Phosphatase Inhibitor

MJE3 is a cell-permeable small-molecule phosphoglycerate mutase 1 (PGAM1) inhibitor. MJE3 is applicable to research related to breast cancer and melanoma.

AZ-PFKFB3-67 (Standard) is the analytical standard of AZ-PFKFB3-67 (HY-101972). This product is intended for research and analytical applications. AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with IC₅₀s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1, respectively. AZ-PFKFB3-67 reduces MCL-1. AZ-PFKFB3-67 has neuroprotective activity.

NSC 95397 (Standard) is the analytical standard of NSC 95397 (HY-108543). This product is intended for research and analytical applications. NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (K_i=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC₅₀=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein K_inase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway.

PDM11 is a derivative of antioxidant resveratrol. PDM11 do not exhibit any significant protective effect against oxidation of linoleate micelles initiated by radiolysis-generated hydroxyl radicals. PDM11 is inactive in resveratrol activity assays.

Dehydrodanshenol A is a non-competitive inhibitor of Protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ value of 8.5 μM. Dehydrodanshenol A can be used in diabetes-related research.

NAZ2329 (Standard) is the analytical standard of NAZ2329 (HY-103693). This product is intended for research and analytical applications. NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC₅₀=7.5 µM for hPTPRZ1) and PTPRG (IC₅₀=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC₅₀ of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC₅₀ of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.

MptpB-IN-3 is a selective inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB) with an IC₅₀ of 0.19 μM. MptpB-IN-3 blocks MptpB-mediated inhibition of the macrophage MAPK pathway and restores the phosphorylation levels of Erk1/2 and p38. MptpB-IN-3 exhibits direct anti-tuberculosis activity against Mycobacterium tuberculosis and reduces the Mycobacterium tuberculosis load in mouse macrophages. MptpB-IN-3 can be used for tuberculosis research.

Ulodesine succinate (BCX4208 succinate) is a purine nucleoside phosphorylase (PNP) inhibitor, with an IC₅₀ of 2.293 nM against human PNP, and low nanomolar IC₅₀ values against mouse, rat and monkey PNP. Ulodesine succinate blocks the production of uric acid precursors, reduces serum uric acid levels, clears accumulated uric acid in the blood, and elevates the levels of purine nucleosides including guanosine. Ulodesine succinate reduces the counts of total lymphocytes, T lymphocytes and lymphocyte subsets, inhibits the proliferation of cancer cells and activated lymphocytes, and enhances vaccine immune responses. Ulodesine succinate can be used in research related to hyperuricemia and gout.

CPT-157633 (Standard) is the analytical standard of CPT-157633 (HY-111469). This product is intended for research and analytical applications. CPT-157633, a difluoro-phosphonomethyl phenylalanine derivative, and is a PTP1B inhibitor. CPT-157633 prevents binge drinK_ing-induced glucose intolerance.

PTP1B-IN-1 (Standard) (PTP1B inhibitor (Standard)) is the analytical standard of PTP1B-IN-1 (HY-10704). This product is intended for research and analytical applications. PTP1B-IN-1 (Compound 7a) is a small molecule inhibitor of PTP1B with an IC₅₀ value of 1.6 mM. It is often used as the mother core for derivatives of analogues.

Cycloepoxydon inhibits the Phorbol 12-myristate 13-acetate (HY-18739) (PMA)-induced NF-KB and AP-1 mediated secreted alkaline phosphatase (SEAP) expression with IC₅₀s of 1-2 μg/mL (4.2-8.4 μM) and 3-5 μg/mL (12.6-21 μM), respectively.

Razuprotafib (Standard) is the analytical standard of Razuprotafib (HY-109041). This product is intended for research and analytical applications. Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC₅₀of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC₅₀ of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC₅₀=36 pM) and HPTPγ (100 pM).

ENT-03 is a centrally acting mammalian aminosterol. ENT-03 upregulates cFos activation, inhibits PTP1b and induces phosphorylation of STAT3. ENT-03 normalizes blood glucose, induces weight loss. ENT-03 can be used in the research of type 2 diabetes and obesity.

3-O-cis-p-Coumaroyl maslinic acid (compound 16) is a natural compound isolated from the ethyl acetate extract of leaves of Miconia albicans.3-O-cis-p-Coumaroyl maslinic acid can inhibit PTP1B, with the IC₅₀ of 0.46 μM, and shows antimicrobial activity on Gram-positive bacteria and yeasts.