tumorigenesis

3-Phenylpropyl isothiocyanate 在抑制N-nitrosomethyl-benzylamine (NMBA) 的肿瘤生成中表现出强大的抑制效果，从而展现出强大的化学预防性质 [1] [2]。

Liensinine Perchlorate 是元莲的成分，可诱导结直肠癌细胞凋亡，具有抗高血压和抗癌活性。

Cyproterone acetate (Cyproterone 17-O-acetate) 是能够抗雄激素(IC50=7.1 nM) 和孕激素合成的类固醇。它与 progesteron 和糖皮质激素受体有亲和力。

EB-3D 是一种选择性胆碱激酶 α 抑制剂，对 ChoKα1 的IC50值为 1 μM。它影响 ChoKα 表达、AMPK 激活、细胞凋亡、内质网应激和脂质代谢，具有抗癌活性。

EN4 (EN4 MYC inhibitor) 是一种靶向 M​​YC 的半胱氨酸 171 (C171) 的共价配体。它抑制 MYC 转录活性，下调 MYC 靶标，并具有抗肿瘤作用。它对 c-MYC 的选择性高于 N-MYC 和 L-MYC。

DT-061 is an orally bioavailable protein phosphatase 2A (PP2A) activator. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.

Broparestrol (E)- 具有抗生育活性，是啮齿动物乳腺肿瘤发生的有效抑制剂。

Retinoic acid (Tretinoin) 是维生素 A 的代谢产物，是一种视黄酸受体 RAR 的天然激动剂，激动 RARα β γ (IC50=14 nM)。Retinoic acid 可以诱导细胞分化、减少细胞增殖和抑制肿瘤发生。

2-Undecanone (Methylnonylketone) 能够抑制 DnaKJE-ClpB 双酮依赖的热灭活细菌萤光素酶重折叠。它对肺肿瘤发生具有抑制作用。

Bardoxolone (CDDO) 是新型核调节因子激活剂。

Copanlisib (BAY 80-6946) 是一种选择性的和 ATP 竞争性的泛 I 类PI3K 抑制剂，具有抗肿瘤活性，对PI3Kα，PI3Kδ，PI3Kβ和PI3Kγ的IC50分别为 0.5 nM、0.7 nM、3.7 nM 和 6.4 nM。

PIM447 (LGH447) 是一种可口服且具有选择性的泛 PIM 激酶抑制剂，具有抗肿瘤和骨保护作用，抑制 PIM1、PIM2 和 PIM3，诱导细胞凋亡，可降低 HuH6 和 COA67 细胞的活力、增殖和运动。PIM447 抑制肝母细胞瘤的肿瘤发生，可用于研究多发性骨髓瘤。

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.

FAK-IN-22 (Compound 26) 是FAK、JAK3和Aurora B的抑制剂，其IC50值分别为50.94 nM、9.99 nM和0.49 nM，有效抑制胰腺导管腺癌 (PDAC) 的肿瘤发生和转移。FAK-IN-22 抑制 PANC-1 细胞的增殖，IC50值为0.15 μM，并通过抑制FAK PI3K Akt信号通路，在 PANC-1 细胞中诱导凋亡和 G2 M 期阻滞。

MTH1 activator-1 是一种MTH1激活剂，能够提升内源性MTH1的活性，同时显著降低细胞DNA中的8-oxo-dG水平。此化合物适用于研究核苷酸池中氧化损伤修复的上调效应，以及用于延迟或减少肿瘤发生的实验。

Ovatodiolide 是从茴香中提取得到的小分子化合物，具有抗炎和潜在的神经保护活性，抑制结肠肿瘤发生，可用于研究神经系统疾病。

ADP-Ribosylarginine can regulate cell proliferation and tumorigenesis.

Ochratoxin A-13C20is intended for use as an internal standard for the quantification of ochratoxin A by GC- or LC-MS. Ochratoxin A is a mycotoxin that has been found inAspergillusandPenicillium.1It increases lipid peroxide levels and the number of apoptotic cells, as well as reduces superoxide dismutase activity in rat kidney when administered at a dose of 120 μg kg.2Topical application of ochratoxin A (80 μg mouse) induces DNA damage, cell cycle arrest at the G0 G1phase, and apoptosis in mouse skin cells.1It also initiates tumor formation in a two-stage mouse skin tumorigenesis model. Ochratoxin A has been found as a contaminant in a variety of foods.3

(S)-GFB-12811 (compound 596) 是一种选择性的、选择性的 CDK5 抑制剂 (IC50<10 nM)。(S)-GFB-12811 能够用于细胞周期进程、神经元发育、肿瘤发生的研究。

NZ28, also known as NSC134754, is potent HSF1 inhibitor, which induced inhibition of HSF1, SP1 and NF-κB triggers the loss of the natural killer cell-activating ligands MICA B on human tumor cells. Heat-shock transcription factor HSF1 has a critical role in human epidermal growth factor receptor-2-induced cellular transformation and tumorigenesis.

LY2780301 is an orally bioavailable inhibitor of the serine threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor LY2780301 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K Akt signaling pathway, thereby leading to inhibition of cell proliferation and the induction of apoptosis in tumor cells. Activation of the PI3K Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

GNE-8525 is a potent and selective pan-TRK inhibitor. GNE-8525 demonstrated potent antiproliferation activity with IC50 = 0.003 μM. In a tumor xenograft model derived from the KM12 cell line, GNE-8525 demonstrated in vivo antitumor efficacy when administered at ascending doses twice daily (bid) for 14 days in rats. Deregulated kinase activities of tropomyosin receptor kinase (TRK) family members have been shown to be associated with tumorigenesis and poor prognosis in a variety of cancer types. In particular, several chromosomal rearrangements involving TRKA have been reported in colorectal, papillary thyroid, glioblastoma, melanoma, and lung tissue that are believed to be the key oncogenic driver in these tumors.

NS-0011 is an inhibitor of CDK5 translocation which increases CDK5 accumulation in the nucleus, suppressing both cancer cell proliferation and xenograft tumorigenesis.

PROTACEZH2 Degrader-1 (Compound 150d)是高效的PROTACEZH2降解剂，能够抑制EZH2甲基转移酶的活性，其IC50值为2.7 nM。由于EZH2在许多肿瘤的发生及进展中具有关键作用，这种化合物的研发具有重要意义。