hdac-in-6

HDAC-IN-6 is an HDAC inhibitor, targeting HDAC2, HDAC3, HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9.

Fluoxetine succinate ester is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder, bulimia nervosa, panic disorder, and premenstrual dysphoric disorder.

HDAC-IN-65 (compound 6) is a selective histone deacetylase (HDAC) inhibitor with an IC50 value of 2.5 μM. It is a prodrug offering excellent bioreductive properties.

HDAC-IN-64 (Compound 13), an HDAC inhibitor, demonstrates potent inhibition of HDAC4/5/6/7/9 with IC50 values of 24, 45, 85, 31, and 37 nM, respectively. It exhibits anti-proliferative and anti-migration effects on prostate cancer (PCA) cells, specifically inhibiting the growth of LNCaP and RWPE-1 cells with GI50 values of 0.32 and 1.1 μM, respectively [1].

HDAC-IN-66 (compound 2F) is a selective inhibitor of HDAC and a derivative of Pomalidomide, effectively inhibiting hematological tumor cells.

HDAC-IN-68 (Compound 29) is a potent HDAC inhibitor that disrupts microtubule structures and suppresses tumor growth. This compound notably inhibits class I HDACs, specifically HDAC1, HDAC2, and HDAC3, with IC50 values of 5.1, 11.5, and 8.8 nM, respectively.

HDAC-IN-68 (hydrochloride) (Compound 29) is an HDACs inhibitor with an IC50 value of 0.04 μM and induces microtubule fragmentation by activating katanin, a microtubule-severing protein. It is applicable in cancer research.

HDAC-IN-60 (compound 21a), a potent histone deacetylase (HDAC) inhibitor, promotes intracellular reactive oxygen species (ROS) production, induces DNA damage, arrests the cell cycle at the G2/M phase, and triggers mitochondria-related apoptotic pathways, leading to cell apoptosis [1].

HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It effectively suppresses MV4-11 cell proliferation (IC50 of 92 nM), induces apoptosis, and arrests the cell cycle in MV4-11 cells. This compound is applied in acute myeloid leukemia (AML) research [1].

HDAC-IN-62 (Compound 5), an HDAC inhibitor, exhibits IC50 values of 0.78, 1.0, and 1.2 μM for HDAC6, HDAC8, and HDAC11, respectively. This compound suppresses microglial activation via autophagy induction and reduces nitric oxide production, demonstrating anti-inflammatory and antidepressant properties. Additionally, HDAC-IN-62 has been shown to inhibit microglial activation in mouse brains [1].

HDAC-IN-61 (compound 12k) is a potent, orally active histone deacetylase (HDAC) inhibitor with anticancer activity, exhibiting an IC50 of 30 nM against Bel-7402 cells and is utilized for cancer research [1].

HDAC-IN-67 (compound 27f) acts as an inhibitor of HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and triggers apoptosis, while also displaying antitumor activity [1].

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.

HDAC6-IN-49 (Compound 3) is an inhibitor of HDAC, with IC50 values of 0.012 and 0.735 µM against HDAC6 and HDAC1, respectively. Additionally, it inhibits MAO-B, cholinesterase (ChE), histamine receptor (H3R), and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective effects in SH-SY5Y cells and enhances cognitive functions and motor abilities in fruit fly models of Parkinson's disease and C. elegans models of Alzheimer's disease.

ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.

CDK4/6/HDAC-IN-1 (Compound N14) is a dual-target inhibitor of CDK4/6 and HDAC, with IC50 values of 7.23 nM for CDK4, 13.20 nM for CDK6, 55.66 nM for HDAC1, and 48.38 nM for HDAC6. It induces apoptosis and G0/G1 phase arrest through the HDAC-p21-CDK signaling pathway and can inhibit hepatocellular carcinoma.

CM-444 is an inhibitor of HDAC (IC50 ranging from 6 nM to 0.6 μM) and DNA methyltransferase (DNMT, IC50 ranging from 1.8 to 2.3 μM). This compound induces differentiation in acute myeloid leukemia cells, exhibits anti-leukemia activity, and enhances survival rates in mouse models.

HDAC1/6-IN-3 is an effective HDAC inhibitor with significant inhibitory effects on HDAC1 (IC50= 1.1 nM) and HDAC6 (IC50= 2.7 nM). In HepG2 cells, it causes cell cycle arrest at the G0/G1 phase and induces apoptosis and pyroptosis. Furthermore, HDAC1/6-IN-3 demonstrates notable antitumor activity in HepG2 tumor xenograft models. This compound is applicable for cancer research, including studies on liver, lung, colon, and breast cancers.

Givinostat (ITF-2357) is an HDAC inhibitor with IC50 values of 198 nM for HDAC1 and 157 nM for HDAC3.

PIM-1/HDAC-IN-1 (compound 4d) is a potent PIM-1 inhibitor with an IC50 of 343.87 nM, and it exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. Additionally, it induces apoptosis and causes G2/M phase cell cycle arrest in MCF-7 cell lines, specifically inducing pre-G1 apoptosis [1].

CDK/HDAC-IN-1 exhibits potent inhibitory activity towards CDK2/4/6 and HDAC6, with IC50 values of 60.9 ± 2.9 nM, 276 ± 22.3 nM, 27.2 ± 4.2 nM, and 128.6 ± 0.4 nM, respectively.

HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82 nM for HDAC 1, 45 nM for HDAC 3, and 24 nM for HDAC 6, and a weak PI3K/mTOR inhibitor with IC50 values of 3.6 μM for PI3K and 3.7 μM for mTOR, exhibiting a broad-spectrum anti-proliferative effect.

HDAC-IN-38 is a potent inhibitor of HDAC. HDAC-IN-38 has similar micromolar inhibitory effects on HDAC1, 2, 3, 5, 6 and 8, and also increases histone acetylation levels (H3K14 or H4K5). HDAC-IN-38 increases cerebral blood flow (CBF), reduces cognitive impairment and improves hippocampal atrophy.

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.