HDAC

Histone deacetylases

HDAC

HDAC Isoform Specific Products:

HDAC Isoform Comparison

Productos relacionados con HDAC (850)
Antibodies (16)
Vía de señalización HDAC
HDAC Isoform Comparison

By Effects:	Inhibitors (742)

Cat. No.	Nombre del producto	Efecto	Pureza	Chemical Structure

HY-119017

SB-429201	Inhibitor	98.15%
SB-429201 is a potent and selective HDAC1 (IC₅₀~1.5 μM). SB-429201 displays at least a 20-fold preference for HDAC1 inhibition over HDAC3 and HDAC8.

HY-124053

BRD2492	Inhibitor	99.22%
BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC₅₀s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC₅₀s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively.

HY-143412

MIR002	Inhibitor	99.0%
MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo.

HY-172157

HDAC11-IN-2	Inhibitor	99.52%
HDAC11-IN-2 (compound B6) is a high selective Histone Deacetylase 11 (HDAC11) inhibitor. HDAC11-IN-2 inhibits HDAC11 and HDAC8 with IC₅₀s of 51.1 ×10^-3 μM and 5 μM, respectively. HDAC11-IN-2 inhibits denovolipogenesis (DNL) and promotes fatty acid oxidation, thus mitigating hepaticlipid accumulation and pathological symptoms in MASLD mice. HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172 through the inhibition of HDAC11, consequently modulating DNL and fatty acid oxidation in the liver.

HY-116818

Crebinostat	Inhibitor	98.83%
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-10224R

Panobinostat (Standard)	Inhibitor
Panobinostat (Standard) (LBH589 (Standard)) is the analytical standard of Panobinostat (HY-10224). This product is intended for research and analytical applications. Panobinostat is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.

HY-100871

WT-161	Inhibitor	98.04%
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-106409

Tefinostat	Inhibitor	99.65%
Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.

HY-10226

JNJ-16241199	Inhibitor	99.05%
JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC₅₀of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21^waf1, ^cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.

HY-RS06058

HDAC1 Human Pre-designed siRNA Set A	Inhibitor
HDAC1 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-15654S

Phenylbutyrate-d₁₁ sodium	Inhibitor	99.85%
Phenylbutyrate-d₁₁ (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.

HY-12310

RSC133	Inhibitor	98.45%
RSC133 is a dual inhibitor of DNA methyltransferase 1 and histone deacetylase 1 inhibitor. RSC133 promotes cell proliferation, up-regulates H₃K₉ histone acetylation, down-regulates p53, p21, p16/INK4A, and ablates pro-senescence phenotypes.

HY-156602

Bocodepsin	Inhibitor	98.01%
Bocodepsin (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin can be used for suppression on solid tumor and hematologic malignancies.

HY-150109A

Purinostat	Inhibitor	98.04%
Purinostat is a selective inhibitor of HDAC I/IIb with anti-leukemic activity. Purinostat mesylate (HY-150109), the mesylate salt of Purinostat, inhibits the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDAC I/IIb to inhibit several important factors for leukemic stem cell (LSC) survival, including c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Purinostat mesylate increases glutamate metabolism in LSC by increasing GLS1.

HY-108701

Nampt-IN-3	Inhibitor	98.97%
Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC₅₀s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.

HY-100384

NKL 22	Inhibitor
NKL 22 is a potent and selective inhibitor of histone deacetylases (HDAC), with IC₅₀ values of 199 and 69 nM for HDAC1 and HDAC3, respectively. NKL 22 can reverse abnormal expression of HD‑related genes and restore the levels of key genes including Ppp1r1b in Huntington's disease transgenic mice. NKL 22 can be used for the researches of Huntington's disease and cancer.

HY-109109

Alteminostat	Inhibitor	98.66%
Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research.

HY-19747

HPOB	Inhibitor	99.54%
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-114483

AES-135	Inhibitor	98.68%
AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC₅₀s ranging from 190-1100 nM.

HY-160092A

Martinostat hydrochloride	Inhibitor	99.01%
Martinostat hydrochloride is a HDAC inhibitor and can be labeled with radionuclides for quantitative imaging of HDACs in vivo in the central nervous system and major peripheral organs.

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:

Productos relacionados con HDAC (850)

Antibodies (16)

Vía de señalización HDAC

HDAC Isoform Comparison

Productos relacionados con HDAC (850):