HDAC

Histone deacetylases

HDAC

HDAC Isoform Specific Products:

HDAC Isoform Comparison

HDAC Related Products (851)
Antibodies (16)
HDAC Signaling Pathway
HDAC Isoform Comparison

By Effects:	Inhibitors (740)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-146153

HDAC-IN-40	Inhibitor	98.71%
HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with K_i values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects.

HY-152174

HDAC-IN-52	Inhibitor	99.46%
HDAC-IN-52 is a pyridine-containing HDAC inhibitor, with IC₅₀s of 0.189, 0.227, 0.440 and 0.446 μM for HDAC1, HDAC2, HDAC3, and HDAC10, respectively. HDAC-IN-52 can be used for the research of cancer.

HY-149819

CDK/HDAC-IN-3	Inhibitor	99.60%
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .

HY-145259

HDAC6-IN-3	Inhibitor	98.0%
HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC₅₀s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC₅₀=0.79 μM) and LSD1 inhibitor. HDAC6-IN-3 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-156273

HDAC/JAK/BRD4-IN-1	Inhibitor
HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo.

HY-159109

HDAC6-IN-46	Inhibitor	98.51%
HDAC6-IN-46 (compound 12) is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ value of 6.2 nM. HDAC6-IN-46 can be used in Alzheimer's disease research.

HY-124782

HDAC8-IN-8	Inhibitor	99.01%
HDAC8-IN-8 (15a) is an HDAC8 inhibitor, with IC₅₀ values of 23.9 μM and 268.2 μM for hHDAC8 and smHDAC8 respectively. And for hHDAC1 and hHDAC6, the IC₅₀ values are 12.1 μM and 2.9 μM respectively. HDAC8-IN-8 can be used in schistosomiasis-related research.

HY-W009732R

Sinapinic acid (Standard)	Inhibitor
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells. Sinapinic acid shows antioxidant and antidiabetic activities. Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats.

HY-RS06060

Hdac1 Rat Pre-designed siRNA Set A	Inhibitor
Hdac1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hdac1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-10585AR

Valproic acid sodium (Standard)	Inhibitor
Valproic acid (sodium) (Standard) is the analytical standard of Valproic acid (sodium). This product is intended for research and analytical applications. Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC₅₀ in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC₅₀, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

HY-139650

HDAC1/2-IN-3	Inhibitor	98.05%
HDAC1/2-IN-3 is a HDAC1 and HDAC2 inhibitor with IC₅₀ values 0-5 and 5-10 nM, respectively.

HY-16138

Ivaltinostat	Inhibitor	99.70%
Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects.

HY-10585AS1

Valproic acid-d₁₄ sodium	Inhibitor
Valproic acid-d₁₄ (sodium) is deuterium labeled Valproic acid (sodium). Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium salt activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

HY-138831

AES-350	Inhibitor	99.30%
AES-350 is a potent and orally active HDAC6 inhibitor with an IC₅₀ and a K_i of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC₅₀ values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

HY-145613

5-Phenylpentan-2-one	Inhibitor	99.81%
5-Phenylpentan-2-one is a potent histone deacetylases (HDACs) inhibitor. 5-Phenylpentan-2-one can be used for urea cycle disorder research.

HY-115412

Vorinostat-d5	Inhibitor	99.0%
Vorinostat-d5 (SAHA-d5) is the deuterium labeled Vorinostat. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC7 (Class II) and HDAC11 (Class IV), with ID₅₀ values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.

HY-W014004

m-Carboxycinnamic acid bishydroxamide	Inhibitor	98.0%
m-Carboxycinnamic acid bishydroxamide (CBHA) is a histone deacetylase inhibitor. m-Carboxycinnamic acid bishydroxamide modulates histone acetylation sites, alters DNA methylation and epigenetic status, increases global histone acetylation, alleviates transcription repression, and facilitates chromatin remodelling. m-Carboxycinnamic acid bishydroxamide can be used for the research of cloned embryo development and epigenetic regulation.

HY-117374

HDAC3-IN-1	Inhibitor	99.28%
HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC₅₀ of 5.96 nM.

HY-13506G

M344 (GMP)	Inhibitor
M344 (GMP) (D 237) (GMP) is the GMP level of M344 (HY-13506). GMP level of small molecules can be used as auxiliary reagents in cell therapy. M344 is a kind of histone acetylation enzyme inhibitor.

HY-149631

HFY-4A	Inhibitor	99.34%
HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models.

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.

Name
Email *

	Sorry, but the email address you supplied was invalid.

HDAC

HDAC

HDAC Isoform Specific Products:

HDAC Isoform Specific Products:

HDAC Related Products (851)

Antibodies (16)

HDAC Signaling Pathway

HDAC Isoform Comparison

HDAC Related Products (851):