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Chromatin/Epigenetic

DNA Methyltransferase

(78)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(204)

Histone Acetyltransferase

(120)

Histone Demethylase

(188)

Histone Methyltransferase

Methionine Adenosyltransferase (MAT)

DNA Damage/DNA Repair

DNA Alkylator/Crosslinker

Nucleoside Antimetabolite/Analog

HDAC

Histone deacetylases (HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on a histone, 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.

Filter HomeSignaling PathwaysDNA Damage/DNA Repair-Chromatin/EpigeneticHDAC

MPI_5a

T161291259296-46-2

MPI_5a is an effective and selective inhibitor of HDAC6 (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms and it also inhibits acyl-tubulin accumulation in cells (IC50: 210 nM).

$278

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Trichostatin A

T627058880-19-6

Trichostatin A (TSA), a natural derivative of diene isohydroxamic acids, is a specific and reversible histone deacetylase inhibitor (IC50=1.8 nM) that induces hyperacetylation of core histones to regulate chromatin structure.

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Romidepsin

T6006128517-07-7

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1/2/4/6 (IC50=36/47/510/1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

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BRD3067

T305781883657-02-0In house

BRD3067 serves as a negative control for Tubacin A (AGCR-13900, TubA, AG-CR13900). BRD3067 is a derivative of Tubacin and functions as a selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 15 nM in cell-free assays. BRD3067 has demonstrated potential anticancer and anti-inflammatory activities, making it a valuable tool for studying HDAC6 inhibition.

$293

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Tasquinimod

T6695254964-60-8

Tasquinimod (ABR-215050) is an oral antiangiogenic agent with potential antitumor activity. It is also an S100A9 inhibitor and binds to the HDAC4Zn2+ binding structural domain with Kd values between 10 and 30 nM.

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BRD-6929

T10603849234-64-6

BRD-6929 is a selective, brain-penetrant HDAC1 and HDAC2 inhibitor (IC50: 1 and 8 nM). BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 (Kis: 0.2 and 1.5 nM) [2]. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV

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Tucidinostat

T44811616493-44-7

Tucidinostat (Chidamide) is an effective and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8/11 (IC50: 733/432 nM), and shows no effect on HDAC4/5/6/7/9.

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Sulforaphane

TQ02074478-93-7

Sulforaphane is a natural isothiocyanate that activates Nrf2 and inhibits AMPK-dependent signaling. Sulforaphane has antitumor and anti-inflammatory activities by increasing the transcription of tumor suppressor proteins and inhibiting histone deacetylase activity.

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RGFP966

T17621357389-11-7

RGFP966 is an HDAC3 inhibitor (IC50: 0.08 μM) and does not affect other HDACs at concentrations up to 15 µM.

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SW-100

T169622126744-35-0

SW-100 is a selective histone deacetylase 6 inhibitor (IC50: 2.3 nM). It also shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays an obviously improved ability to cross the blood-brain-barrier.

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Quisinostat

T6055875320-29-9

Quisinostat (JNJ-26481585) (JNJ-26481585) is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7.

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Belinostat

T8517866323-14-0

Belinostat (PXD101) is an inhibitor of hydroxamic acid-type histone deacetylase (HDAC, IC50 of 27 nM in HeLa cell extracts),and with antineoplastic activity.

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Entinostat

T6233209783-80-2

Entinostat (MS-275) is an HDAC class I selective inhibitor of HDAC1, HDAC2 and HDAC3 (IC50=243/453/248 nM) with oral activity. Entinostat has antitumor activity.

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Curcumin

T1516458-37-7

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

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Raddeanin A

T387889412-79-3

Raddeanin A is a natural triterpenoid saponin from Cyperus japonicus that inhibits histone deacetylase and is also a potent immunogenic cell death inducer with strong anti-angiogenic and anti-tumor activities.

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ACY-1083

T102441708113-43-2In house

ACY-1083 is a selective, brain-penetrating HDAC6 inhibitor (IC50: 3 nM) that effectively reverses chemotherapy-induced peripheral neuropathy.

$155

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Valproic Acid

T706499-66-1

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

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Sodium butanoate

T1393156-54-7

Sodium butanoate (Sodium Butyrate) is the sodium salt of butyrate with potential antineoplastic activity. Butyrate, a short chain fatty acid, competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).

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Panobinostat

T2383404950-80-7

Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.

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Vorinostat

T1583149647-78-9

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

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ST7612AA1

T706921428535-92-5In house

ST7612AA1 is a novel potent and oral HDCA inhibitor that acts as an HIV-1 latency reactivator. ST7612AA1 showed significant antitumor activity at low concentrations in vitro and in vivo. ST7612AA1 has potential anticancer activity and can be used to study malaria.

$195

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CM-675

T108411872466-47-1In house

CM-675 is a dual inhibitor of phosphodiesterase 5 (PDE5) and class I histone deacetylases (IC50s: 114 nM and 673 nM for PDE5 and HDAC1) with the potential to treat Alzheimer's disease.

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