hd2

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。

PRO-HD2为针对HDAC6的细胞特异性PROTAC降解剂。

JHD205为CDK4 6抑制剂类化合物。

PHD2-IN-4 (compound 1) 是一种PHD2抑制剂，其对PHD2的抑制IC50为4 nM，可用于慢性肾病研究。

PHD2 HDACs-IN-1 是一种有效的 PHD2 HDACs 混合抑制剂，能够作用于 PHD2 (IC50: 1.15 μM)、HDAC1 (IC50: 19.75 μM)、HDAC2 (IC50: 26.60 μM)、HDAC16 (IC50: 15.98 μM)。PHD2 HDACs-IN-1 是一种低毒性肾保护剂，能够用于顺铂诱导的急性肾损伤 (AKI) 的研究。

PHD2-IN-1 为一种口服活性强效 HIF-脯氨酰羟化酶2 (PHD2) 抑制剂，具有 22.53 nM 的 IC50 值，适用于贫血病研究。

PhD2是一种源自猴血白细胞的抗菌肽，对细菌与(真菌)Candida albicans显示出抗生活性。

IOX2 (IOX 2) 是特异性的脯氨酰羟化酶-2 抑制剂，IC50=22 nM。

Molidustat (BAY 85-3934) 是新型HIF-PH 抑制剂，对PHD1(IC50:480 nM)、PHD2(IC50:280 nM)、PHD3(IC50:450 nM)。

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.

Adaptaquin 是缺氧诱导因子脯氨酰羟化酶（HIF-PH）的抑制剂。

FG-2216 (YM-311) 是一种有效的、口服具有活力的HIF 脯氨酰羟化酶-2 (PHD2) 抑制剂，IC50=3.9 nM。它在体内能够诱导促红细胞生成素生成和胎儿血红蛋白的表达。

JNJ-42041935 (HIF-PHD Inhibitor II) 是一种高效的，竞争性的、选择性的脯氨酰羟化酶PHD 抑制剂，抑制PHD1(pKi= 7.91±0.04)，PHD2 (pKi= 7.29 ±0.05) 和 PHD3 (pKi= 7.65±0.09)。

HIF-PHD-IN-1 is a pharmacological compound that acts as an orally active inhibitor of the hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), displaying an IC50 of 54 nM for hHIF-PHD2. Its potential as a therapeutic agent for renal anemia is highly promising.

MK-8617 是一种口服具有活力的低氧诱导因子脯氨酰羟化酶 1-3 (HIF PHD1-3) 泛抑制剂，对于PHD2的IC50=1 nM。

TP0463518 是缺氧诱导因子脯氨酰羟化酶抑制剂，能够作用于人 PHD2(Ki= 5.3 nM)。它还抑制人PHD1 PHD3，IC50分别为 18 和 63 nM，以及猴 PHD2(IC50=22 nM)。

tert-butyl 4-[[1-[(4-chlorophenyl)methyl]-3-hydroxy-2-oxopyridin-4-yl]methyl]piperazine-1-carboxylate 是一种脯氨酰羟化酶抑制剂。

H-D-2-Pal-OH 是一种氨基酸衍生物，在生命科学相关研究中具有广泛的应用。

IOX4 是选择性 PHD2抑制剂，IC50=1.6 nM，在细胞和野生型小鼠中诱导 HIFα表达，可透过血脑屏障。它与 PHD2 特性位点的 2-氧代戊二酸竞争并置换。

HA-2a通过降低RAW264.7细胞内circDcbld2的表达，从而抑制JAK2 STAT3信号传导途径。

FHD-286 是 BRM BRG1 ATPase 的抑制剂，可用于治疗 BAF 相关疾病如急性髓性白血病的研究。

Adoprazine (SLV313) 是 5-HT 1A 受体的完全激动剂，其在 h5-HT1A 受体的 pEC50 为 9。Adoprazine 是 D2 和 D3 受体的完全拮抗剂，在 hD2 受体中的 pA2 值是 9.3，在 hD3 受体中的 pA2 值是 8.9。Adoprazine 具有非典型抗精神病的特征。

Ropinirole hydrochloride (SKF-101468A) 是D3 D2受体激动剂，对 D2受体的Ki=29 nM。它对 hD2，hD3和 hD4受体的pEC50分别为 7.4、8.4 和 6.8。它对 D1受体没有亲和力。它对帕金森氏病具有潜在的研究价值。