hdac2

HDAC2-IN-1 (Compound 17) is an orally active, competitive HDAC2 inhibitor (IC50: 0.5 μM) that crosses the blood-brain barrier and also inhibits HDAC1 (IC50: 1.61 μM) and HDAC8 (IC50: 0.98 μM).

PI3K HDAC-IN-2 is a potent dual PI3K HDAC inhibitor with IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, 29 nM for PI3Kδ, and 1.3 nM for HDAC1. PI3K HDAC-IN-2 is selective for PI3Kδ and class I and IIb HDACs, exhibiting significant anticancer effects.

Tubulin HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with IC50 values of 0.403 μM for HDAC1, 0.591 μM for HDAC2, 3.552 μM for HDAC3, and 0.459 μM for HDAC6. The compound induces G2 phase cell cycle arrest, promotes apoptosis, hampers hematoma and solid tumor cell proliferation, diminishes tumor metastasis, and inhibits tumor growth in a liver tumor allograft mouse model [1].

CDK HDAC-IN-2 is a potent dual HDAC CDK inhibitor that acts on HDAC1 (IC50: 6.4 nM), HDAC2 (IC50: 0.25 nM), HDAC3 (IC50: 45 nM), HDAC6 and 8 (IC50 > 1000 nM), CDK1 (IC50: 8.63 nM), CDK2 (IC50: 0.30 nM), and CDK4, 6, and 7 (IC50 > 1000 nM). CDK HDAC-IN-2 can arrest the cell cycle in the G2 M phase and induce apoptosis, demonstrating excellent anti-proliferative and significant anti-tumor effects.

JAK HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1 2 and HDAC3 6 at nanomolar concentrations. This compound exhibits proapoptotic properties, inhibits histone deacetylation, and impedes STAT3 phosphorylation, demonstrating notable antiproliferative activity against various hematological malignancies and solid tumors [1].

A2AAR HDAC-IN-2 is a potent dual A2AAR HDAC inhibitor with good affinity for A2AAR (Ki: 10.3 nM) and effective HDAC1 inhibition (IC50: 18.5 nM). A2AAR HDAC-IN-2 is applicable in anti-tumour studies.

c-Met HDAC-IN-2 is a potent dual inhibitor of c-Met and HDAC, exhibiting IC50 values of 5.40 nM for c-Met and 18.49 nM for HDAC1, respectively. It demonstrates antiproliferative effects on various cancer cell lines, induces G2 M-phase arrest, and triggers apoptosis in HCT-116 cells, making it a promising candidate for anti-cancer resistance research.

Top HDAC-IN-2 (45b) is a dual Top and HDAC inhibitor that induces apoptosis and demonstrates significant anti-tumor effects.

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

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.

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.

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].

HDAC-IN-52, a pyridine-containing HDAC inhibitor, effectively inhibits HDAC1, HDAC2, HDAC3, and HDAC10 with IC50 values of 0.189, 0.227, 0.440, and 0.446 μM, respectively. HDAC-IN-52 can be used in cancer research.

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.

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.

HDAC-IN-51 is an HDAC inhibitor.

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.

ACY-957 (HDAC Inhibitor C001) is an orally active and selective inhibitor of HDAC1 and HDAC2 (IC50s: 7 nM, 18 nM, and 1300 nM against HDAC1 2 3) and shows no inhibition on HDAC4 5 6 7 8 9.

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.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50 values of 30 nM and 16 nM, respectively. It exhibits greater selectivity for HDAC2 3 over other HDAC isomers and induces apoptosis in myeloid leukemic cells, indicating potential therapeutic use in leukemia and as an anti-stroke agent [1] [2].

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.

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.

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.

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.

SantacruzaMate A (CAY-10683) is a potent and selective HDAC inhibitor.

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.

ACY-738 demonstrates inhibitory activity against recombinant HDAC6 (IC50: 1.7 nM), with respective average selectivity over class I HDACs being 100-fold.

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.

7,4'-Dihydroxyflavone (4',7-Dihydroxyflavone) can induce transcription of nodulation (nod) genes in Rhizobium meliloti. It has inhibitory activities against COX-2.

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.

CXD101 is a novel class I-selective HDACi (HDAC1 (IC50 : 63nM), HDAC2 (IC50 :570nM), HDAC3 (IC50 :550nM)). CXD101(CXD-101) has no activity against HDAC class II

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

BRD3308 is a highly selective inhibitor of HDAC3(IC50 of 54 nM), attenuating PE-mediated phosphorylation of ERK but not JNK.

LMK-235 is a potent HDAC inhibitor, and is used in cancer research.

Pimelic diphenylamide 106 (RGFA-8) 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.

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.

Ricolinostat (Rocilinostat) is an orally bioavailable, specific inhibitor of histone deacetylase 6 (HDAC6) with potential antineoplastic activity.

Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor targeting HDAC1 2 3 with IC50 values of 1.20 1.12 0.57 μM, respectively, and also inhibits Lysine-specific demethylase 1 (LSD1).

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.

HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with a Ki of 60 nM for HDAC2 and 30 nM for HDAC6, exhibiting antitumor effects.

NKL 22 (Histone Deacetylase Inhibitor IV) is an effective Histone Deacetylase Inhibitor.

Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 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.

M122 is a selective histone deacetylase HDAC1 and HDAC2 inhibitor and potent antitumor agent.

CM-414 is a dual inhibitor of HDACs and PDE5 for the Treatment of Alzheimer’s Disease (IC50 values of 60 nM, 310 nM, 490 nM, 322 nM, and 91 nM against PDE5, HDAC1, HDAC2, HDAC3, and HDAC6, respectively). Chronic treatment of Tg2576 mice with CM-414 dimini

MRLB-223 is a potent inhibitor of HDAC1 and HDAC2.

HDAC-IN-41 (Compound 7c) is an orally active, selective class I HDAC inhibitor targeting HDAC1 (IC50: 0.62 μM), HDAC2 (IC50: 1.46 μM), and HDAC3 (IC50: 0.62 μM). HDAC-IN-41 also exhibits NO-releasing activity.

CDK HDAC-IN-3 is an orally active dual inhibitor of HDACs and CDKs, offering potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM, respectively, and is applicable in the treatment of acute myeloid leukemia (AML) [1].

HDAC6-IN-19 (Compound 14g), an HDAC6 inhibitor with an IC50 of 2.68 nM, additionally inhibits HDAC1, HDAC2, and HDAC3, with IC50 values of 61.6 nM, 98.7 nM, and 103 nM, respectively. This compound effectively suppresses the proliferation of various cancer cell lines, such as leukemia, colon cancer, melanoma, and breast cancer [1].