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Chromatin/Epigenetic

DNA Methyltransferase

(45)

Epigenetic Reader Domain

HIF/HIF Prolyl-Hydroxylase

(82)

Histone Acetyltransferase

(51)

Histone Demethylase

(96)

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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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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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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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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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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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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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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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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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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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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R306465

T21324604769-01-9In house

R306465 (JNJ-16241199) is an orally active and selective class I histone deacetylase (HDAC 1) inhibitor with an IC50 of 3.3 nM. R306465 has a broad spectrum of antitumor activity, can induce histone 3 acetylation, and induce apoptosis, and can be used to study solid tumors and hematological malignancies.

$139

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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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Valproic Acid

T706499-66-1

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that inhibits HDAC1 activity, induces HDAC2 degradation, and is orally active. Valproic Acid can be used in epilepsy and bipolar disorder research.

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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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Tacedinaline

T1888112522-64-2

Tacedinaline (CI994) is a selective class I HDAC inhibitor with potential antineoplastic activity.

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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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SS-208

T169362245942-72-5In house

SS-208 is a selective inhibitor of HDAC6 (IC50 = 12 nM) with anti-tumor activity. SS-208 shows selectivity over other HDAC subtypes.

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KH16

T77664

KH16 is a potent HDAC inhibitor that specifically targets class I HDACs (HDAC1, HDAC2 and HDAC3) with IC50 values between 6 and 34 nM. KH16 is able to stimulate apoptosis and can inhibit gene expression patterns in a wide range of tumor cells.

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Givinostat hydrochloride

T6279L199657-29-9

Givinostat hydrochloride (ITF2357 hydrochloride) is an inhibitor of HDAC with IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat hydrochloride exhibits anti-inflammatory, anti-angiogenic, and antineoplastic activities.

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Exifone

T2008052479-85-3

Exifone (NSC-680919) is a mixed, nonessential activator of HDAC1 that is capable of binding to both free and substrate-bound enzyme, resulting in an increased relative maximal rate of HDAC1-catalyzed deacetylation.

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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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