hdac8

HDAC8-IN-20a (HDAC8 inhibitor-20a) is a potent and selective HDAC8 inhibitor with an IC50 of 27 nM. HDAC8-IN-20a blocks activation of growth receptor survival signals.

MDK-7933 (HDAC8-IN-1) is a HDAC8 inhibitor with an IC50 of 27.2 nM in cancer cell lines. MDK-7933 shows antiproliferative effects toward several human lung cancer cell lines (A549, H1299, and CL1-5). HDAC8-IN-1 exhibits cytotoxicity against human lung CL1-5 cells without significant cytotoxicity for normal IMR-90 cells[1].

HDAC8-IN-3 (compound P19) is a highly potent HDAC8 inhibitor with an IC50 value of 9.3 μM, inducing thermal stabilization, cytotoxicity, and apoptosis specifically in leukemic cell lines [1].

HDAC8-IN-4 is a selective HDAC8 inhibitor with IC50 values of 0.15 μM for HDAC8 and 12 μM for HDAC3 [1].

HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor with IC50 values of 0.27 μM and 0.32 μM for smHDAC8 (Schistosoma mansoni histone deacetylase 8) and hHDAC8, respectively. It effectively kills schistosome larvae and significantly reduces egg laying in adult worm pairs [1].

HDAC8-IN-5 (Compound 6a), with an inhibitory concentration (IC50) of 28 nM, is a potent HDAC8 inhibitor suitable for cancer research [1].

HDAC8 BRPF1-IN-1 (Compound 23a) is a dual inhibitor targeting human HDAC8 (IC50: 443 nM) and human BRPF1 (Kd: 67 nM), with low in vitro activity against HDAC1 and HDAC6.

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.

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-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.

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.

SS-208 is a selective inhibitor of HDAC6 (IC50 = 12 nM) with anti-tumor activity. SS-208 shows selectivity over other HDAC subtypes.

Tubastatin A Hydrochloride (TSA HCl) is an effective and specific HDAC6 inhibitor (IC50: 15 nM). It has selectivity (>1000-fold) against all other isozymes except HDAC8 (>57-fold).

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.

Tenovin-6 Hydrochloride is an SIRT1, SIRT2 and HDAC8 inhibitor(IC50s of 21 μM, 10 μM, and 67 μM for SirT1, SirT2, and SirT3, respectively), and is also a potent p53 activator .

BRD73954, an effective and specific HDAC inhibitor, which is with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM, demonstrating greater selectivity for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). It does not increase global histone H4 acetylation or reduce total intracellular HDAC activity but can induce tubulin acetylation[1][2].

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.

Droxinostat (NS 41080) is a selective HDAC inhibitor, primarily targeting HDACs 6 and 8 with IC50 values of 2.47 μM and 1.46 μM, respectively. It is over 8-fold more selective against HDAC3 and shows no inhibition for HDAC1, 2, 4, 5, 7, 9, and 10.

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.

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor and also has microtubule-disrupting ability.

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

HDAC-IN-30 is a multi-target HDAC inhibitor. HDAC-IN-30 inhibits HDAC1 (IC50 =13.4 nM), HDAC2 (IC50 =28.0 nM), HDAC3 (IC50 =9.18 nM), HDAC6 (IC50 =42.7 nM), HDAC8 (IC50 =131 nM). HDAC-IN-30 shows potent antitumor efficacy.

HDAC6-IN-17 (compound 5b) is a potent HDAC6 inhibitor with IC50 values of 150 nM for HDAC6, 1400 nM for HDAC8, and 2300 nM for HDAC4, demonstrating cytotoxic activity against human cancer cell lines and being utilized in cancer research [1].

TH-6 is a potent inhibitor of HDAC, acting on HDAC1 (IC50: 0.115 μM), HDAC2 (IC50: 0.135 μM), HDAC3 (IC50: 0.242 μM), HDAC6 (IC50: 0.138 μM), HDAC8 (IC50: 2.120 μM). TH-6 inhibits cell migration and invasion and exhibits anti-tumour effects.

J1075 is an histone deacetylase 8 (HDAC8) inhibitor.

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.

Thr101, also known as NOX Inhibitor VII, is a dose-dependent inhibitor of HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9. Thr101 is also a NOX inhibitor.

HDAC-IN-31 is a selective, potent, orally active HDAC inhibitor that acts on HDAC1 (IC50: 84.90 nM), HDAC2 (IC50: 168.0 nM), HDAC3 (IC50: 442.7 nM), HDAC8 (IC50>10000 nM). HDAC-IN-31 has good anti-tumour effects. HDAC-IN-31 has shown potential research value in diffuse large B-cell lymphoma.

RTS-V5 is a dual inhibitor of HDAC/proteasome (IC50s: 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively).

HDAC/Top-IN-1 is a broad-spectrum, orally active dual HDAC/Top inhibitor that acts on HDAC1 (IC50: 0.036 μM), HDAC2 (IC50: 0.14 μM), HDAC3 (IC50: 0.059 μM), HDAC6 (IC50: 0.089 μM) and HDAC8 ( IC50: 9.8 μM). HDAC/Top-IN-1 was able to block HEL cells in S-phase and effectively induce apoptosis.

Ebselen oxide (EB-2), a novel variant of HER2 inhibitor for HER2-positive cancers, is an EB-1 analog with antibacterial and antifungal activity, and has shown cytoprotective effects in vitro in addition to cytoprotective effects against HN2.Ebselen oxide inhibits alginate production by Pseudomonas aeruginosa and inhibits HDAC1, HDAC3, HDAC3, and HDAC3. Ebselen oxide inhibits alginate production by Pseudomonas aeruginosa, inhibits HDAC1, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC9, and can be used in the study of fungal infections.

CAY10603 (BML-281) is a potent and selective HDAC6 inhibitor.

PCI-34051 is an effective and selective HDAC8 inhibitor (IC50: 10 nM).

HDAC6-IN-27 (compound 8C), an HDAC inhibitor, exhibits IC 50 values of 15.9 nM, 136.5 nM, and 6180.2 nM against HDAC6, HDAC8, and HDAC1, respectively. It also demonstrates potent antiparasitic effects [1].

SIRT6-IN-3 (compound 8a), a selective SIRT6 inhibitor (IC50 = 7.49 μM), impedes the proliferation of pancreatic ductal adenocarcinoma (PDAC) cells and prompts apoptosis. It enhances the responsiveness of cancer cells to gemcitabine by obstructing the DNA damage repair pathway, thus serving as a valuable tool in pancreatic cancer research [1].

SB379278A is a potent inhibitor of HDAC8(IC50 = 0.5 μM).

HDAC-IN-37 is a potent inhibitor of HDAC, targeting HDAC1 (IC50: 0.0551 μM), HDAC3 (IC50: 1.24 μM), HDAC8 (IC50: 0.948 μM), and HDAC6 (IC50: 34.2 μM). It slowly induces histone acetylation, prevents the transition from G1 to S phase, and induces early apoptosis.

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.

PCI-24781 (Abexinostat (PCI24781)) 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.

Tubulin HDAC-IN-3 (compound 12a) is a potent dual inhibitor of tubulin polymerization and HDAC1 8, with IC50 values of 5.4 μM for tubulin polymerization, and 0.155 and 0.177 μM for HDAC1 and HDAC8, respectively. It obstructs the cell cycle, triggers apoptosis, and suppresses colony formation [1].

H8-A5, a HDAC8 inhibitor, shows antiproliferation activity in MDA-MB-231 cancer cells.

FNDR-20123 is the first safe and effective anti-malarial HDAC inhibitor, acting on both Plasmodium falciparum HDAC (IC50: 31 nM) and human HDAC (IC50: 3 nM). FNDR-20123 inhibited HDAC1 (IC50: 25 nM), HDAC2 (IC50: 29 nM), HDAC3 (IC50: 2 nM), HDAC6 (IC50: 11 nM), HDAC8 (IC50: 282 nM) and, at nanomolar concentrations, HDAC3 (IC50: 2 nM). The inhibitor of HDAC subtype III was also observed at nanomolar concentrations.

NCC-149 is a HDAC8 inhibitor.

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].

SZUH280 is a potent, selective PROTAC (proteolysis targeting chimera) HDAC8 (histone deacetylase 8) degrader, demonstrating a DC50 of 0.58 μM in A549 cells. It induces apoptosis in cancer cells and impedes DNA damage repair, thereby enhancing cellular radiosensitization [1].

NHNB is a selective inhibitor of histone deacetylases-8 (HDAC8). NHNB provides the most potent CE4 inhibitor reported to date.