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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Leuxinostat
0 ImagesCat. No.: HY-162658Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models.
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Nanatinostat TFA
0 ImagesCat. No.: HY-13432ACAS No.: 1256448-48-2Synonyms: CHR-3996 TFANanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC50s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC50 of 200 nM) and HDAC6 (IC50 of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.
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CM-414
0 ImagesCat. No.: HY-119316CAS No.: 2007971-51-7CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD).
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MC2625
0 ImagesCat. No.: HY-152225CAS No.: 1776116-75-6MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction.
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IOR-160
0 ImagesCat. No.: HY-176561CAS No.: 2421119-78-8IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research.
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HDAC6-IN-69
0 ImagesCat. No.: HY-180214HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
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NL-103
0 ImagesCat. No.: HY-12487CAS No.: 1788896-33-2
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A2AAR/HDAC-IN-1
0 ImagesCat. No.: HY-143324CAS No.: 2767560-51-8A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity.
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HDAC6-IN-62
0 ImagesCat. No.: HY-174449CAS No.: 3056725-89-1HDAC6-IN-62 (Compound 2.12) is a selective HDAC6 inhibitor, with an IC50 value of 0.25 nM. HDAC6-IN-62 can be used in the research of Charcot-Marie-Tooth disease.
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Rodin-C
0 ImagesCat. No.: HY-176868CAS No.: 2065162-16-3Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18 and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.
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HDAC1-IN-14
0 ImagesCat. No.: HY-183366HDAC1-IN-14 is an indole-based benzamide selective HDAC1 inhibitor with an IC50 of 77 nM. HDAC1-IN-14 acts as an antiproliferative agent, with GI50 values ranging from nanomolar to low micromolar levels in various cancer cells. HDAC1-IN-14 induces G0-G1 cell cycle arrest in colon cancer cells. HDAC1-IN-14 upregulates the expression of Caspase-3, Cyto-C and Bax, and downregulates the expression of AKT-1. HDAC1-IN-14 can be used in research related to leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer.
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HDAC6-IN-82
0 ImagesCat. No.: HY-183560CAS No.: 1228571-33-2HDAC6-IN-82 is a selective HDAC6 inhibitor with an IC50 of 4.9 nM against HDAC6. HDAC6-IN-82 inhibits HDAC1 (112 nM), HDAC2 (737 nM), HDAC3 (623 nM), HDAC8 (1140 nM), HDAC10 (91.4 nM) and HDAC11 (219 nM). HDAC6-IN-82 reduces cancer cell viability, induces cell cycle arrest, triggers apoptosis, and increases the acetylation levels of H3K9 and α-tubulin. HDAC6-IN-82 can be used in cancer-related research such as leukemia.
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HDAC-IN-46
0 ImagesCat. No.: HY-150597CAS No.: 2562386-85-8HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC).
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HDAC-IN-51
0 ImagesCat. No.: HY-152173CAS No.: 3026728-28-6HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer.
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HDAC6-IN-61
0 ImagesCat. No.: HY-176733HDAC6-IN-61 (Compound 4e) is a HDAC6 inhibitor (IC50: 73 nM) with selectivity over other HDAC isoforms. HDAC6-IN-61 is also a GPR40 activator. HDAC6-IN-61 increases acetylated tubulin and ERK phosphorylation levels. HDAC6-IN-61 can be used for research of neuroinflammation such as Alzheimer's disease.
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HDAC-IN-91
0 ImagesCat. No.: HY-175021HDAC-IN-91 is a multiple inhibitor of HDAC (IC50 = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (Ki = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC50 = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research.
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FF2039
0 ImagesCat. No.: HY-172159FF2039 is a pan-HDAC PROTAC degrader that binds to DCAF11, acting on HDAC6, HDAC1, HDAC2 and HDAC4. FF2039 recruits the DCAF11 E3 ligase and mediates the polyubiquitination and degradation of HDACs via the ubiquitin-proteasome system. FF2039 induces cell cycle arrest, apoptosis, cytotoxicity and antiproliferative activity in cancer cells, and reduces the clonogenic capacity of cancer cells. FF2039 is applicable to research related to multiple myeloma, triple-negative breast cancer and glioblastoma.
