homology

NVP-BSK805 (BSK 805) 是 ATP 竞争性的 JAK2抑制剂，对 JAK1 JH1、 JAK2 JH1 (JAK 同源 1)、JAK3 JH1和 TYK2 JH1 的 IC50值分别为 31.63、0.48、8.68 和 10.76 nM。

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。

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。

NSC45586 是一种蛋白磷酸酶 PHLPP 抑制剂，对 PHLPP1 和 PHLPP2 具有选择性。

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。

Fibronectin CS1 Peptide acetate 存在于 III 型同源连接段 (IIICS) 以及 C-274（细胞结合结构域）中。 Fibronectin CS1 Peptide 缺乏含有 Arg-Gly-Asp 的结构域，在自发和实验性转移模型中积极抑制肿瘤转移。

FPA-124是一种细胞可渗透的铜配合物，作为选择性Akt（蛋白激酶B）抑制剂与Akt的同源结构域（PH）和激酶结构域相互作用，诱导细胞凋亡。具有高效的优点，在多种癌细胞系表现出剂量依赖性的生长抑制作用。

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。

PHT-7.3 is a selective connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain inhibitor

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。

SCR7 pyrazine (SCR7) 是一种 DNA 连接酶 IV 抑制剂，以连接酶 IV 依赖的方式阻断非同源末端连接。它也是 CRISPR/Cas9的增强子，可提高 Cas9 介导的同源性定向修复的效率。它诱导细胞凋亡，具有抗癌活性。

YL-5092是一种YTHDC1抑制剂（IC50=7.4 nM，KD=29.6 nM），能够抑制癌细胞增殖，诱导细胞G0/G1期阻滞和凋亡，可用于研究急性髓系白血病 (AML)。

SJ1008066作为MAGE-A11抑制剂，其IC50值为0.13 μM。该化合物通过与MAGE 同源结构域 (MHD)结合，进而干扰MAGE-A11:PCF11之间的相互作用。

AKT-IN-26 (Compound 453) 是一种能结合AKT Pleckstrin同源结构域 (PH) 的AKT抑制剂，可用于研究AKT通路在细胞增殖及癌症中的作用。

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)。

SHP2-IN-28 (Compound 7188-0011) 是Src同源 2- 含蛋白酪氨酸磷酸酶 2 (SHP2) 的抑制剂，IC50为54.31 μM。其通过结合SHP2的变构位点来发挥抑制作用，并且展现出较高的选择性。

SHP2-IN-42 是一种Src同源 2 结构域磷酸酶 2 (SHP2) 的抑制剂，IC50为15 nM。SHP2-IN-42 能抑制细胞增殖，诱导细胞凋亡 (apoptosis) 和 G1 期周期停滞。SHP2-IN-42 适用于癌症研究，包括急性髓系白血病 (AML)。

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.

PtdIns-(3,4,5)-P3 (PIP3) serves as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH) domains such as phosphatidylinositol 3-kinase (PI3K) or PTEN. Protein binding to PIP3 is important for cytoskeletal rearrangement and membrane trafficking and initiates an intricate signaling cascade that has been implicated in cancer. 3,5-dimethyl PIT-1 is a dimethyl analog of PIT-1, the selective inhibitor of PIP3/Akt PH domain binding, that is designed for more favorable solubility in vivo. 3,5-dimethyl PIT-1 inhibits PI3K/Akt signaling (IC50 = 27 μM), suppressing PI3K-PDK1-Akt-dependent phosphorylation, which has been shown to reduce cell viability and induce apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 36 μM). 4T1 breast cancer growth is significantly attenuated in BALB/c mice with a dose of 1 mg/kg of 3,5-dimethyl PIT-1 per day.

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.