hdac-in-6

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

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].

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.

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-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-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].

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-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].

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.

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.

HDAC4 CHDI Degrader 11 is a potent, selective degrader of HDAC4 (PROTAC) with DC_50 values of 4 nM and 6 nM in Jurkat E6-1 and Jurkat cells, respectively. This compound integrates the class IIa HDAC inhibitor trifluoromethyloxadiazole with a ligand for the Von Hippel-Lindau (VHL) protein through a linker. Demonstrating significant efficacy, HDAC4 CHDI Degrader 11 achieves a DC_50 value of 1 nM in a mouse cell model of Huntington's disease. For enhanced degradation in neuroblastoma cell lines, it can be administered alongside the P-glycoprotein inhibitor, Elacridar.

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-53 is an orally active, selective inhibitor of HDAC1-3, with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. It exhibits no inhibitory effects on class II HDACs (HDAC4, 5, 6, 7, 9; IC50 >10 μM). The compound induces caspase-dependent apoptosis and significantly hampers the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice with MC38 colon cancer [1].

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].

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.

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.

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.

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].

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.

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

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.

Butyricacid-d7 is a deuterated compound of Butyricacid. Butyricacid has a CAS number of 107-92-6. Butyric acid is a fatty acid isolated from many dairy products that exhibits anticancer activity. Butyric acid inhibits histone deacetylases (HDACs) and induces apoptosis and G1 phase cell cycle arrest in glioma cells. Additionally, butyric acid stimulates epithelial cell proliferation at low doses and inhibits proliferation at high doses.

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.

KH16 is a potent HDAC inhibitor that specifically targets class I HDACs (HDAC1, HDAC2 and HDAC3) with IC50 values between 6 and 34 nM. KH16 is able to stimulate apoptosis and can inhibit gene expression patterns in a wide range of tumor cells.