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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.

  • Tasquinimod
    T6695254964-60-8
    Tasquinimod (ABR-215050) is a quinoline-3-carboxamide linomide analog with antiangiogenic and potential antineoplastic activities. Tasquinimod has been shown to decrease blood vessel density but the exact mechanism of action is not known. This agent has also been shown to augment the antineoplastic effects of docetaxel and androgen ablation in a murine model of prostate cancer involving human prostate cancer xenografts.
    • $45
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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.
    • $86
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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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  • 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.
    • $98
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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.
    • $30
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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.
    • $48
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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.
    • $58
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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.
    • $30
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  • Sodium 4-phenylbutyrate
    T15351716-12-7
    Sodium 4-phenylbutyrate (TriButyrate), a transcriptional regulator, reversibly inhibits class I and II histone deacetylases (HDACs )resulting in a global increase in gene expression, decreased cellular proliferation, increased cell differentiation, and the induction of apoptosis in susceptible tumor cell populations.
    • $38
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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.
    • $32
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  • Fimepinostat
    T20781339928-25-4
    Fimepinostat (CUDC 907) is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan-histone deacetylase (HDAC) enzymes, with potential antineoplastic activity. Upon oral administration, CUDC-907 inhibits the activity of both PI3K class I isoforms and HDAC, thereby preventing the activation of the PI3K-AKT-mTOR signal transduction pathway that is often overactivated in many cancer cell types.
    • $39
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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.
    • $40
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  • Raddeanin A
    T387889412-79-3
    Raddeanin A (NSC-382873) has moderate inhibitory activity against histone deacetylases (HDACs). Raddeanin A has high antiangiogenic potency, antitumor activity.
    • $40
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  • TMP195
    T39831314891-22-9
    TMP195 (TFMO 2) is a selective class IIa histone deacetylase (HDAC) inhibitor.
    • $67
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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.
    • $67
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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.
    • $44
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  • Givinostat hydrochloride monohydrate
    T6279732302-99-7
    Givinostat hydrochloride monohydrate (ITF2357) is an HDAC inhibitor.
    • $31
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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.
    • $50
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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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  • ACY-738
    T35091375465-91-0
    ACY-738 demonstrates inhibitory activity against recombinant HDAC6 (IC50: 1.7 nM), with respective average selectivity over class I HDACs being 100-fold.
    • $41
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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.
    • $31
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  • Corin
    T108641808113-09-8In house
    Corin is an irreversible inhibitor of HDAC1(IC50 = 147 nM) and LSD1(Ki = 110 nM).
    • $179
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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.
    • $50
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  • Parthenolide
    T214020554-84-1
    Parthenolide ((-)-Parthenolide) is a natural sesquiterpene lactone that is an NF-κB inhibitor and also specifically inhibits HDAC1 protein, but is inactive against other class I II HDACs. Parthenolide has anti-inflammatory, anti-tumor, and anti-viral activities.
    • $50
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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.
    • $50
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  • Dacinostat
    T2454404951-53-7
    LAQ824 (Dacinostat (NVP-LAQ824)) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.
    • $45
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  • CAY10603
    T19831045792-66-2
    CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor.
    • $57
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  • Tacedinaline
    T1888112522-64-2
    Tacedinaline (CI994) is a selective class I HDAC inhibitor with potential antineoplastic activity.
    • $43
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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.
    • $54
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  • Tubacin
    T6327537049-40-4
    Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.
    • $77
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  • Tubastatin A
    T19661252003-15-8
    Tubastatin A (Tubastatin A BASE) is an effective and specific HDAC6 inhibitor (IC50: 15 nM, in a cell-free assay). Its selectivity is 1000-fold against all the other isozymes except HDAC8.
    • $41
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  • Nexturastat A
    T18191403783-31-2
    Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is >190-fold than other HDACs.
    • $63
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  • TMP269
    T18571314890-29-3
    TMP269 is an effective, specific class IIa HDAC inhibitor for HDAC4 (IC50: 157 nM), HDAC5 (IC50: 97 nM), HDAC7 (IC50: 43 nM), and HDAC9 (IC50: 23 nM), respectively.
    • $66
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  • HDAC6 degrader 9c
    T697532235382-05-3In house
    HDAC6 degrader 9c is a small molecule histone deacetylase 6 (HDAC6) degrader that can be used to study cancer or other diseases.
    • $195
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  • Mocetinostat
    T2512726169-73-9
    Mocetinostat (MG0103) is an orally available HDAC inhibitor with most potency for HDAC1 (IC50: 0.15 μM), 2- to 10- fold selectivity against HDAC2 3 11.
    • $36
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  • PCI-34051
    T6325950762-95-5
    PCI-34051 is an effective and selective HDAC8 inhibitor (IC50: 10 nM).
    • $55
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  • CRA-026440 hydrochloride
    T10883L847459-98-7In house
    CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor. CRA-026440 hydrochloride exhibits Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM, respectively. CRA-026440 hydrochloride exhibits antitumor and antiangiogenic activities.
    • $117
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  • MC2590
    T735152284460-01-9In house
    MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.
    • $518
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  • 4-Phenylbutyric acid
    T58861821-12-1
    4-Phenylbutyric acid (Benzenebutyric acid) is a histone deacetylase (HDAC) inhibitor and an endoplasmic reticulum stress (ERS) inhibitor. 4-Phenylbutyric acid can be used to treat urea cycle disorders.
    • $41
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  • Pracinostat
    T1890929016-96-6
    Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.
    • $43
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  • WT-161
    T73851206731-57-8
    WT161 is a potent and selective inhibitor of HDAC6 (IC50:0.40 nM).
    • $36
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  • Citarinostat
    T36611316215-12-9
    ACY-241, also known as Citarinostat (ACY241), is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.
    • $44
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  • MPT0G211
    T606162151853-97-1In house
    MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.
    • $98
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  • Domatinostat
    T6362910462-43-0
    Domatinostat (4SC202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
    • $35
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  • Valproic acid sodium salt
    T16021069-66-5
    Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.
    • $42
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  • FT895
    T113292225728-57-2
    FT895 is a selective and potent HDAC11 inhibitor with antifungal and antitumor activity, inhibiting HDAC11 expression and limiting EV71 replication in vitro (in vitro).
    • $766
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  • Tefinostat
    T17028914382-60-8
    Tefinostat (CHR-2845) is a potent monocyte macrophage-targeted histone deacetylase (HDAC) inhibitor that is cleaved to the active acid CHR-2847 by intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat exhibits antitumor activity and can be used in the study of leukemia and advanced hematologic malignancies.
    • $97
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  • SantacruzaMate A
    T22661477949-42-0
    SantacruzaMate A (CAY-10683) is a potent and selective HDAC inhibitor.
    • $30
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  • HDAC-IN-7
    T2025743420-02-2
    HDAC-IN-7 (HBI-8000) (Chidamide impurity) is an impurity of Chidamide, a potent and orally bioavailable inhibitor of HDAC enzymes class I (HDAC1 2 3) and class IIb [HDAC10].
    • $56
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  • Tubastatin A Hydrochloride
    T61611310693-92-5
    Tubastatin A Hydrochloride (TSA HCl) is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).
    • $45
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