HDAC

Histone deacetylases

HDAC

HDAC Isoform Specific Products:

HDAC Isoform Comparison

HDAC Related Products (556)
Antibodies (16)
HDAC Signaling Pathway
HDAC Isoform Comparison

By Effects:	Inhibitors (501) Degraders (10) Antagonists (2) Activators (7) Modulators (2)

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-19328

ACY-775	Inhibitor	99.69%
ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC₅₀ of 7.5 nM. ACY775 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).

HY-123295

HDAC3-IN-T247	Inhibitor	98.94%
HDAC3-IN-T247 is a potent and selective HDAC3 (histone deacetylase 3) inhibitor, with an IC₅₀ of 0.24 µM. HDAC3-IN-T247 induces a selective increase of NF-κB acetylation in HCT116 cells. HDAC3-IN-T247 shows anticancer and antiviral activity. HDAC3-IN-T247 inhibits growth of cancer cells, and activates HIV gene expression in latent HIV-infected cells.

HY-126147

J22352	Inhibitor	99.04%
J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC₅₀ value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.

HY-19350

BML-210	Inhibitor	98.06%
BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC₅₀ of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice.

HY-100871

WT-161	Inhibitor	98.36%
WT-161 is a potent and selective HDAC6 inhibitor with an IC₅₀ of 0.40 nM. WT-161 also inhibits metallo-β-lactamase domain-containing protein?2 (MBLAC2).

HY-145816A

JPS016 TFA		98.70%
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells.

HY-144779

HDAC10-IN-1	Inhibitor	99.11%
HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC₅₀ of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells.

HY-N7676

Marein	Inhibitor	99.71%
Marein has the neuroprotective effect due to a reduction of damage to mitochondria function and activation of the AMPK signal pathway. Marein improves insulin resistance induced by high glucose in HepG2 cells through CaMKK/AMPK/GLUT1 to promote glucose uptake, through IRS/Akt/GSK-3β to increase glycogen synthesis, and through Akt/FoxO1 to decrease gluconeogenesis. Marein is a HDAC inhibitor with an IC₅₀ of 100 μM. Marein has beneficial antioxidative, antihypertensive, antihyperlipidemic and antidiabetic effects.

HY-101780

Tinostamustine	Inhibitor	99.42%
Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 6 nM, 9 nM, 9 nM and 25 nM, respectively.

HY-126052

Gnetol	Inhibitor	99.86%
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC₅₀ of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC₅₀ of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.

HY-18712

BG45	Inhibitor	99.96%
BG45 is a potent HDAC3 inhibitor with IC₅₀ values of 0.289, 2, 2.2 and ﹥20 μM for HDAC3, HDAC1, HDAC2 and HDAC6, respectively. BG45 selectively targets multiple myeloma (MM) cells and induces caspase-dependent apoptosis.

HY-19348

Pimelic Diphenylamide 106	Inhibitor	98.54%
Pimelic Diphenylamide 106 (TC-H 106) is a slow, tight binding class I HDAC inhibitor (inhibits HDAC1, 2, and 3 with IC₅₀ values of 150 nM, 760 nM, and 370 nM, respectively), with no activity against class II HDACs. Pimelic Diphenylamide 106 modulates dopamine concentration and protects dopamine cells by inducing VMAT2 expression. Pimelic Diphenylamide 106 can be used in the study of neuropsychiatric diseases such as attention deficit hyperactivity disorder (ADHD).

HY-102033

Oxamflatin	Inhibitor	98.13%
Oxamflatin (Metacept-3) is a potent HDAC inhibitor with an IC₅₀ of 15.7 nM. Oxamflatin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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-100365

Remetinostat	Inhibitor	≥98.0%
Remetinostat (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.

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-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-100585

Splitomicin	Inhibitor	98.42%
Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD⁺-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC₅₀ of 60 μM.

HY-114414

HDACs/mTOR Inhibitor 1	Inhibitor	99.01%
HDACs/mTOR Inhibitor 1 is a dual HDAC.html" class="link-product" target="_blank">HDACs and mTOR.html" class="link-product" target="_blank">mTOR inhibitor, with IC₅₀s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies.

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 (556)

Antibodies (16)

HDAC Signaling Pathway

HDAC Isoform Comparison

HDAC Related Products (556):