pp2a inhibitor

Endothall 是蛋白磷酸酶 2A (PP2A) 抑制剂，能够抑制PP2A (IC50: 90 nM) 和 PP1 (IC50: 5 uM) 。它可作为除草剂，在癌症化疗过程中也能够发挥作用。

MKI-1 (MASTL Kinase Inhibitor-1) 是微管相关丝氨酸 苏氨酸样激酶 (MASTL) 抑制剂 (IC50= 9.9 μM)。MKI-1 通过激活乳腺癌中的PP2A 发挥放射增敏和抗肿瘤活性。

Calyculin A ((-)-Calyculin A) 是日本海洋海绵 CDiscodermia calyxC 中的毒性物质，是一种具有选择性和高效性的蛋白磷酸酶 1 (PP1) 和蛋白磷酸酶 2A (PP2A) 抑制剂， 诱导冷冻保存牛精子的过度激活，抑制人淋巴细胞中辐射诱导的 gammaH2AX DNA 修复病灶的消失。

D-erythro-Sphingosine (trans-4-Sphingenine) 是一种非常有效的p32激酶活化剂，EC50为 8 μM。它也是一种PP2A 激活剂，抑制蛋白激酶 C (PKC)。

(Rac)-LB-100 是-LB-100 的外消旋体。LB-100 是一种新型蛋白磷酸酶 2A (PP2A) 抑制剂，可使恶性脑膜瘤细胞对放射治疗效果敏感。

LB100 (LB-100) 是一种水溶性蛋白磷酸酶 2A(PP2A) 抑制剂。

Ethoxysanguinarine (6-Ethoxydihydrosanguinarine) 是存在于龙葵中的一种苯并菲啶生物碱天然产物，通过抑制蛋白磷酸酶 2A，可抑制结直肠癌细胞活力，诱导细胞凋亡。

MP07-66 是 FTY720 的一种类似物，没有免疫抑制作用。MP07-66通过破坏 SET-PP2A 复合物导致PP2A 重新激活。MP07-66在慢性淋巴细胞白血病中显示出良好的抗肿瘤作用。

TAT-PDHPS1是一种针对Yes-associated protein (YAP) 信号的肽抑制剂。它由内源性肽PDHPS1和能穿透细胞的肽序列TAT组成。PDHPS1与蛋白磷酸酶2磷酸酶激活因子(PTPA)结合, 激活蛋白磷酸酶2A (PP2A)。该激活促进YAP的磷酸化和抑制YAP靶向基因的表达。TAT-PDHPS1能够抑制体外卵巢癌细胞的增殖和小鼠皮下异种移植肿瘤模型中的卵巢肿瘤生长。

AMZ30是磷酸酯酶PME-1高效抑制剂(IC50:600nM)。它可减少活细胞中 PP2A 的去甲基化形式。

Rubratoxin A is a classical mycotoxin used as a PP2A-specific inhibitor.

Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

Tautomycin is a potent and specific protein phosphatases 1 and 2A inhibitor (Kiapp of 0.16 nM and 0.4 nM for PP1 and PP2A, respectively), and is an antifungal antibiotic isolated from the bacterium Streptomyces verticillatus.

N-Stearoylsphingosine (Cer(d18:1 18:0)) 是一种广泛存在真核生物体内的酰胺类化合物，通过干扰PP2A与PP2A抑制剂2的结合来增强蛋白质磷酸酶2A(PP2A)活性，导致Akt去磷酸化。N-Stearoylsphingosine 可用于研究前列腺癌。

Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 μM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).

Cytostatin (sodium salt) is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin (sodium salt) potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

TD52 是 PP2A (CIP2A) 癌性抑制剂的口服活性抑制剂。 TD52 是厄洛替尼衍生物，通过干扰 Elk1 与 CIP2A 启动子的结合间接降低了 CIP2A。

Microcystin YR (Cyanoginosin YR) 是一种环肽，具有抑制蛋白磷酸酶 2A (PP2A) 的作用。

The cyanobacterium Nodularia spumigena often contaminates the drinking water of rural communities in developing countries and accumulates in mussels, flounder, and cod from the northern Baltic Sea. Nodularin is a hepatotoxic monocylic pentapeptide produced by the N. spumigena. It is a potent inhibitor of protein phosphatase types 1 (PP1) and 2A (PP2A), exhibiting IC50 values of 1.8 and 0.026 nM, respectively. PP2B is inhibited to a lesser extent with an IC50 of 1.8 μM. No apparent inhibitory effect is observed with PP2C, alkaline phosphatase, acid phosphatase, insulin receptor tyrosine kinase, protein kinase A, phosphorylase kinase, or protein kinase C.

TD52 dihydrochloride(TD52 2HCl)，一种Erlotinib的衍生物，是一种强效且口服活性的蛋白磷酸酶2A(CIP2A)的抑制剂，通过调节CIP2A PP2A p-Akt信号通路，展现出强大的抗癌特性，导致三阴性乳腺癌(TNBC)细胞的凋亡。机制上，TD52 dihydrochloride 干扰Elk1与CIP2A启动子的结合，有效降低CIP2A水平。值得注意的是，TD52 dihydrochloride 在展示强大的抗癌活性的同时，对p-EGFR的抑制作用较小。

Fostriecin (free base) is an inhibitor of the serine threonine protein phosphatases 2A (PP2A) and 4 (PP4) (IC50s = 3.2 and 3 nM, respectively). It less effectively inhibits topoisomerase II and PP1 (IC50s = 40 and 131 μM, respectively) and does not inhibit PP2B. Through its effects on protein phosphatases, fostriecin increases the level of histone H3 phosphorylation and may alter epigenetic regulation of cell proliferation. On a related note, fostriecin was first identified as an antitumor antibiotic.

PP2A Cancerous-IN-1 是强效的 CIP2A(Cancerous inhibitor of PP2A) 和 p-Akt 抑制剂，表现出强大的抗增殖作用。

Okadaic acid ammonium salt, a marine toxin, serves as an inhibitor of protein phosphatases (PP), displaying a higher affinity for PP2A (IC 50 =0.1-0.3 nM) alongside inhibitory effects on PP1 (IC 50 =15-50 nM), PP3 (IC 50 =3.7-4 nM), PP4 (IC 50 =0.1 nM), and PP5 (IC 50 =3.5 nM), but does not affect PP2C. By inhibiting PPs, this compound promotes protein phosphorylation and acts as a tumor promoter. Additionally, it is involved in inducing tau phosphorylation.

Okadaic acid 是一种强效的聚醚海洋毒素，在海洋软体动物的消化腺中积聚。Okadaic acid 是一种具有高效性和选择性的蛋白质磷酸酶 (PP) 抑制剂，抑制 PP1、PP2A 、PP3 、PP4 和 PP5 。Okadaic acid 激活人 HepaRG 细胞中的 Wnt β-catenin 信号传导。