homology-2

Tetramethylcurcumin 是一种新型姜黄素类似物，是一种有效的 STAT3 磷酸化、DNA 结合活性和体外反式激活抑制剂。它具有抗炎和抗癌作用。

2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) 是一种PTP1B 的有效抑制剂，其Ki=42 μM。

PTP inhibitor 1 是蛋白酪氨酸磷酸酶 (PTP) 抑制剂，具有抗血管生成作用。

SMIFH2 是formin 特异性抑制剂。它利用 Formins 阻碍肌动蛋白聚合，影响肌动蛋白细胞骨架。

NSC117079是一种新型的的PHLPP1 2（Pleckstrin homology domain and leucine rich repeat protein phosphatase）抑制剂，在神经元中能够激活神经元AKT并改善staurosporine诱导的细胞死亡。

TNO155 是具有口服活性野生型SHP2的选择性变构抑制剂 (IC50= 0.011 µM)。它有研究 RTK 依赖性恶性肿瘤（尤其是晚期实体瘤）的潜力。

Bragsin2 (6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one) 是非竞争性的核苷酸交换因子 BRAG2选择性抑制剂，其 IC50值为 3 μM。它能够结合到 BRAG2 的 PH 结构域和磷脂双分子层的界面处，使 BRAG2 无法激活磷脂化的 Arf GTPase。它能够影响乳腺癌干细胞。

YTHDF2-IN-1 (Compound CK-75) 是一种 YT521-B 同源域家族 2 (YTHDF2) 的抑制剂，其 Kd 值为 26.2 μM，能够阻止 YTHDF2 与 m6A RNA 的作用。YTHDF2-IN-1 可阻碍 JAR 细胞的集落形成，并在多种癌细胞中展现出抗增殖活性（IC50 为微摩尔）。此外，它在 G0 G1 期阻滞细胞周期，并诱导 K562 细胞发生凋亡 (apoptosis)。

CHS-111 is a benzyl indazole compound. CHS-111 inhibits superoxide anion (O(2)(-)) generation. CHS-111 reduces the fMLP-stimulated PLD activity (IC(50) 3.9±1.2μM). CHS-111 inhibits the interaction of PLD1 with ADP-ribosylation factor (Arf) 6 and Ras homol

1-O-Octadecyl-2-O-methyl-sn-glycerol is a metabolite of a phosphotidylinositol ether lipid analog (PIA). PIAs are known to target the pleckstrin homology domain of the serine threonine kinase Akt and to induce apoptosis in cancer cell lines with high levels of endogenous Akt activity.

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).

The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking. PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) is a synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacylglycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this analog give it different physical properties from naturally-occurring PIP3, including higher solubility in aqueous media.

EPQpYEEIPIYL, a phosphopeptide, is a ligand for the Src homology 2 (SH2) domain. It activates members of the Src family, such as Lck, Hck, and Fyn, through the binding interaction with SH2 domains.

Migoprotafib(GDC-1971)是一种有效的、高选择性的SHP2(Src Homology-2 Domain-Containing Phosphatase 2)抑制剂，用于研究晚期实体瘤。

Beinaglutide 是一种重组人 GLP-1(rhGLP-1) 多肽，与人 GLP-1(7-36) 具有几乎 100% 的同源性。Beinaglutide 在血糖控制、抑制食物摄入和胃排空和促进体重减轻方面表现出依赖于剂量的作用。Beinaglutide 具有研究超重 肥胖和非酒精性脂肪性肝炎 (NASH) 的潜力。

Neuropeptide Y (2-36) (porcine) 是一种具有 97.14% 与大鼠 人类同源性的猪源性神经肽。作为一种大鼠神经肽受体激动剂，其对Y5、Y2和Y1受体的EC50值为1.2, 1.6 和 3.4 nM，能显著增加食物摄入量，适用于肥胖和饮食失调研究。

STAT6-IN-3 (Compound 18a)，一种针对STAT6的Src同源2 (SH2) 结构域的抑制剂，具有44 nM的IC50值。该化合物主要适用于研究哮喘等炎症性疾病。