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20

抑制剂 & 化合物

4

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 PP2APP1 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。
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
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。
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。
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。
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...
T26164 Rubratoxin A

Rubratoxin A is a classical mycotoxin used as a PP2A-specific inhibitor.
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。
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PP2APP2A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。
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.
T83530 LB-100

(Rac)-LB-100为LB-100的外消旋体,系一种蛋白磷酸酶2APP2A)抑制剂。
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).
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...
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.
T35613 Cytostatin (sodium salt)

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 agai...
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。

化合物

Endothall
Cat.No: T2747
Synonym:
Target: Others
MP07-66
Cat.No: T9744
Synonym:
Target: Phosphatase
TD52
Cat.No: T35528
Synonym:
Target: Apoptosis, Phosphatase, Akt
LB100
Cat.No: T4449
Synonym: LB-100,LB 100
Target: Phosphatase
AMZ30
Cat.No: T5182
Synonym:
Target: Others
MKI-1
Cat.No: T60688
Synonym: MASTL Kinase Inhibitor-1
Target: Others
(Rac)-LB-100
Cat.No: T2068
Synonym:
Target: Phosphatase
TD52 dihydrochloride
Cat.No: T35528L
Synonym: TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl
Target: Others
Rubratoxin A
Cat.No: T26164
Synonym:
Target:
PP2A Cancerous-IN-1
Cat.No: T63259
Synonym:
Target:
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
Calyculin A
Cat.No: T14859
Synonym: (-)-Calyculin A
Target: Others
Tautomycin
Cat.No: T13095
Synonym:
Target: Others
LB-100
Cat.No: T83530
Synonym:
Target:
Calcineurin Autoinhibitory Peptide
Cat.No: TP2054
Synonym:
Target:
Fostriecin (free base)
Cat.No: T68458
Synonym:
Target:
Okadaic acid ammonium salt
Cat.No: T39183
Synonym:
Target:
Cytostatin (sodium salt)
Cat.No: T35613
Synonym:
Target:
Nodularin
Cat.No: T35777
Synonym:
Target:
TAT-PDHPS1
Cat.No: T83938
Synonym:
Target:
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)。
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
Okadaic acid
Cat.No: T16381
Synonym:
Target: Others
Cytostatin
Cat.No: T37055
Synonym:
Target:
TargetMol Loading
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