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HDAC
T3108 CUDC-101 CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively.
T1983 CAY10603 CAY10603 is a potent and selective inhibitor of HDAC6.
T1602 Valproic acid sodium salt Valproate Sodium is the sodium salt form of valproic acid with anti-epileptic activity. Valproate sodium is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, valproate sodium increases concentrations of gamma-aminobutyric acid (GABA)
T1888 CI-994 Tacedinaline (CI994) is a selective class I HDAC inhibitor with potential antineoplastic activity.
T4370 Resminostat hydrochloride Resminostat hydrochloride is an effective inhibitor of HDAC1/HDAC3/HDAC6 (IC50: 42.5/50.1/71.8 nM), respectively, and shows less potent activities against HDAC8 (IC50: 877 nM).
T6639 RG2833 (RGFP109) RG2833 (RGFP109), a brain-penetrant HDAC inhibitor, is with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3, respectively.
T3516 Minomustine EDO-S101 is a pan HDAC inhibitor with IC50 values of 9, 9 and 25 nM for HDAC1, HDAC2 and HDAC3 , respectively.
T1966 Tubastatin A BASE Tubastatin A 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.
T6006 Romidepsin (FK228, Depsipeptide) Romidepsin is an intravenously administered histone deacetylase inhibitor and antineoplastic agent that is approved for use in refractory or relapsed cutaneous and peripheral T cell lymphomas.
T6161 Tubastatin A hydrochloride Tubastatin A HCl is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).
T1857 TMP269 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.
T3983 TMP 195 TMP195 is a selective class IIa histone deacetylase (HDAC) inhibitor.
T2489 Rocilinostat (ACY-1215) Ricolinostat is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.
T3661 ACY-241 ACY-241, also known as Citarinostat, 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, th
T2078 CUDC-907 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 ac
T1762 RGFP 966 RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
T3509 ACY-738 ACY-738 demonstrates inhibitory activity against recombinant HDAC6 (IC50: 1.7 nM), with respective average selectivity over class I HDACs being 100-fold.
T1819 Nexturastat A Nexturastat A is an effective and specific HDAC6 inhibitor (IC50: 5 nM). Its selectivity is >190-fold than other HDACs.
T6061 LMK-235 LMK-235 is a potent HDAC inhibitor, and is used in cancer research.
T2430 HPOB HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), >30-fold selectivity over other HDACs.
T6421 BRD73954 BRD73954, an effective and specific HDAC inhibitor, which is with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
T2266 CAY10683 (SantacruzaMate A) Santacruzamate A (CAY10683) is a potent and selective HDAC inhibitor.
T1583 Vorinostat Vorinostat is a Histone Deacetylase Inhibitor. Vorinostat is a synthetic hydroxamic acid derivative with antineoplastic activity. This allows the hydroxamic moiety to chelate zinc ion located in the catalytic pockets of HDAC, thereby inhibiting deacetylation and leading to an accumulation of both hy
T1535 Sodium Phenylbutyrate Sodium Phenylbutyrate, 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 populatio
T4389 SR-4370 SR-?4370 is an HDAC inhibitor. SR-?4370 exhibited IC50 values of 0.5 μM, 0.1 μM and 0.06 μM towards HDAC1, HDAC2 and HDAC3, resp. SR-?4370 is reported in WO 2015153516.
T3358 ITSA1 ITSA-1 is membrane permeable and specifically suppresses TSA inhibition of HDAC (histone deacetylase), but shows no activity towards other HDAC inhibitors.
T6233 Entinostat (MS-275) Entinostat (MS-275) is an effective inhibitor of HDAC1 and HDAC3. The IC50 of Entinostat for HDAC1 and HDAC3 is 0.51 μM and 1.7 μM, respectively.
T2157 Histone Deacetylase Inhibitor III(M344) M344 is a potent HDAC inhibitor with IC50 of 100 nM and able to induce cell differentiation.
T6695 Tasquinimod Tasquinimod 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 do
T6980 Scriptaid Scriptaid is an inhibitor of HDAC,and has a greater effect on acetylated H4 than H3.
T2383 Panobinostat Panobinostat is an oral histone deacetylase inhibitor and antineoplastic agent that is approved for use in combination with other agents in refractory or relapsed multiple myeloma.
T2454 Dacinostat LAQ824 (Dacinostat) is a novel HDAC inhibitor with IC50 of 32 nM and is an activator of the p21 promoter.
T1852 Belinostat Belinostat is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize dr
T3206 Histone Deacetylase Inhibitor IV An effective Histone Deacetylase Inhibitor.
T3204 BML-210 BML-210 is a new-type HDAC inhibitor.
T6327 Tubacin Tubacin is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM, approximately 350-fold selectivity over HDAC1.
T3205 UF010 UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively.
T1083 Theophylline Theophylline is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agent
T6270 Trichostatin A (TSA) Trichostatin A is a natural derivative of dienohydroxamic acid isolated from species of the bacterial genus Streptomyces. Trichostatin A (TSA) reversibly and specifically inhibits histone deacetylases, resulting in hyperacetylation of core histones which modulate chromatin structure. The increase in
T1083L Theophylline monohydrate Theophylline appears to inhibit phosphodiesterase and prostaglandin production, regulate calcium flux and intracellular calcium distribution, and antagonize adenosine. Theophylline is a natural alkaloid derivative of xanthine isolated from the plants Camellia sinensis and Coffea arabica. Physiologic
T2205 Theophylline-7-acetic acid Theophylline-7-acetic acid, a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects
T2512 Mocetinostat Mocetinostat (MGCD0103) is an orally available, Class 1-selective and small molecule HDAC inhibitor with most potency for HDAC1 (IC50: 0.15 μM) in a cell-free assay, 2- to 10- fold selectivity against HDAC2/3/11, and no activity to HDAC4/5/6/7/8.
T3937 Methyl L-histidinate dihydrochloride Inhibition of histidine decarboxylase in Sprague-Dawley rat stomach assessed as decrease in 14CO2 production with activty value of 1.8μM
T2025 chidamide analog Chidamide(CS055; HBI-8000) is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM).
T0431 PCI-24781 (Abexinostat) PCI-24781 (Abexinostat) is a new pan-HDAC inhibitor mainly targeting HDAC1 (Ki: 7 nM), also have moderate inhibitory for HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.
T3199 PTACH PTACH (NCH-51) is a SAHA-based inhibitor of human HDAC. It can potently inhibit the growth of various human Y cells (EC50: 1 to 10 μM).
T2023 MC1568 MC1568 is a specific HDAC inhibitor for maize HD1-A (IC50: 100 nM, in a cell-free assay). It is 34-fold more selective for HD1-A than HD1-B.
T6637 Resminostat Resminostat is an orally bioavailable inhibitor of histone deacetylases (HDACs) with potential antineoplastic activity.
T6055 Quisinostat (JNJ-26481585) Quisinostat (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.
T6865 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.
T3878 Raddeanin(Anemodeanin) A Raddeanin A has moderate inhibitory activity against histone deacetylases (HDACs). Raddeanin A has high antiangiogenic potency, antitumor activity.
T6362 4SC-202 free base 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.
T2294 BG45 BG45 is an HDAC I type inhibitor with IC50 of 289 nM, 2.0 μM, 2.2 μM and >20 μM for HDAC3/1/2/6 in cell-free assays, respectively.
T1890 Pracinostat Pracinostat is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in clinical 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 hematologi
T6392 AR-42 AR-42 is an HDAC inhibitor (IC50: 30 nM).
T3193 Pimelic diphenylamide 106 Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (with IC50 values of 150 nM , 760 nM and 370 nM for HDAC 1, 2, and 3, respectively), showing no activity against class II HDACs.
T6325 PCI-34051 PCI-34051 is an effective and selective HDAC8 inhibitor (IC50: 10 nM).
T6481 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.
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