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AS2717638 是一种具有口服生物活性的，选择性的溶血磷脂酸受体5 (LPA5) 的拮抗剂，其对 hLPA4 的 IC50值为38 nM。AS2717638 还能显著改善 PGE2、PGF2α以及 AMPA 诱导的异位疼痛。

VAS2870 是一种NADPH 氧化酶抑制剂。

AS2863619 free base enables the conversion of antigen-specific effector memory T cells into Foxp3+ regulatory T (Treg) cells. It is a potent, orally active CDK8 and CDK19 inhibitor (IC50s: 0.61 nM and 4.28 nM). STAT5 activation enhanced by AS2863619 free base inhibition of CDK8 19, which consequently activates the Foxp3 gene.

AS2521780 is an inhibitor of PKCθ (IC50: 0.48 nM).

TAS2940是一种不可逆的泛ERBB抑制剂，具有更强的脑部渗透能力，用于治疗肺癌脑转移以及含有HER2 EGFR 20号外显子插入和EGFR异常的胶质母细胞性瘤。在HER2 EGFR癌症的颅内异种移植模型中，TAS2940证明可以有效提高小鼠的生存率。目前，TAS29440正处于一期临床试验阶段，旨在确定固态肿瘤的最大耐受剂量。

AS2690168 freebase 是一种口服有效的 RANKL 信号传导抑制剂，能够抑制 RANKL 诱导的 RAW264 细胞的破骨细胞生成，适用于研究病理性骨溶解相关的情况。

AS2690168 hydrochloride 是一种口服活性RANKL信号转导抑制剂，能够抑制 RANKL 诱导的 RAW264 细胞中的破骨细胞生成。AS2690168 适用于病理性骨溶解领域的研究。

AS2553627 is a JAK inhibitor. AS2553627 prevents chronic rejection in rat cardiac allografts.

AS2541019 is a selective Phosphatidylinositol-3-kinase p110δ (PI3Kδ) inhibitor.

JAS239 is a novel carbocyanine dye that binds and competitively inhibits choline kinase (ChoK) intracellularly. JAS239 attenuated choline phosphorylation and viability in a panel of human breast cancer cell lines. Antibody blockade prevented cellular retention of JAS239 indicating direct interaction with ChoKα independent of the choline transporters and catabolic choline pathways. In mice bearing orthotopic MCF7 breast xenografts, optical imaging with JAS239 distinguished tumors overexpressing ChoKα from their empty vector counterparts and delineated tumor margins.

AS2575959 is a novel GPR40 agonist, exhibiting glucose metabolism improvement and synergistic effect with sitagliptin on insulin and incretin secretion.

TAS2R14 agonist-2 (compound 28.1) 作为选择性TAS2R14抑制剂，其EC50为72 nM。

TAS2R14 agonist为一种TAS2R14受体的部分激活分子，其EC50值确定为116.6±23.6 nM。

AS2863619 是一种口服的细胞周期蛋白依赖性激酶 8（CDK8） 和CDK19抑制剂，抑制CDK8 19可增强STAT5的激活，从而激活 Foxp3 基因。它可将抗原特异性效应子 记忆 T 细胞转换为 Foxp3+调节性 T 细胞，以研究各种免疫疾病。

TAS2940 fumarate 是一种具有口服活性的泛ERBB抑制剂，能够不可逆地选择性抑制泛ERBB并可穿透大脑。该化合物对HER2野生型、HER2 V777L和A775_G776insYVMA的IC50值分别是5.6 nM、2.1 nM和1.0 nM。TAS2940 fumarate 主要用于研究存在HER2与EGFR异常的肿瘤。

Pevonedistat (MLN4924) 是一种 NEDD8 活化酶 (NAE) 抑制剂 (IC50=4.7 nM)，具有有效性和选择性。Pevonedistat 可以用于骨髓增生异常综合症 (MDS)的治疗，也具有抗肿瘤活性。

AS252424 是一种有效的、选择性的 PI3Kγ 抑制剂，其 IC50=30±10 nM。

AS-254s 是 absent, small, or homeotic-like 1 protein (ASH1L) 的抑制剂，IC50 为 94 nM (FP 测定)。对于 MLL1 重排的白血病细胞，AS-254s 显示出抗增殖活性，GI50 < 1 μM，并能诱导 MLL1-r 白血病细胞的分化。

MMAF (MonoMethyl auristatin F) 是一种抗有丝分裂剂，通过阻断微管蛋白的聚合来抑制细胞分裂，用作抗肿瘤药物和抗体偶联药物的细胞毒性成分。

TAS-119 (TAS-2104) 是一种可口服且具有选择性和有效性的 Aurora A 抑制剂，IC50为1.0 nM。TAS-119 对 Aurora B 也具有抑制作用，IC50 为 95 nM。TAS-119 对 Aurora A 的亲和力比 Aurora B高。TAS-119 具有有效的抗肿瘤活性和潜在的抗有丝分裂活性。

TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50= 55.8 nM).1It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg kg. 1.Aoyagi, H., Kajiwara, D., Tsunekuni, K., et al.Potential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitisEur. J. Pharmacol.875173030(2020)

AS2444697 是一种口服有效的IRAK-4抑制剂，IC50为 21 nM。它对人和大鼠 IRAK-4 活性具有抑制作用。它通过抗炎作用表现出肾脏保护作用。

Resminostat (4SC-201) 是一种可口服的HDAC1、HDAC3和HDAC6抑制剂，IC50值分别为 42.5、50.1和71.8 nM，具有潜在抗肿瘤活性。

CU-6PM is a new fluorescent RXR agonist. CU-6PMN was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay CU-6PMN enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such as filtration.