histone deacetylase 1

ITSA-1 是一种具有膜渗透性的HDAC 激活剂，抵消曲古抑菌素 A (TSA) 诱导的细胞周期停滞，组蛋白乙酰化和转录水平。

R306465 (JNJ-16241199) 是一种具有口服活性和选择性的 I类组蛋白去乙酰化酶 (HDAC 1) 抑制剂，IC50 为 3.3 nM 。R306465 具有广谱的抗肿瘤活性，可诱导组蛋白 3 乙酰化，诱导细胞凋亡，可用于研究实体瘤和血液系统恶性肿瘤。

Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂，对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用， IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性，增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化，并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。

Acetyl Pentapeptide-1 acetate 是一种组蛋白脱乙酰酶抑制剂。

Tefinostat (CHR-2845) 是一种有效的单核细胞 巨噬细胞靶向组蛋白脱乙酰酶 (HDAC) 抑制剂。 Tefinostat 可被胞内酯酶人羧酸酯酶-1 (hCE-1) 裂解成活性酸 CHR-2847。Tefinostat 具有抗肿瘤活性，可用于研究白血病和晚期血液系统恶性肿瘤。

4-Iodo-SAHA (1k) 是一种具有口服活性的I 类和II 类histone deacetylase (HDAC)抑制剂，对 Skbr3、 HT29、 U937、 JA16 和 HL60细胞的EC50值分别为1.1、0.95、0.12、0.24、0.85和1.3 μM。4-Iodo-SAHA (1k) 可用于癌症的研究。

CRT5 是一种吡嗪苯甲酰胺，对经 VEGF 处理的内皮细胞中的所有三种 PKD 亚型 (对 PKD1、PKD2 和 PKD3 的 IC50s 分别为 1、2 和 1.5 nM) 都是一种有效的选择性抑制剂，并且 CRT5 减少 VEGF 诱导的内皮细胞迁移、增殖和微管生成。

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

ATRA-BA hybrid is a mutual prodrug form of all-transretinoic acid and butyric acid .1ATRA-BA hybrid is cleaved to release ATRA and BA in isolated mouse plasma. It inhibits the growth of MDA-MB-231 breast and PC3 prostate cancer cells with GI50values of 0.01 and 1.02 μM, respectively. ATRA-BA (20 μM) has 15-fold greater antiproliferative activity in PC3 cells compared to an equimolar concentration of ATRA and BA. 1.Gediya, L.K., Khandelwal, A., Patel, J., et al.Design, synthesis, and evaluation of novel mutual prodrugs (hybrid drugs) of all-trans-retinoic acid and histone deacetylase inhibitors with enhanced anticancer activities in breast and prostate cancer cells in vitroJ. Med. Chem.51(13)3895-3904(2008)

TW9 is a dual inhibitor of bromodomain 2 (BD2) in bromodomain-containing protein 4 (BRD4) and histone deacetylase 1 (HDAC1; IC50s = 0.074 and 0.29 μM, respectively).1It is selective for BD2 over BD1 in BRD4 (IC50= 0.72 μM) and for HDAC1 over HDAC2 (IC50= 2.5 μM). TW9 (50 nM) induces apoptosis in, and inhibits proliferation of, MIA PaCa-2 pancreatic cancer cells. It induces cell cycle arrest at the G1phase in HPAC pancreatic cancer cells when used at a concentration of 2 μM. TW9 acts synergistically with gemcitabine to reduce the viability of HPAC cells. 1.Zhang, X., Zegar, T., Weiser, T., et al.Characterization of a dual BET HDAC inhibitor for treatment of pancreatic ductal adenocarcinomaInt. J. Cancer147(10)2847-2861(2020)

Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino cap group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm

L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitorsBioorg. Med. Chem. Lett.24(1)61-64(2014)

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.

9-hydroxy Stearic Acid 是一种羟基脂肪酸，是9-PAHSA 的活性代谢物。9-hydroxy Stearic Acid 是由9-PAHSA 通过肝脏和胰腺的羧基酯脂肪酶形成的。9-hydroxy Stearic Acid (5 μM)抑制HT-29结肠癌细胞裂解物中组蛋白去乙酰化酶1 (HDAC1)的表达。3 .当浓度为100 μM.1时，可抑制HT-29细胞的增殖，并诱导细胞周期阻滞于G0 g1期。

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

Theophylline (1,3-Dimethylxanthine) sodium glycinate 是一种有效的磷酸二酯酶 (PDE) 抑制剂，可抑制 PDE3 活性以松弛气道平滑肌。Theophylline sodium glycinate 可用于研究哮喘和慢性阻塞性肺疾病 (COPD) 。Theophylline sodium glycinate 也是一种腺苷受体拮抗剂和组蛋白脱乙酰酶 (HDAC) 激活剂。 Theophylline sodium glycinate 通过增加 IL-10 和抑制 NF-κB 的核输入而具有抗炎活性。Theophyllin sodium glycinate 可诱导细胞凋亡。

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].

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 greatly reduces egg laying in adult worm pairs [1].

FNDR-20123 free base 是一种有效、安全、首创的抗疟疾HDAC 抑制剂，对疟原虫和人类 HDAC 的IC50分别为 31 nM 和 3 nM。FNDR-20123 free base 对恶性疟原虫 (Plasmodium falciparum) 无性期 (IC50=41 nM) 和性血期 (雄性配子体 IC50=190 nM) 具有抗疟疾活性。FNDR-20123 free base 抑制 HDAC1，HDAC2，HDAC3，HDAC6，HDAC8 的 IC50分别为 25，29，2，11，282 nM，并在纳摩尔浓度下抑制 III 类 HDAC 亚型。

HDAC-IN-42 (compound 14f) is a highly potent and selective inhibitor of histone deacetylase (HDAC) enzymes, with IC50 values of 0.19 μM for HDAC1 and 4.98 μM for HDAC6. It exhibits remarkable anticancer properties and inhibits cell proliferation. Additionally, HDAC-IN-42 induces apoptosis and causes cell cycle arrest specifically at the G2 M phase [1].

mTOR HDAC6-IN-1 是一种有效的组蛋白去乙酰酶 (HDAC6)和哺乳动物雷帕霉素 (mTOR) 的双重抑制剂，对于HDAC6 和 mTOR 的IC50值分别为56 nM 和133.7 nM。mTOR HDAC6-IN-1 对细胞自噬 (autophagy)、细胞凋亡 (apoptosis)具有明显的诱导作用，对迁移具有抑制作用。mTOR HDAC6-IN-1 在三阴性乳腺癌 (TNBC) 的研究中具有潜力

Splitomicin (1-Naphthalenepropanoic Acid) 是 NAD(+) 依赖性组蛋白去乙酰化酶 Sir2p 的特异性抑制剂，可抑制酵母提取物中 HDAC，IC50为 60 μM。

OKI-006 是一种有效的、具有口服活性的组蛋白脱乙酰酶 (HDAC) 抑制剂。OKI-006 是天然产物HDAC 抑制剂 largazole 的独特同系物。组蛋白去乙酰化酶 (HDAC) 在表观基因组调控中起关键作用，并且组蛋白乙酰化在许多人类癌症中失调。OKI-006 具有研究癌症疾病的潜力。