HDAC

Histone deacetylases

HDAC

HDAC Isoform Specific Products:

HDAC Isoform Comparison

HDAC Related Products (726)
Antibodies (16)
HDAC Signaling Pathway
HDAC Isoform Comparison

By Effects:	Controls (3) Ligands (3) Inhibitors (643) Substrate (1) Degraders (24) Antagonists (3) Activators (9) Modulators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-14718A

Resminostat hydrochloride	Inhibitor	99.68%
Resminostat hydrochloride is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC₅₀ values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC₅₀ of 877 nM.

HY-N6017

Bakkenolide A	Inhibitor	99.99%
Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.

HY-164050

HDAC2-IN-2	Inhibitor	99.74%
HDAC2-IN-2 (compound 124) is an inhibitor of HDAC2 with Kd value of 0.1-1 μM.

HY-164233

YX968	Inhibitor	98.06%
YX968 is a potent and selective HDAC3/8 PROTAC dual degrader with DC₅₀ values of 1.7 and 6.8 nM. YX968 exhibits antitumor activity by promoting apoptosis.(Pink: Target protein ligand (HY-168287); Black: linker (HY-W007700); Blue: E3 ligase ligand (HY-112078))

HY-B0809R

Theophylline (Standard)	Activator
Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.

HY-10585R

Valproic acid (Standard)	Inhibitor
Valproic acid (Dipropylacetic Acid) (Standard) is an analytical standard for valproic acid. This product is intended for research and analytical applications. Valproic acid is an orally active HDAC inhibitor (IC₅₀=0.5-2 mM), inhibits the activity of HDAC1 (IC₅₀=400 μM), and induces the degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits the proliferation of small cell lung cancer (SCLC) cells. Valproic acid is used in the study of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and migraine.

HY-132242

DL-Sulforaphane N-acetyl-L-cysteine	Inhibitor	99.90%
DL-Sulforaphane N-acetyl-L-cysteine (SFN-NAC) is an orally active HDAC inhibitor and metabolite of sulforaphane (HY-13755) with longer half-life and better blood-brain barrier permeability. DL-Sulforaphane N-acetyl-L-cysteine activates autophagy-mediated downregulation of α-tubulin expression through the ERK pathway and can be used in cancer research.

HY-118052

BPKDi		99.60%
BPKDi is an inhibitor of PKD. BPKDi inhibits three members of the PKD family, PKD1, PKD2, and PKD3, with IC₅₀ values of 1 nM, 9 nM, and 1 nM, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes and concomitantly suppresses hypertrophy of these cells.

HY-164099

LSD1/HDAC6-IN-2	Inhibitor	99.66%
LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC₅₀ values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma.

HY-W009776

Suberoyl bis-hydroxamic acid	Inhibitor	98.0%
Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID₅₀ values of 0.25 μM and 0.30 μM, respectively.Suberoyl bis-hydroxamic acid renders MM cells susceptible to apoptosis and facilitates the mitochondrial apoptotic pathways.Suberoyl bis-hydroxamic acid can be used for the study of medullary thyroid carcinoma (MTC).

HY-116818

Crebinostat	Inhibitor	99.79%
Crebinostat is a potent histone deacetylase (HDAC) inhibitor with IC₅₀ values of 0.7 nM, 1.0 nM, 2.0 nM and 9.3 nM for HDAC1, HDAC2, HDAC3 and HDAC6, respectively. Crebinostat potently induces acetylation of both histone H3 and histone H4 as well as enhances the expression of the cAMP response element-binding protein (CREB) target gene Egr1. Crebinostat increases the density of synapsin-1 punctae along dendrites in cultured neurons. Crebinostat can modulate chromatin-mediated neuroplasticity and exhibits enhanced memory in mice.

HY-14842A

Givinostat hydrochloride	Inhibitor	98.06%
Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC₅₀ of 198 and 157 nM for HDAC1 and HDAC3, respectively.

HY-14718

Resminostat	Inhibitor	99.84%
Resminostat (RAS2410; 4SC-201) is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC₅₀ values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC₅₀ of 877 nM.

HY-19772

GSK3117391	Inhibitor	99.40%
GSK3117391 (ESM-HDAC391) is a histone deacetylase (HDAC) inhibitor, extracted from patent WO/2008040934 A1.

HY-19747

HPOB	Inhibitor	99.80%
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC₅₀ of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.

HY-169259

HDAC9-IN-1	Inhibitor
HDAC9-IN-1 (Compound 7g) is a potent HDAC9 inhibitor, with an IC₅₀ of 40 nM. HDAC9-IN-1 significantly inhibits several human cancer cells, induces apoptosis, modulates caspase-related proteins as well as p38, and causes DNA damage.

HY-149285

NT160	Inhibitor	99.58%
NT160 is a highly potent class-IIa HDAC inhibitor with an IC₅₀ value of 0.046 μM. NT160 can be used for the research of central nervous system diseases.

HY-171139

PROTAC HDAC6 degrader 2	Inhibitor	99.80%
PROTAC HDAC6 degrader 2 (Compound 1) is a HDAC6 PROTAC degrader, with IC₅₀ of 0.643 μM. PROTAC HDAC6 degrader 2 promotes ubiquitination and degradation of HDAC6. PROTAC HDAC6 degrader 2 can be used for the research of haematological and solid cancers (Pink: HDAC6 ligand (HY-171141); Blue: E3 ligase CRBN ligand (HY-10984)).

HY-145815A

JPS014 TFA	Degrader	98.40%
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.

HY-117709

BRD6688	Inhibitor	98.90%
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model.

TCR CD3 GPCR Adrenergic Agonists, Endothelin, Angiotensin, 5-HT, and Others PKC PKD Rho PLCβ CaMK 14-3-3 14-3-3 HDACII LMB CRM1 HDACII HDACII 14-3-3 HDACII MEF2 p300 Cytokines
Cytokine receptors
Adhesion molecules
(e.e., LFA1) HSP90 p23 HDAC6 HDACi p23 HSP90
HDAC6 Proteasome HDAC1 p53 HDAC1 p53 HATs HDAC Antigen presentation:
Co-stimulatory molecules
(e.g., CD40, CD86)
MHCII expression Anti-viral response: IFN-stimulated
genes (e.g., Rsad2, Ifit2, ISG54) Cyclin E/A, TLR TRIF TRAM HDAC6 MyD88 Mal HDAC
1/2/3 NF-κB HDAC2 HDAC6 MTA-1 HDAC
1/2/3 HATs MKP-1 p38 HDAC
1/8 IRF AP-1 HDAC11 IL-10 HATs HDAC CBP p53 HAT
activity CBP p53 CBP p53 IFNGR IFNγ HDAC
1/2 CIITA IFNα/β IFNAR HDAC1 JAK STAT PLZF HDAC
1/2/3 HATs HDAC HDAC BAX HATs BAX Apoptosis E2F p53 p21 CDK Cyclin HDAC RB HDAC RB E2F DP TF E2F DP TK, DHFR, ... Inflammatory mediators:
Cytokines
(e.g., IL-6, TNFα, Ifnβ) Chemokines (e.g., CXCL10, Ccl2/7)
Other mediators
(e.g., MMP9, Edn-1)

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.

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HDAC

HDAC

HDAC Isoform Specific Products:

HDAC Isoform Specific Products:

HDAC Related Products (726)

Antibodies (16)

HDAC Signaling Pathway

HDAC Isoform Comparison

HDAC Related Products (726):