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Search Results for " pp2a "

30

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2747	Endothall	Others	Others
	Endothall 是一种有效的蛋白磷酸酶 2A (PP2A) 抑制剂，对 PP2A 和 PP1 具有抑制作用， IC50 分别为 90 nM 和 5 µM。Endothall 具有抗癌活性，可用于癌症化疗，可用作除草剂。
T63259	PP2A Cancerous-IN-1
	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。
T9744	MP07-66	Phosphatase	Metabolism
	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。
T35528	TD52	Apoptosis; Phosphatase; Akt	Apoptosis; Cytoskeletal Signaling; Metabolism; PI3K/Akt/mTOR signaling
	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。
T70131	TPP2a bromide
	TPP2a is a mitochondrial thioredoxin reductase (TrxR) inhibitor.
T4449	LB100 LB-100,LB 100	Phosphatase	Metabolism
	LB100 (LB-100) 是一种水溶性蛋白磷酸酶 2A(PP2A) 抑制剂。
T5182	AMZ30	Others	Others
	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。
T2068	(Rac)-LB-100	Phosphatase	Metabolism
	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。
T3635	IQ 1 IQ1,IQ-1	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	IQ 1 有多种作用，如保持小鼠ESCs 的多功能性、降低Wnt 刺激的磷酸化、阻止PP2A/Nkd 的相互作用等等。
T60688	MKI-1 MASTL Kinase Inhibitor-1	Others	Others
	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。
T35528L	TD52 dihydrochloride TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl	Others	Others
	TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti...
T14859	Calyculin A (-)-Calyculin A	Others	Others
	Calyculin A is a potent and cell-permeable inhibitor of protein phosphatase 1 (PP1; IC50s: 2 nM). It also is a protein phosphatase 2A (PP2A) inhibitor (IC50s: 0.5-1 nM).
T13095	Tautomycin	Others	Others
	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.
T12934	SMAP-2 DT-1154	Phosphatase	Metabolism
	SMAP-2 is an orally bioavailable activator of phosphatase 2A (PP2A) which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. It inhibits the growth of KRAS-mutant lung cancers .
T26164	Rubratoxin A
	Rubratoxin A is a classical mycotoxin used as a PP2A-specific inhibitor.
T78681	ITH12711	Phosphatase	Metabolism
	ITH12711为PP2A配体，具有穿透血脑屏障（BBB）的能力，其神经保护机制是通过恢复PP2A磷酸酶活性来实现。
T35806	N-Stearoylsphingosine C(18:0)/C(18:1),Cer(d18:1/18:0),C18 Ceramide (d18:1/18:0),C18 Ceramide	Phosphatase	Metabolism
	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。
T31882	FTY720-Mitoxy FTY 720 Mitoxy,FTY-720-Mitoxy
	FTY720-Mitoxy is an FTY720 analog that can be uesd as a novel stimulator of the activity of the protein phosphatase 2A (PP2A), targeting mitochondria.
T10060	(1S,2S,3R)-DT-061	Others	Others
	(1S,2S,3R)-DT-061 is an enantiomer of DT-061 which is an orally bioavailable activator of PP2A.
T83530	LB-100
	(Rac)-LB-100为LB-100的外消旋体，系一种蛋白磷酸酶2A（PP2A）抑制剂。
T10060L	DT-061	Phosphatase	Metabolism
	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.
T39239	TRC-766
	TRC-766, a negative control of RTC-5 (TRC-382), is a compound that exhibits protein phosphatase 2A (PP2A) binding properties while lacking phosphatase activation capabilities.
TP2054	Calcineurin Autoinhibitory Peptide
	Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 μM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM).
TP1698	Microcystin-LA
	Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
T82938	ATUX-1215
	ATUX-1215是一种蛋白磷酸酶 2A (PP2A)的激活剂，能够在BLM治疗的动物模型中降低ERK、p38、JNK和Akt的磷酸化及IL-12p70、GM-CSF与IL1α的分泌，从而有助于减缓肺纤维化的发展。
T39183	Okadaic acid ammonium salt
	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.
T68458	Fostriecin (free base)
	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 antib...
T35777	Nodularin
	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 eff...
T83938	TAT-PDHPS1
	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。
T35613	Cytostatin (sodium salt)
	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.

化合物

Cat.No: T2747

Target: Others

PP2A Cancerous-IN-1

Cat.No: T63259

Cat.No: T9744

Target: Phosphatase

Cat.No: T35528

Target: Apoptosis, Phosphatase, Akt

Cat.No: T70131

Cat.No: T4449

Synonym: LB-100,LB 100

Target: Phosphatase

Cat.No: T5182

Target: Others

Cat.No: T2068

Target: Phosphatase

Cat.No: T3635

Synonym: IQ1,IQ-1

Target: Wnt/beta-catenin

Cat.No: T60688

Synonym: MASTL Kinase Inhibitor-1

Target: Others

TD52 dihydrochloride

Cat.No: T35528L

Synonym: TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl

Target: Others

Cat.No: T14859

Synonym: (-)-Calyculin A

Target: Others

Cat.No: T13095

Target: Others

Cat.No: T12934

Synonym: DT-1154

Target: Phosphatase

Cat.No: T26164

Cat.No: T78681

Target: Phosphatase

N-Stearoylsphingosine

Cat.No: T35806

Synonym: C(18:0)/C(18:1),Cer(d18:1/18:0),C18 Ceramide (d18:1/18:0),C18 Ceramide

Target: Phosphatase

Cat.No: T31882

Synonym: FTY 720 Mitoxy,FTY-720-Mitoxy

(1S,2S,3R)-DT-061

Cat.No: T10060

Target: Others

Cat.No: T83530

Cat.No: T10060L

Target: Phosphatase

Cat.No: T39239

Calcineurin Autoinhibitory Peptide

Cat.No: TP2054

Cat.No: TP1698

Cat.No: T82938

Okadaic acid ammonium salt

Cat.No: T39183

Fostriecin (free base)

Cat.No: T68458

Cat.No: T35777

Cat.No: T83938

Cytostatin (sodium salt)

Cat.No: T35613

Cat. No.	Product Name	Target	Signaling Pathways
TN1305	Ethoxysanguinarine 乙氧基血根碱,6-Ethoxydihydrosanguinarine	Apoptosis; AChR	Apoptosis; Neuroscience
	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。
T5891	D-ERYTHRO-SPHINGOSINE trans-4-Sphingenine,erythro-C18-Sphingosine,Erythrosphingosine,鞘氨醇,D-鞘氨醇	Phosphatase; Endogenous Metabolite; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism
	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)。
TN5174	Trichosanatine	MMP; LDL; p38 MAPK; Lipoxygenase; ROS	Immunology/Inflammation; MAPK; Metabolism; Proteases/Proteasome
	Trichosanatine and squamosamide, as potential candidates as lead compounds for further study in drug development process with the PP2A- α protein. Trichosanatine can alleviate oxidized low-density lipoprotein induced endothelial cells injury via inhibiting the LOX-1/p38 MAPK pathway.
T16381	Okadaic acid	Others	Others
	Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A, and PP3 inhibitor (IC50s: 10-15 nM, 0.5 nM, and 4 nM, respectively). Okadaic acid is extracted from black sponges of the genus Halic
T37055	Cytostatin
	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.

天然产物

Ethoxysanguinarine

Cat.No: TN1305

Synonym: 乙氧基血根碱,6-Ethoxydihydrosanguinarine

Target: Apoptosis, AChR

D-ERYTHRO-SPHINGOSINE

Cat.No: T5891

Synonym: trans-4-Sphingenine,erythro-C18-Sphingosine,Erythrosphingosine,鞘氨醇,D-鞘氨醇

Target: Phosphatase, Endogenous Metabolite, PKC

Cat.No: TN5174

Target: MMP, LDL, p38 MAPK, Lipoxygenase, ROS

Cat.No: T16381

Target: Others

Cat.No: T37055

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