histone deacetylase 6

Vorinostat (SAHA) 是一种泛的组蛋白脱乙酰酶 (HDAC) 抑制剂 (IC50=10 nM)，对 HDAC1 2 3 6 7 11 均有抑制活性。 Vorinostat 具有抗肿瘤活性，可以诱导细胞分化，阻滞细胞周期，诱导细胞凋亡。

HDAC6 degrader 9c 是一种小分子组蛋白脱乙酰酶 6 （HDAC6） 降解剂，可用于研究癌症或其他疾病。

MC2590 是一种具有有效性和选择性的组蛋白脱乙酰酶 (HDAC) 抑制剂 ，抑制 HDAC1-3、-6、-8 和 -10 的活性，诱导细胞周期停滞，促进细胞凋亡。

Ricolinostat (Rocilinostat) 是一种选择性HDAC6抑制剂，IC50为 5 nM。它还抑制HDAC1，HDAC2和HDAC3，IC50分别为 58，48 和 51 nM。

SW-100 是一种选择性组蛋白去乙酰化酶 6 抑制剂，IC50为2.3 nM。它有提高的穿过血脑屏障的能力，相对于其他 HDAC 同工酶，还显示出对 HDAC6 的至少高 1000 倍的选择性。

Trichostatin A S-isomer is the s-isomer of Trichostatin A. Trichostatin A is a histone deacetylase inhibitors (HDIs or HDACIs) that have a broad spectrum of epigenetic activities. Trichostatin A inhibits HDACs 1, 3, 4, 6 and 10 with IC50 values around 20

LSD1 HDAC6-IN-1 is an orally active compound that functions as a dual inhibitor, targeting lysine specific demethylase 1 (LSD1) and histone deacetylase 6 (HDAC6). This compound demonstrates promising anti-tumor activity and is particularly valuable for research focused on multiple myeloma (MM) [1].

Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2]. Givinostat (ITF2357) at 10 mg kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of Givinostat (ITF-2357) (1 or 5 mg kg), there is a 22% reduction for 1 mg kg and 40% for 5 mg kg[1]. [1]. Li S, et al. Specific inhibition of histone deacetylase 8 reduces gene expression and production of proinflammatory cytokines in vitro and in vivo. J Biol Chem. 2015 Jan 23;290(4):2368-78. [2]. Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39. [3]. Leoni F, et al. The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo. Mol Med. 2005 Jan-Dec;11(1-12):1-15.

NR-160 is an inhibitor of histone deacetylase 6 (HDAC6; IC50= 0.03 μM).1It is selective for HDAC6 over HDAC1, -2, -3, -4, and -8 (IC50s = 5.18, 2.26, 8.48, 55.4, and 14.7 μM, respectively). NR-160 is cytotoxic against a panel of seven cancer cell lines (IC50s = 22.5-51.8 μM). It enhances cytotoxicity induced by bortezomib in HL-60 cells, as well as cytotoxicity induced by epirubicin or daunorubicin in CCRF-HSB-2 T cell acute lymphoblastic leukemia cells.

(2R S)-6-PNG (6-Prenylnaringenin) 是新型天然组蛋白脱乙酰酶抑制剂，具有抗癌抗肿瘤活性，可阻断T型钙通道可减轻小鼠的神经性和内脏疼痛。

PTG-0861 is a highly specific inhibitor of histone deacetylase 6 (HDAC6), demonstrating an impressive IC50 value of 5.92 nm. This compound effectively triggers apoptosis and holds potential for research pertaining to acute myeloid leukemia, multiple myeloma, and other hematological cancers [1].

HDAC6-IN-15 是一种选择性组蛋白脱乙酰酶 6(HDAC6)抑制剂。HDAC6-IN-15 对 HDAC6具有有效的抑制活性，IC50值为 38.2 nM。HDAC6-IN-15 可用于癌症和神经退行性疾病的研究。

HDAC6-IN-16（compound 5c）是基于Quinazolin-4(3H)-One的一种HDAC6抑制剂，具备抑制肿瘤细胞集落形成的抗癌活性。该化合物能够引发G2期细胞周期阻滞并诱导细胞凋亡(apoptosis)。

HDAC6-IN-24（化合物N1）是一种HDAC6抑制剂。

HDAC6-IN-21（化合物13）为一种靶向组蛋白去乙酰化酶6（histone deacetylase 6（HDAC6））的不可逆抑制剂。

HDAC6-IN-38 (Compound Z-7) 作为一种组蛋白脱乙酰酶 6 (HDAC6) 的抑制剂，其 IC50 值达到 3.25 nM。此外，它还能抑制 MGC-803 细胞的增殖。

HPO-DAEE (4-Hydroperoxy-2-decenoic acid ethyl ester) 通过诱导 Nrf2的核积累和激活抗氧化反应元件 (ARE) 来发挥作用。此化合物增强了通过 Nrf2-ARE 信号通路的抗氧化基因（例如：HO-1）的表达，并促进了活性氧 (reactive oxygen species) 的生成。同时，HPO-DAEE 抑制了组蛋白脱乙酰酶的活性，并通过促进组蛋白的乙酰化来上调细胞外超氧化物歧化酶的表达。此外，该化合物还通过激活 Nrf2-ARE 和 eIF2α-ATF4 路径，有效防止了6-羟基多巴胺引起的细胞死亡。

HDAC6-IN-46（compound 12）作为选择性的组蛋白去乙酰化酶6（HDAC6）抑制剂，展现出了6.2 nM的IC50。该化合物主要应用于阿尔茨海默病的相关研究。

SelSA是一种选择性针对组蛋白去乙酰化酶6 (HDAC6) 的口服有效抑制剂，其IC50值为56.9 nM。此化合物能够抑制ERK1 2的磷酸化，并在IC50为0.58-2.6 μM的范围内抑制乳腺癌和肝癌细胞的增殖。同时，SelSA抑制Huh7细胞的迁移和侵袭，并可诱导细胞凋亡(apoptosis)。在小鼠模型中，SelSA展示了其抗肿瘤活性。