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32

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T18888 4-Methylumbelliferyl phosphate

4-甲基伞形酮磷酸酯,4-MUP

Others Others
4-Methylumbelliferyl phosphate (4-MUP) 是碱性磷酸酶的荧光底物。
T21980 PD 198306

MEK MAPK
PD 198306 是一种具有抗痛觉过敏作用的 MAPK/ERK 激酶 (MEK) 选择性抑制剂。 PD 198306 可降低链脲佐菌素诱导的活性 ERK1 水平升高。
T2160 Suramin Sodium Salt

苏拉明钠,BAY-205,Suramin hexasodium salt,苏拉明钠盐,NF-060

Apoptosis; Phosphatase; SARS-CoV; Sirtuin; Reverse Transcriptase; Topoisomerase; Parasite Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K,是抗寄生虫,抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂,也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。
T9325 2-(2-Aminothiazole-4-yl)-2-methoxyiminoa

Others Others
2-(2-Aminothiazole-4-yl)-2-methoxyiminoa 是一种蛋白质酪氨酸磷酸酶的抑制剂,蛋白质酪氨酸磷酸酶可以导致细胞信号通路的变化,从而影响细胞的行为。
T16554 PNPP

Others Others
PNPP 是用于 ELISA 和常规分光光度测定的碱性和酸性磷酸酶的非蛋白质显色底物。
T34973 Tyrphostin 8

4-Hydroxybenzylidenemalononitrile

EGFR; GTPase Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Tyrosine Kinase/Adaptors
Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) 是一种有效的 GTP 酶抑制剂,对 EGFR 激酶有抑制作用, IC50 值为 560 μM。Tyrphostin 8 可抑制蛋白丝氨酸/苏氨酸钙调磷酸酶 (IC50=21 μM),增强 Caco-2 细胞中转铁蛋白受体介导的转吞作用,并增加口服胰岛素 - 转铁蛋白的降血糖作用。
T16350 NSC-87877

Apoptosis; Phosphatase Apoptosis; Metabolism
NSC-87877 是一种Shp2和Shp1蛋白质酪氨酸磷酸酶抑制剂,IC50值分别为0.318 μM 和0.355 μM。它还抑制双特异性磷酸酶26。
T3045 Salubrinal

Apoptosis; Phosphatase; PERK; Autophagy; HSV Apoptosis; Autophagy; Metabolism; Microbiology/Virology
Salubrinal 是一种磷酸酶抑制剂 ,对真核翻译起始因子 2 亚基 (eIF2α) 发挥作用。它作为双特异性磷酸酶 2 抑制剂,抑制抗胶原蛋白抗体诱导的关节炎。它具有抗HSV-1病毒的活性,并抑制由HSV-1蛋白 ICP34.5 介导的eIF2α的去磷酸化。
T7084 2-Bromo-4'-hydroxyacetophenone

SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide,2-溴-4'-羟基苯乙酮

Phosphatase Metabolism
2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) 是一种PTP1B 的有效抑制剂,其Ki=42 μM。
T23132 Pentamidine dihydrochloride

喷他脒二盐酸盐,MP-601205 dihydrochloride

Phosphatase; Antibacterial; Antibiotic; Parasite; Antifungal Metabolism; Microbiology/Virology
Pentamidine dihydrochloride (MP-601205 dihydrochloride) 是一种抗微生物剂,会干扰 DNA 的生物合成。它是选择性蛋白酪氨酸磷酸酶和再生肝磷酸酶抑制剂。它可用于冈比亚锥虫病,抗锑利什曼病和卡氏肺孢子虫肺炎的研究,有抗肿瘤活性,抗菌活性。
T22276 Bis(maltolato)oxovanadium(IV)

双(麦芽醇)氧钒(IV),BMOV,Bis maltolato oxovanadium,Bis(maltolato)oxovanadium (IV),bis maltolato oxo vanadium,Bis(maltolato)oxovanadium (IV)

Phosphatase; Others Metabolism; Others
Bis(maltolato)oxovanadium(IV) (BMOV) 是一种有效的胰岛素增敏剂,也是一种有效的、竞争性的、可逆的、口服具有活性的光谱蛋白酪氨酸磷酸酶 (PTP) 抑制剂。它抑制HCPTPA,PTP1B,HPTPβ和SHP2的IC50分别为 126 nM,109 nM,26 nM 和 201 nM。
T70523 RK-682

RK-682 is a natural selective inhibitor of protein tyrosine phosphatases (PTPases).
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.
T41370 (Rac)-RK-682

(Rac)-RK-682 是 RK-682 的外消旋体。(Rac)-RK-682 是一种蛋白质酪氨酸磷酸酶 (PTPases) 抑制剂。(Rac)-RK-682 抑制蛋白酪氨酸磷酸酶 1B (PTP-1B)、低分子量蛋白酪氨酸磷酸酶 (LMW-PTP)、细胞分裂周期 25B (CDC-25B),IC50分别为 8.6 μM、12.4 μM 和 0.7 μM。
T40846 3,5-Difluoro-L-tyrosine

3,5-Difluoro-L-tyrosine is a functional and tyrosinase-resistant mimic of tyrosine, commonly utilized for evaluating the substrate specificity of protein tyrosine phosphatases (PTPs).
T20421 Fluorescein diphosphate

Fluorescein diphosphate Tetraammonium salt,FDP

Fluorescein diphosphate is a colorless and nonfluorescent substrate for alkaline phosphatases. The sequential alkaline phosphatase mediated hydrolysis of its two phosphate substituents yielding weakly fluorescent fluorescein monophosphate followed by stro
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...
T40968 MLS-0437605

MLS-0437605 is a potent and selective inhibitor of dual-specificity phosphatase 3 (DUSP3), with an IC50 of 3.7 μM. It exhibits higher selectivity towards DUSP3 in comparison to DUSP22 and other protein tyrosine phosphatases (PTPs).
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.
T35877 MurA-IN-1

MurA-IN-1 (compound 1a) is a PTPRR inhibitor, with IC50 values of 0.23 μM, 0.8 μM, 0.75 μM and 0.09 μM for PTP1B, PTPN5, PTPN7 and PTPRR, respectively[1]. (A family of human MAPK-specific protein tyrosine phosphatases) [1]. Jeyanthy Eswaran, et al. Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases. Biochem J. 2006 May 1;395(3):483-91.
T40216 PTPN22-IN-1

PTPN22-IN-1

PTPN22-IN-1 is a potent PTPN22 inhibitor ( IC 50 =1.4 μM; K i =0.50 μM). PTPN22-IN-1 exhibits >7-10 fold selectivity for PTPN22 over similar phosphatases. PTPN22-IN-1 augments antitumor immune responses. From WO2021007491A1 compound L-1.
T71845 Lockdown

Lockdown is a reversible and non-competitive PPM1F inhibitor. Lockdown is selective for PPM1F, because this compound does not inhibit other protein phosphatases in vitro and does not induce additional phenotypes in PPM1F knockout cells. Lockdown acts in a dose-dependent, allosteric manner with high selectivity for PPM1F
T75366 Naphthol AS-GR phosphate disodium

Naphthol AS-GR phosphate disodium 为酸性及碱性磷酸酶底物,此化合物展现出强烈绿色荧光,广泛应用于组织化学研究中。
T11314 Fosmanogepix

APX001,E1211

Others Others
Fosmanogepix (APX001) is a first-in-class, orally available broad-spectrum antifungal agent. It acts as an N-phosphonooxymethyl prodrug that undergoes rapid and complete metabolism by systemic alkaline phosphatases. This metabolism leads to the formation of the active moiety, APX001A. Fosmanogepix (APX001), with its ability to target the highly conserved Gwt1 fungal enzyme, holds great potential for the development of treatments against invasive fungal infections.
T36367 RK-682 (calcium salt)

Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the...
T75340 4-Methylumbelliferyl phosphate disodium

4-Methylumbelliferyl phosphate disodium (4-MUP) 是一种阴离子有机磷酸酯,作为酸性和碱性磷酸酶(phosphatase)的荧光底物,同时也用作神经毒剂模拟剂。
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.
T76486 Ac-MBP (4-14) Peptide

Ac-MBP (4-14) Peptide 是一种乙酰化的 MBP (4-14) Peptide。MBP (4-14) Peptide 是一种选择性的 (蛋白激酶 C)PKC 底物。Ac-MBP (4-14) Peptide 可用于提取物中的PKC 检测,无需事先纯化便可消除干扰蛋白激酶或磷酸酶。
T68918 Phenytoin-d10

Phenytoin-d10 is intended for use as an internal standard for the quantification of phenytoin by GC- or LC-MS. Phenytoin is an anticonvulsant agent and active metabolite of fosphenytoin. Phenytoin is formed from fosphenytoin by tissue phosphatases. It inhibits neuronal voltage-gated sodium channels in a voltage-dependent manner. Phenytoin reduces the neuronal firing frequency and decreases the amplitude of excitatory post-synaptic potentials (EPSPs) in electrically stimulated rat corticostriatal...
T75303 Suramin

Suramin为一种可逆的,竞争性PTPases抑制剂,有效抑制sirtuins:SirT1(IC50=297 nM),SirT2(IC50=1.15 μM),SirT5(IC50=22 μM)。同时,Suramin作为DNAtopoisomeraseII(IC50=5 μM)的竞争性逆转录酶抑制剂,以及SARS-CoV-2 RdRp有效抑制剂。此外,Suramin还能有效抑制IP5K,具有抗寄生虫、抗肿瘤及抗血管生成的作用。
T81548 PAP-IN-1

PAP-IN-1(化合物28)为紫色酸性磷酸酶(PAP)的抑制剂,后者是一种普遍存在的双核金属水解酶。该抑制剂对哺乳动物PAP显示出较强的抑制活性,具有Ki值为168 nM;对猪PAP的抑制活性亦显著,具有Kic值为0.17 μM。此类PAP抑制剂主要用于抗骨质疏松药物研究。
T63405 NAZ2329

NAZ2329 是受体型蛋白质酪氨酸磷酸酶 (RPTPs) R5 亚家族的一个细胞可渗透抑制剂,与其他 PTPs 相比,其变构且能够优先抑制 PTPRZ (hPTPRZ1 的IC50= 7.5 μM) 和PTPRG (hPTPRGIC50= 4.8 μM)。NAZ2329 能够与PTPRZ 的 D1结构域结合,与PTPRZ 整个 (D1 + D2) 片段相比,其能够更有效地抑制 PTPRZ1-D1片段 (IC50: 1.1 μM)。NAZ2329 能够抑制胶质母细胞瘤细胞的肿瘤生长,并表现出抑制干细胞样特性。

化合物

4-Methylumbelliferyl phosphate
Cat.No: T18888
Synonym: 4-甲基伞形酮磷酸酯,4-MUP
Target: Others
PD 198306
Cat.No: T21980
Synonym:
Target: MEK
Suramin Sodium Salt
Cat.No: T2160
Synonym: 苏拉明钠,BAY-205,Suramin hexasodium salt,苏拉明钠盐,NF-060
Target: Apoptosis, Phosphatase, SARS-CoV, Sirtuin, Reverse Transcriptase, Topoisomerase, Parasite
2-(2-Aminothiazole-4-yl)-2-methoxyiminoa
Cat.No: T9325
Synonym:
Target: Others
PNPP
Cat.No: T16554
Synonym:
Target: Others
Tyrphostin 8
Cat.No: T34973
Synonym: 4-Hydroxybenzylidenemalononitrile
Target: EGFR, GTPase
NSC-87877
Cat.No: T16350
Synonym:
Target: Apoptosis, Phosphatase
Salubrinal
Cat.No: T3045
Synonym:
Target: Apoptosis, Phosphatase, PERK, Autophagy, HSV
2-Bromo-4'-hydroxyacetophenone
Cat.No: T7084
Synonym: SHP-1 Inhibitor II,PTP Inhibitor I,α-Bromo-4-hydroxyacetophenone,4-Hydroxyphenacyl bromide,2-溴-4'-羟基苯乙酮
Target: Phosphatase
Pentamidine dihydrochloride
Cat.No: T23132
Synonym: 喷他脒二盐酸盐,MP-601205 dihydrochloride
Target: Phosphatase, Antibacterial, Antibiotic, Parasite, Antifungal
Bis(maltolato)oxovanadium(IV)
Cat.No: T22276
Synonym: 双(麦芽醇)氧钒(IV),BMOV,Bis maltolato oxovanadium,Bis(maltolato)oxovanadium (IV),bis maltolato oxo vanadium,Bis(maltolato)oxovanadium (IV)
Target: Phosphatase, Others
RK-682
Cat.No: T70523
Synonym:
Target:
Tautomycin
Cat.No: T13095
Synonym:
Target: Others
(Rac)-RK-682
Cat.No: T41370
Synonym:
Target:
3,5-Difluoro-L-tyrosine
Cat.No: T40846
Synonym:
Target:
Fluorescein diphosphate
Cat.No: T20421
Synonym: Fluorescein diphosphate Tetraammonium salt,FDP
Target:
Fostriecin (free base)
Cat.No: T68458
Synonym:
Target:
MLS-0437605
Cat.No: T40968
Synonym:
Target:
Microcystin-LA
Cat.No: TP1698
Synonym:
Target:
MurA-IN-1
Cat.No: T35877
Synonym:
Target:
PTPN22-IN-1
Cat.No: T40216
Synonym: PTPN22-IN-1
Target:
Lockdown
Cat.No: T71845
Synonym:
Target:
Naphthol AS-GR phosphate disodium
Cat.No: T75366
Synonym:
Target:
Fosmanogepix
Cat.No: T11314
Synonym: APX001,E1211
Target: Others
RK-682 (calcium salt)
Cat.No: T36367
Synonym:
Target:
4-Methylumbelliferyl phosphate disodium
Cat.No: T75340
Synonym:
Target:
Okadaic acid ammonium salt
Cat.No: T39183
Synonym:
Target:
Ac-MBP (4-14) Peptide
Cat.No: T76486
Synonym:
Target:
Phenytoin-d10
Cat.No: T68918
Synonym:
Target:
Suramin
Cat.No: T75303
Synonym:
Target:
PAP-IN-1
Cat.No: T81548
Synonym:
Target:
NAZ2329
Cat.No: T63405
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T38587 Chrysophanol triglucoside

Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia , inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC 50 s of 80.17 and 197.06 μM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
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

天然产物

Chrysophanol triglucoside
Cat.No: T38587
Synonym:
Target:
Okadaic acid
Cat.No: T16381
Synonym:
Target: Others
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