HDAC

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1047 Vorinostat (SAHA, MK0683) <1 mg/mL 52 mg/mL 3 mg/mL
S1053 Entinostat (MS-275) <1 mg/mL 75 mg/mL <1 mg/mL
S1030 Panobinostat (LBH589) <1 mg/mL 69 mg/mL <1 mg/mL
S1045 Trichostatin A (TSA) <1 mg/mL 23 mg/mL <1 mg/mL
S1122 Mocetinostat (MGCD0103) <1 mg/mL 13 mg/mL <1 mg/mL
S8648 ACY-738 <1 mg/mL 54 mg/mL 1 mg/mL
S8567 Tucidinostat (Chidamide) <1 mg/mL 78 mg/mL 2 mg/mL
S8502 TMP195 <1 mg/mL 91 mg/mL 91 mg/mL
S8464 Citarinostat (ACY-241) <1 mg/mL 41 mg/mL 93 mg/mL
S1085 Belinostat (PXD101) <1 mg/mL 64 mg/mL <1 mg/mL
S3020 Romidepsin (FK228, Depsipeptide) <1 mg/mL 10 mg/mL <1 mg/mL
S1484 MC1568 <1 mg/mL 13 mg/mL <1 mg/mL
S2627 Tubastatin A HCl <1 mg/mL 74 mg/mL <1 mg/mL
S2170 Givinostat (ITF2357) <1 mg/mL 95 mg/mL 3 mg/mL
S1095 Dacinostat (LAQ824) <1 mg/mL 76 mg/mL <1 mg/mL
S1194 CUDC-101 <1 mg/mL 20 mg/mL <1 mg/mL
S1096 Quisinostat (JNJ-26481585) 2HCl <1 mg/mL 79 mg/mL <1 mg/mL
S1515 Pracinostat (SB939) <1 mg/mL 72 mg/mL 27 mg/mL
S2012 PCI-34051 <1 mg/mL 59 mg/mL <1 mg/mL
S1422 Droxinostat <1 mg/mL 49 mg/mL 49 mg/mL
S1090 Abexinostat (PCI-24781) <1 mg/mL 80 mg/mL <1 mg/mL
S7229 RGFP966 <1 mg/mL 72 mg/mL <1 mg/mL
S2244 AR-42 <1 mg/mL 63 mg/mL 63 mg/mL
S8001 Ricolinostat (ACY-1215) <1 mg/mL 86 mg/mL <1 mg/mL
S1168 Valproic acid sodium salt (Sodium valproate) 33 mg/mL 33 mg/mL 33 mg/mL
S2818 Tacedinaline (CI994) <1 mg/mL 54 mg/mL <1 mg/mL
S2759 CUDC-907 <1 mg/mL 102 mg/mL <1 mg/mL
S1999 Sodium butyrate 22 mg/mL <1 mg/mL 22 mg/mL
S1848 Curcumin <1 mg/mL 73 mg/mL <1 mg/mL
S2779 M344 <1 mg/mL 62 mg/mL 4 mg/mL
S2239 Tubacin <1 mg/mL 100 mg/mL <1 mg/mL
S7292 RG2833 (RGFP109) <1 mg/mL 68 mg/mL 10 mg/mL
S2693 Resminostat <1 mg/mL 70 mg/mL 70 mg/mL
S1703 Divalproex Sodium 62 mg/mL 62 mg/mL 62 mg/mL
S8043 Scriptaid <1 mg/mL 65 mg/mL <1 mg/mL
S4125 Sodium Phenylbutyrate 30 mg/mL 8 mg/mL <1 mg/mL
S8049 Tubastatin A <1 mg/mL 67 mg/mL <1 mg/mL
S7324 TMP269 <1 mg/mL 100 mg/mL 2 mg/mL
S7595 Santacruzamate A (CAY10683) <1 mg/mL 55 mg/mL 55 mg/mL
S7617 Tasquinimod <1 mg/mL 81 mg/mL 11 mg/mL
S7726 BRD73954 <1 mg/mL 56 mg/mL 9 mg/mL
S7593 Splitomicin <1 mg/mL 39 mg/mL 39 mg/mL
S7278 HPOB <1 mg/mL 62 mg/mL 38 mg/mL
S7569 LMK-235 <1 mg/mL 58 mg/mL 58 mg/mL
S7473 Nexturastat A <1 mg/mL 68 mg/mL 2 mg/mL
S8323 ITSA-1 (ITSA1) <1 mg/mL 58 mg/mL 5 mg/mL
S2341 (-)-Parthenolide <1 mg/mL 49 mg/mL 49 mg/mL
S7596 CAY10603 <1 mg/mL 89 mg/mL 5 mg/mL
S7555 4SC-202 <1 mg/mL 89 mg/mL <1 mg/mL
S7689 BG45 <1 mg/mL 42 mg/mL 2 mg/mL

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S1047

Vorinostat (SAHA, MK0683)

Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM in a cell-free assay.

S1053

Entinostat (MS-275)

Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Phase 3.

S1030

Panobinostat (LBH589)

Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.

S1045

Trichostatin A (TSA)

Trichostatin A (TSA) is an HDAC inhibitor with IC50 of ~1.8 nM in cell-free assays.

S1122

Mocetinostat (MGCD0103)

Mocetinostat (MGCD0103) is a potent HDAC inhibitor with most potency for HDAC1 with IC50 of 0.15 μM in a cell-free assay, 2- to 10- fold selectivity against HDAC2, 3, and 11, and no activity to HDAC4, 5, 6, 7, and 8. Phase 2.

S8648New

ACY-738

ACY-738 inhibits HDAC6 with low nanomolar potency (IC50=1.7 nM) and a selectivity of 60- to 1500-fold over class I HDACs.

S8567New

Tucidinostat (Chidamide)

Chidamide is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.

S8502New

TMP195

TMP195 is a selective, first-in-class, class IIa HDAC inhibitor with IC50 of 300 nM in cell-based class IIa HDAC assays.

S8464New

Citarinostat (ACY-241)

Citarinostat (ACY-241) is an orally available selective HDAC6 inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.

S1085

Belinostat (PXD101)

Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors.

S3020

Romidepsin (FK228, Depsipeptide)

Romidepsin (FK228, depsipeptide) is a potent HDAC1 and HDAC2 inhibitor with IC50 of 36 nM and 47 nM in cell-free assays, respectively.

S1484

MC1568

MC1568 is a selective HDAC inhibitor for maize HD1-A with IC50 of 100 nM in a cell-free assay. It is 34-fold more selective for HD1-A than HD1-B.

S2627

Tubastatin A HCl

Tubastatin A HCl is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).

S2170

Givinostat (ITF2357)

Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.

S1095

Dacinostat (LAQ824)

Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.

S1194

CUDC-101

CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1.

S1096

Quisinostat (JNJ-26481585) 2HCl

Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, 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. Phase 2.

S1515

Pracinostat (SB939)

Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.

S2012

PCI-34051

PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM in a cell-free assay. It has greater than 200-fold selectivity over HDAC1 and 6, more than 1000-fold selectivity over HDAC2, 3, and 10.

S1422

Droxinostat

Droxinostat is a selective inhibitor of HDAC, mostly for HDACs 6 and 8 with IC50 of 2.47 μM and 1.46 μM, greater than 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.

S1090

Abexinostat (PCI-24781)

Abexinostat (PCI-24781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.

S7229

RGFP966

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.

S2244

AR-42

AR-42 is an HDAC inhibitor with IC50 of 30 nM. Phase 1.

S8001

Ricolinostat (ACY-1215)

Ricolinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Phase 2.

S1168

Valproic acid sodium salt (Sodium valproate)

Valproic acid sodium salt (Sodium valproate) is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

S2818

Tacedinaline (CI994)

Tacedinaline (CI994) is a selective class I HDAC inhibitor with IC50 of 0.9, 0.9, 1.2, and >20 μM for human HDAC 1, 2, 3, and 8, respectively. Phase 3.

S2759

CUDC-907

CUDC-907 is a dual PI3K and HDAC inhibitor for PI3Kα and HDAC1/2/3/10 with IC50 of 19 nM and 1.7 nM/5 nM/1.8 nM/2.8 nM, respectively. Phase 1.

S1999

Sodium butyrate

Sodium butyrate, sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).

S1848

Curcumin

Curcumin is the principal curcuminoid of the popular Indian spice turmeric, which is a member of the ginger family (Zingiberaceae). It is an inhibitor of p300 histone acetylatransferase(IC50~25 μM) and Histone deacetylase; activates Nrf2 pathway and supresses the activation of transcription factor NF-κB.

S2779

M344

M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.

S2239

Tubacin

Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM in a cell-free assay, approximately 350-fold selectivity over HDAC1.

S7292

RG2833 (RGFP109)

RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.

S2693

Resminostat

Resminostat dose-dependently and selectively inhibits HDAC1/3/6 with IC50 of 42.5 nM/50.1 nM/71.8 nM, less potent to HDAC8 with IC50 of 877 nM.

S1703

Divalproex Sodium

Divalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy.

S8043

Scriptaid

Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.

S4125

Sodium Phenylbutyrate

Sodium phenylbutyrate is a histone deacetylase inhibitor, used to treat urea cycle disorders.

S8049

Tubastatin A

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).

S7324

TMP269

TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

S7595

Santacruzamate A (CAY10683)

Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor with IC50 of 119 pM for HDAC2, >3600-fold selectivity over other HDACs.

S7617

Tasquinimod

Tasquinimod is an orally active antiangiogenic agent by allosterically inhibiting HDAC4 signalling. Phase 3.

S7726

BRD73954

BRD73954 is a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

S7593

Splitomicin

Splitomicin is a selective NAD(+)-dependent histone deacetylase Sir2p inhibitor with IC50 of 60 μM, showing a higher activity in a cell-based assay.

S7278

HPOB

HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.

S7569

LMK-235

LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.

S7473

Nexturastat A

Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs.

S8323

ITSA-1 (ITSA1)

ITSA-1 (ITSA1) is an HDAC activator via TSA suppression, but shows no activity towards other HDAC inhibitors.

S2341

(-)-Parthenolide

(-)-Parthenolide, an inhibitor of the Nuclear Factor-κB Pathway, specifically depletes HDAC1 protein without affecting other class I/II HDACs; Also promotes the ubiquitination of MDM2 and activates p53 cellular functions.

S7596

CAY10603

CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.

S7555

4SC-202

4SC-202 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.

S7689

BG45

BG45 is a class I HDAC inhibitor with IC50 of 289 nM, 2.0 µM, 2.2 µM and >20 µM for HDAC3, HDAC1, HDAC2, and HDAC6 in cell-free assays, respectively.

Catalog No. Information Product Use Citations Product Validations
A5000New

HDAC2 Rabbit Recombinant mAb

A5021New

HDAC6 Rabbit Recombinant mAb

Tags: HDAC inhibition | HDAC cancer | HDAC assay | histone deacetylase activity | HDAC inhibitors cancer | HDAC activity assay | HDAC activation | HDAC inhibitor mechanism | selective HDAC inhibitors | HDAC phosphorylation | HDAC inhibitor drugs | HDAC inhibitors in clinical trials | HDAC inhibitors list | HDAC inhibitor review