itf

ITF3756 是一种选择性 HDAC6 抑制剂。

ITF5924 (compound 1) 是一种高效且极具选择性的HDAC6抑制剂，IC50为7.7 nM，对其他HDAC亚型的选择性超过104倍。ITF5924 含有二氟甲基-1,3,4-恶二唑 (DFMO) 结构，作为HDAC6缓慢结合的底物类似物，通过酶催化开环反应形成紧密且持久的酶抑制剂复合物。

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。

AZD3229 Tosylate is a highly potent inhibitor targeting mutant forms of the pan-KIT enzyme, with a primary application in the treatment of gastrointestinal stromal tumors (GISTs).

Sinitrodil (ITF-296) 是一种鸟苷酸环化酶兴奋剂，可用于治疗心肌缺血和心绞痛。

Icrocaptide is used potentially for the treatment of acute myocardial infarction.

Imidazole Salicylate, a non-steroidal anti-inflammatory drug, has limited inhibitory effects on prostaglandin synthesis.

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.

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。

FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.

Dihydrocitflavanone 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T124352。

Adhesamine diTFA, 一种哑铃状的分子，主要激活MAPK FAK通路。该化合物不仅促进哺乳动物细胞的粘附与生长，还能加快原代培养小鼠海马神经元的分化，并显著提升其存活率。

NOX2-IN-2 diTFA (compound 33) 作为靶向 p47phox-p22phox 蛋白之间相互作用的有效NOX2抑制剂，显示出 0.24 μM 的Ki值。同时，它还能抑制细胞内由NOX2产生的 ROS。

Protease-Activated Receptor-4 diTFA 是蛋白酶激活受体 4 (PAR4) 激动剂。

BSJ-03-204 triTFA是一种融合了Cereblon配体和CDK配体的PROTAC，作为基于Palbociclib的、高效的CDK4 6双重降解剂，选择性地对CDK4 D1和CDK6 D1表现出26.9 nM和10.4 nM的IC50值。它不会引发IKZF1 3的降解，展现了潜在的抗癌活性。

Apelin-13 triTFA(217082-58-1(free base)) 是 APJ 受体的内源性配体，可激活该 G 蛋白偶联受体，EC50 值为 0.37 nM。

PROTACEGFRdegrader 7 diTFA (compound 13b) 是高效且选择性的 CRBN 招募 PROTACEGFRL858R T790M 降解剂，DC50 值为 13.2 nM。它在抑制 NCI-H1975 细胞增殖方面表现出强效，IC50 值为 46.82 nM，并且能够显着诱导这些细胞发生凋亡以及 G2 M 期的阻滞。PROTACEGFRdegrader 7 diTFA 展现了潜在的抗肿瘤活性，适合应用于非小细胞肺癌 (NSCLC) 的相关研究。

Lanreotide (BIM 23014) diTFA是一种生长抑素类似物，具抗肿瘤活性，适用于类癌综合症研究。

BIBO3304 (diTFA) 是口服有效、选择性的神经肽Y(NPY)Y1受体高效拮抗剂。对人类及大鼠Y1受体具高亲和力，IC50值分别为0.38和0.72 nM。BIBO3304 (diTFA) 通过Wnt/β-catenin信号通路促进骨肌腱愈合。

CITFA为一种GPER激动剂，能够促进E18大鼠胚胎海马神经元的神经突生长。

iBRD4-BD1 diTFA 是一种选择性 BRD4 溴结构域抑制剂，具有抑制活性，IC50值为 12 nM。iBRD4-BD1 diTFA 可用于炎症和肿瘤学研究。

Philanthotoxin 74 (PhTx 74) diTFA 作为AMPAR的拮抗剂，对GluR3和GluR1的抑制效果显著，其IC50值分别约为263 nM和296 nM。

STING agonist-18 diTFA (compound 1a) 是用于合成抗体活性分子偶联物 (ADCs) 的关键成分,例如用于Trastuzumab 偶联物的生产.

Nemifitide diTFA (INN 00835 diTFA) 是一种合成的五肽，是一种可透过血脑屏障的黑色素细胞抑制因子 (MIF) 的肽类似物，具有有效的抗抑郁活性。