research of chronic myeloid leukemia.
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HDAC-IN-37
0 ImagesCat. No.: HY-146750CAS No.: 2766466-56-0
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HDAC6-IN-47
0 ImagesCat. No.: HY-163834HDAC6-IN-47 (Compound S-29b) is inhibitor for HDAC, which exhibits high affinities to HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 with Ki of 60, 56, 162, 0.44, 362 and 849 nM, respectively. HDAC6-IN-47 causes tubulin hyperacetylation in MV4-11, inhibits the proliferation of MV4-11 with an EC50 of 0.50 µM. HDAC6-IN-47 can be used in research of leukemia.
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GSK-3β/HDAC-IN-2
0 ImagesCat. No.: HY-174398GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.
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HDAC-IN-31
0 ImagesCat. No.: HY-144293CAS No.: 1916505-13-9HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma.
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cGAS/HDAC-IN-1
0 ImagesCat. No.: HY-184398cGAS/HDAC-IN-1 is an orally active dual cGAS/HDAC inhibitor that exhibits potent inhibitory activity against human and mouse cGAS (IC50: 0.17 and 1.80 μM, respectively) and moderate activity against HDAC3 and HDAC6 (IC50: 1.2 and 0.4 μM, respectively). cGAS/HDAC-IN-1 directly suppresses cGAS activity and increases its acetylation levels via HDAC3 inhibition. cGAS/HDAC-IN-1 is effective in murine models of inflammatory bowel disease and Aicardi-Goutières syndrome, and can be used in research on cGAS-dependent disorders.
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F2F-202
0 ImagesCat. No.: HY-184165F2F-202 is a selective HDAC6 inhibitor with an IC50 of 7.1 nM, exhibiting high selectivity toward HDAC1. F2F-202 does not directly bind to or inhibit the Hda1 protease activity of Candida albicans itself, but reduces the mRNA transcription level of the Hda1 gene. When combined with Voriconazole (HY-76200), F2F-202 decreases the yeast-hypha transition rate of azole-resistant Candida albicans and impairs the antioxidant response of azole-resistant Candida albicans. F2F-202 can be used in studies related to azole-resistant Candida albicans infections.
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SHN7
0 ImagesCat. No.: HY-184706CAS No.: 3126116-06-8SHN7 is a selective HDAC1/HDAC6 inhibitor, NQO1 substrate and ROS inducer, with an IC50 of 30 nM against HDAC1 and an IC50 of 10 nM against HDAC6. SHN7 inhibits STAT3 with a Kd of 8.9 μM. SHN7 arrests the cell cycle at the G2/M phase and induces Apoptosis. SHN7 exhibits anti-tumor effects in triple-negative breast cancer (TNBC) xenograft models. SHN7 can be used for the research of triple-negative breast cancer.
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HDAC ligand-5
0 ImagesCat. No.: HY-168864HDAC ligand-5 is a template for the non-selective HDAC inhibitor Vorinostat (HY-10221). HDAC ligand-5 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC HDAC degraders with antitumor activity. HDAC ligand-5 can be used for the synthesis of FF2049 (HY-168863).
