2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Epigenetics
  4. HDAC

HDAC

Histone deacetylases

HDAC

Related Products

PDF 2.58 MB

HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on ahistone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily.

HDAC Isoform Specific Products:

HDAC Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-176207
    HDAC degrader-1
    		Degrader
    HDAC6 degrader-6 (compound 10c) is a ByeTAC protein degrader targeting HDAC6, with IC50 values of 0.034 μM, 0.166 μM, 0.703 μM, and 0.293 μM for HDAC6, HDAC1, HDAC2, and HDAC3, respectively. HDAC6 degrader-6 induces cell apoptosis and can be used for the study of multiple myeloma(Blue: USP14 ligand HY-159808; Pink: HDAC ligand HY-176209; Black: linker HY-W016871)
    HDAC degrader-1
  • HY-RS06089
    Hdac9 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Hdac9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Hdac9 Mouse Pre-designed siRNA Set A
  • HY-178485
    SJY26
    		Inhibitor
    SJY26 is a PI3K/HDAC dual-target inhibitor with IC50s of 0.59 nM (PI3Kα and PI3Kδ), 2.02 nM (PI3Kγ), 12.69 nM (PI3Kβ) and 114 nM (HDAC1). SJY26 exhibits potent broad-spectrum anti-proliferative activity, and is particularly sensitive to Jurkat and PC9R cells. SJY26 inhibited the migration of PC9R cells, arrested the cell cycle and induced cell apoptosis. SJY26 reduces AKT phosphorylation, and decreases histone H3 deacetylation (Ac-H3). SJY26 can be used for the studies of non-small cell lung cancer and leukemia.
    SJY26
  • HY-149371
    HDAC6-IN-16
    		Inhibitor
    HDAC6-IN-16 (compound 5c) is a histone deacetylase 6 (HDAC6) inhibitor, based on Quinazolin-4(3H)-One. HDAC6-IN-16 exhibits anticancer effect, inhibits colony-forming. And HDAC6-IN-16 arrests cell cycle at G2 phase and induces apoptosis.
    HDAC6-IN-16
  • HY-176866
    Rodin-A
    		Inhibitor
    Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.
    Rodin-A
  • HY-151443
    HDAC-IN-47
    		Inhibitor
    HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.
    HDAC-IN-47
  • HY-178351
    HDAC6-IN-67
    		Inhibitor
    HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.
    HDAC6-IN-67
  • HY-162060
    YPX-C-05
    		Inhibitor
    YPX-C-05 is a hydroxamic acid-based HDAC inhibitor. YPX-C-05 exerts significant vasodilatory effects. YPX-C-05 exhibits inhibitory effects on HDACs and increases histone H4 acetylation in endothelial cells. YPX-C-05 can be used for hypertension research.
    YPX-C-05
  • HY-149718
    Antitumor agent-123
    		Inhibitor
    Antitumor agent-123 (Copmound 4d) effectively inhibits multiple kinase targets with anti-cancer effects, including JAK2, JAK3, HDAC1 and HDAC6, with IC50 values of 34.6 and 2.6 μM for JAK2 and JAK3, respectively. Antitumor agent-123 exhibits moderate activity in solid tumor models.
    Antitumor agent-123
  • HY-142965
    HDAC-IN-28
    HDAC-IN-28, a novel HDAC inhibitor, shows potent activities against tumor growth and metastasis
    HDAC-IN-28
  • HY-N0931R
    Santacruzamate A (Standard)
    		Inhibitor
    Santacruzamate A (Standard) is the analytical standard of Santacruzamate A. This product is intended for research and analytical applications. Santacruzamate A (CAY-10683, STA) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM. STA also exerts neuroprotective property against amyloid-β protein fragment 25–35. STA can be used for cancer and neurological disease research[1][2].
    Santacruzamate A (Standard)
  • HY-172878
    HDAC/PSMD14-IN-1
    		Inhibitor
    HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research.
    HDAC/PSMD14-IN-1
  • HY-W700378
    Valproic acid β-D-glucuronide-d6
    Valproic acid β-D-glucuronide-d6-1 is the deuterium labeled Valproic acid β-D-glucuronide (HY-W400496). Valproic acid β-D-glucuronide is the major urinary metabolite of Valproic acid (HY-10585).
    Valproic acid β-D-glucuronide-d<sub>6</sub>
  • HY-172193
    UBD1031
    		Antagonist
    UBD1031 (SGC-UBD1031) is a potent USP16-UBD and HDAC6-UBD antagonist, with Kd values of 48 and 16 nM, respectively. UBD1031 inhibits the interaction between USP16 and ISG15 with an EC50 of 1.7 nM. UBD1031 can be used a chemical probe for USP16 UBD.
    UBD1031
  • HY-P2698
    1-Alaninechlamydocin
    		Inhibitor
    1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
    1-Alaninechlamydocin
  • HY-162955
    LSD1/HDAC-IN-1
    		Inhibitor
    LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC50s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research.
    LSD1/HDAC-IN-1
  • HY-142690
    HDAC-IN-27
    		Inhibitor
    HDAC-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).
    HDAC-IN-27
  • HY-RS06071
    Hdac3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Hdac3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Hdac3 Mouse Pre-designed siRNA Set A
  • HY-162378
    LT-630
    		Inhibitor
    LT-630 is a HDAC6 inhibitor. LT-630 ameliorates liver injury by reducing oxidative damage.
    LT-630
  • HY-172781
    HDAC6-IN-55
    		Inhibitor
    HDAC6-IN-55 (Compound 15B) is a potent HDAC6 inhibitor and an effective anti-inflammatory agent. HDAC6-IN-55 alleviates atopic dermatitis through anti-inflammatory effects facilitated via TLR4/MAPK, STAT3 and NF-κB pathways. HDAC6-IN-55 alleviates symptoms such as skin edema, dryness, crusting, and peeling in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis mice.
    HDAC6-IN-55
Cat. No. Product Name / Synonyms Application Reactivity
All Rights Reserved.
Download HDAC Signaling Pathway Map.

TCR, GPCR and HDAC II interaction: Diverse agonists act through G-protein-coupled receptors (GPCRs) to activate the PKC-PKD axis, CaMK, Rho, or MHC binding to antigens stimulates TCR to activate PKD, leading to phosphorylation of class II HDACs. Phospho-HDACs dissociate from MEF2, bind 14-3-3, and are exported to the cytoplasm through a CRM1-dependent mechanism. CRM1 is inhibited by leptomycin B (LMB). Release of MEF2 from class II HDACs allows p300 to dock on MEF2 and stimulate gene expression. Dephosphorylation of class II HDACs in the cytoplasm enables reentry into the nucleus[1].

 

TLR: TLR signaling is initiated by ligand binding to receptors. The recruitment of TLR domain-containing adaptor protein MyD88 is repressed by HDAC6, whereas NF-κB and MTA-1 can be negatively regulated by HDAC1/2/3 and HDAC2, respectively. Acetylation by HATs enhance MKP-1 which inhibits p38-mediated inflammatory responses, while HDAC1/2/3 inhibits MKP-1 activity. HDAC1 and HDAC8 repress, whereas HDAC6 promotes, IRF function in response to viral challenge. HDAC11 inhibits IL-10 expression and HDAC1 and HDAC2 represses IFNγ-dependent activation of the CIITA transcription factor, thus affecting antigen presentation[2][3].

 

IRNAR: IFN-α/β induce activation of the type I IFN receptor and then bring the receptor-associated JAKs into proximity. JAK adds phosphates to the receptor. STATs bind to the phosphates and then phosphorylated by JAKs to form a dimer, leading to nuclear translocation and gene expression. HDACs positively regulate STATs and PZLF to promote antiviral responses and IFN-induced gene expression[2][3].

 

Cell cycle: In G1 phase, HDAC, Retinoblastoma protein (RB), E2F and polypeptide (DP) form a repressor complex. HDAC acts on surrounding chromatin, causing it to adopt a closed chromatin conformation, and transcription is repressed. Prior to the G1-S transition, phosphorylation of RB by CDKs dissociates the repressor complex. Transcription factors (TFs) gain access to their binding sites and, together with the now unmasked E2F activation domain. E2F is then free to activate transcription by contacting basal factors or by contacting histone acetyltransferases, such as CBP, that can alter chromatin structure[4].

 

The function of non-histone proteins is also regulated by HATs/HDACs. p53: HDAC1 impairs the function of p53. p53 is acetylated under conditions of stress or HDAC inhibition by its cofactor CREB binding protein (CBP) and the transcription of genes involved in differentiation is activated. HSP90: HSP90 is a chaperone that complexes with other chaperones, such as p23, to maintain correct conformational folding of its client proteins. HDAC6 deacetylates HSP90. Inhibition of HDAC6 would result in hyperacetylated HSP90, which would be unable to interact with its co-chaperones and properly lead to misfolded client proteins being targeted for degradation via the ubiquitin-proteasome system[5][6].
 

Reference:

[1]. Vega RB, et al. Protein kinases C and D mediate agonist-dependent cardiac hypertrophy through nuclear export of histone deacetylase 5.Mol Cell Biol. 2004 Oct;24(19):8374-85.
[2]. Shakespear MR, et al. Histone deacetylases as regulators of inflammation and immunity. Trends Immunol. 2011 Jul;32(7):335-43.
[3]. Suliman BA, et al. HDACi: molecular mechanisms and therapeutic implications in the innate immune system.Immunol Cell Biol. 2012 Jan;90(1):23-32. 
[4]. Brehm A, et al. Retinoblastoma protein meets chromatin.Trends Biochem Sci. 1999 Apr;24(4):142-5.
[5]. Butler R, et al. Histone deacetylase inhibitors as therapeutics for polyglutamine disorders.Nat Rev Neurosci. 2006 Oct;7(10):784-96
[6]. Minucci S, et al. Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer.Nat Rev Cancer. 2006 Jan;6(1):38-51.

HDAC Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.