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Phosphatase

Phosphatase相关产品(54)
货号 产品名 中文名称 产品描述
SJ-MX0285 TNO155

TNO155 是一种有效的,选择性的,和具有口服活性野生型 SHP2 的变构抑制剂, 对应的IC50值为0.011 μM。TNO155 有研究 RTK 依赖性恶性肿瘤的潜力,尤其是晚期实体瘤。

SJ-MX0383 Salubrinal

Salubrinal 是有效的选择性 eIF2α 去磷酸化抑制剂。可以抑制ER应激介导的细胞凋亡,无细胞试验中EC50约为15 μM。Salubrinal 作为双特异性磷酸酶 2 (Dusp2) 抑制剂,抑制抗胶原蛋白抗体诱导的关节炎。Salubrinal 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。

SJ-MX0324 LB-100

LB-100是水溶性的protein phosphatase 2A (PP2A)抑制剂,在BxPc-3和Panc-1细胞中,IC50分别为0.85和3.87 μM。

SJ-MX0097 RMC-4550 RMC-4550 是一个有效的、选择性的蛋白酪氨酸磷酸酶 2 的 (SHP2)变构抑制剂,其 IC50 值为0.583 nM。
SJ-MX3462 CPDA CPDA [N-[4-(4-chlorobenzyloxy)pyridin-2-yl]-2-(2,6-difluorophenyl)- acetamide] is a novel potent inhibitor of SHIP2 [SH2-containing 5'-inositol phosphatase 2] that can effectively ameliorate insulin resistance in 3T3-L1 adipocytes. CPDA was identified using in-silico ligand-based drug design (LBDD) in an attempt to identify inhibitors of SH2-containing 5'-inositol phosphatase 2 (SHIP2), which is implicated in insulin-resistant type 2 diabetes. Among the compounds synthesized,  (CPDA, 4a) was identified as a potent SHIP2 inhibitor. CPDA was found to enhance in vitro insulin signaling through the Akt pathway more efficiently than the previously reported SHIP2 inhibitor AS1949490, and ameliorated abnormal glucose metabolism in diabetic (db/db) mice.
SJ-MX3489 Sal003 Sal003 is a potent, selective and cell-permeable eIF-2α phosphatase inhibitor. Sal003 increases eIF2α phosphorylation status by blocking eIF2a phosphatases in cells. In mouse embryonic fibroblasts (MEFs), Sal003 causes dissociation of polysomes by increasing eIF2a phosphorylation. Sal003 impairs late-long-term potentiation (L-LTP) in an ATF4-dependent mode in hippocampal slices from WT mice. In addition, eIF2α phosphorylation by Sal003 also enhances apoptotic signaling induced by subtilase cytotoxin (SubAB).
SJ-MX3563 SHP099 SHP099 is a highly potent, selective and orally bioavailable SHP2 inhibitor (IC50 value 0.071 μM) that stabilizes SHP2 in an auto-inhibited conformation. SHP099 potently inhibits ERK phosphorylation and the growth of cancer cell lines that have alterations in RTKs or other tyrosine kinases such as the Janus kinases JAK1 and JAK2. SHP099 showed no detectable activity against a panel of 21 phosphatases and 66 kinases (including the closest homologue SHP1), and only had modest activity against 5HT3 when profiled against a preclinical safety pharmacology panel representing 49 common adverse drug reaction targets.
SJ-MX3609 PTP1B-IN-1 PTP1B-IN-1 is a potent and new class of inhibitor of protein tyrosine phosphatase-1B (PTP1B) with IC50 of 1.6 mM; It incorporates the 1,2,5-thiadiazolidin-3-one-1,1-dioxide template that was identified through structure-based design. The site specific functionalization of phosphate groups with amino acid side chains of substrate proteins represents one of the most important regulatory mechanisms of biological systems. Phosphorylation and dephosphorylation are reversibly catalyzed by protein kinases and protein phosphatases, and the aberrant regulation of these enzymes is associated with the onset and progression of various disease states such as cancer, diabetes, neurodegenerative and autoimmune disorders, making these proteins attractive targets for drug discovery.
SJ-MX3756 F1063-0967 F1063-0967 是一种双特异性磷酸酶 26 (DUSP26) 抑制剂,其 IC50 值为 11.62 μM。
SJ-MX1609 KY-226 KY-226 是一种有效的,选择性的,口服活性的和变构蛋白酪氨酸磷酸酶 1B (PTP1B) 抑制剂,IC50 为 0.25 μM,且不激活 PPARγ 。KY-226 通过增强胰岛素和瘦素信号传导发挥抗糖尿病和抗肥胖作用。KY-226 还可以保护神经元免受脑缺血损伤。
SJ-MX1690 MSI-1436 MSI-1436 是具有选择性的 PTP1B 的非竞争性抑制剂,其 IC50 为 1 μM,而对 TCPTP 的 IC50 值为 224 μM。
SJ-MX2017 Rbin-1

Rbin-1 (Ribozinoindole-1)是有效的,可逆的真核核糖体组装的化学抑制剂,GI50 为 136 nM。体外实验显示Rbin-1有效抑制重组的全长Mdn1的ATPase活性。

SJ-MX2715 Sodium orthovanadate 钒酸钠 Sodium Orthovanadate is a commonly used general inhibitor for protein tyrosine phosphatases (PTPs). It is a competitive inhibitor. The inhibition by Vanadate is completely reversible upon the addition of EDTA or by dilution.
SJ-MX3717 2-Bromo-4'-hydroxyacetophenone 2-Bromo-4'-hydroxyacetophenone 是PTP1B 的有效抑制剂,其Ki 值为42 μM。
SJ-MX3718 PTP inhibitor 1 PTP inhibitor 1 是一种蛋白酪氨酸磷酸酶 (PTP) 抑制剂,具有抗血管生成活性。
SJ-MX0018 CCT007093 CCT007093 是有效的蛋白磷酸酶 1D (PPM1D Wip1) 的抑制剂。Wip1 的抑制可激活mTORC1 通路,增强肝切除手术后肝细胞的增殖。
SJ-MX1806 NSC-87877 disodium NSC-87877 disodium 是一种有效的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。NSC-87877还抑制双特异性磷酸酶26 (DUSP26)。
SJ-MB0013 (-)-p-Bromotetramisole Oxalate (-)-对溴四咪唑草酸盐 (-)-p-Bromotetramisole Oxalate 是强效的非特异性的碱性磷酸酶抑制剂。
SJ-MX1100 PRL-3 Inhibitor (Compound 5e) PRL-3 Inhibitor (Compound 5e)是一种有效的 PRL-3 抑制剂,IC50 为 0.9 μM。PRL-3 Inhibitor (Compound 5e)在细胞检测中显示降低侵袭性。
SJ-MX2244 NCGC00378430 NCGC00378430 是一种 SIX1/EYA2 complex 的抑制剂,可在体内显着抑制乳腺癌相关的转移,而不会显着改变原发性肿瘤的生长。