hd1-a

Givinostat hydrochloride monohydrate (ITF2357) 是一种HDAC 抑制剂，对HDAC1和HDAC3的IC50分别为 198 nM 和 157 nM。

Givinostat hydrochloride (ITF2357 hydrochloride) 是一种 HDAC 抑制剂，对 HDAC1 和 HDAC3 的 IC50 分别为 198 和 157 nM。 Givinostat hydrochloride 具有抗炎、抗血管生成和抗肿瘤活性。

μ-TRTX-Hd1a为特异性NaV 1.7抑制剂，源自蜘蛛毒液。该化合物作为门控修饰剂，通过与人NaV 1.7通道域II中S3b-S4桨基序互作，实现抑制功能。

MC1568是一种针对玉米 HD1-A 的特异性 HDAC 抑制剂，在无细胞试验中的IC50为100 nM，可用于癌症研究。

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.

11β-HSD1-IN-11 是一种有效的、具有竞争性的 11- β-羟基类固醇脱氢酶1 (11β-HSD1)抑制剂，对大鼠和人的 11β-HSD1具有抑制作用，IC50 分别为 0.34 μM 和 0.13 μM。11β-HSD1- in -11是一种作为的化合物。11β-HSD1-IN-11是一种参与调节各种生理过程的激素，例如代谢、炎症和应激反应。11β-HSD1-IN-11是治疗代谢紊乱、肥胖和某些炎症状况的潜在化合物。

GR 103691 是选择性的多巴胺 D3受体拮抗剂，Ki=0.4 nM。它对人多巴胺 D3的选择性超过 D4和 D1的 100 倍以上。

PRO-HD1，一种PROTAC HDAC6降解剂（IC50：5.8 μM），能够在A549细胞中降解HDAC6并在Jurkat细胞中抑制增殖（IC50：5.8 μM）。