CDP-Star is a chemiluminescent substrate for alkaline phosphatase. CDP-Star can be used for enzyme-linked immunoassays[1].
Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 µM[1][2].
Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent Apoptosis. Bonannione A induces Autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity[1][2][3].
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research[1].
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively[1].
Anticancer agent 143 (compound 369) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 143 can be used in cancer research[1].
PTP1B-IN-8 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1[1].
SF1670 is a potent and specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor.
PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
h-NTPDase-IN-3 (compound 4d) is a pan-inhibitor of NTPDase with IC50s of 34.13 μM (h-NTPDase1), 0.33 μM (h-NTPDase2), 23.21 μM (h-NTPDase3), 2.48 μM (h- NTPDase8).
D-3 is a selective PSC eliminating agent, inducing toxicity in cultured iPSCs and ESCs after 1 h of incubation, via an alkaline phosphatase-dependent mechanism.
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. SMAP-2 (DT-1154) inhibits the growth of KRAS-mutant lung cancers [1].
Phosphatase-IN-1 (compound II-8), a propranolol (HY-B0573B) derivative, is a phosphatidate phosphatase (Pah) inhibitor. Phosphatase-IN-1 can binds to MoPah1, with an affinity constant of 19.8 μM. Phosphatase-IN-1 inhibits growth of plant pathogens and shows anti-fungal ability. Phosphatase-IN-1 is not toxic to rice seedlings and wheat heads[1].
PSB-06126 is a selective nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with the Ki values of 0.33 μM for rat NTPDase 1, 19.1 μM for NTPDase 2 and 2.22 μM for NTPDase 3, respectively. PSB-06126 acts on human NTPDase 3 with an IC50 value of 7.76 μM and a Ki value of 4.39 μM[1][2].
GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4][1].
(E/Z)-Icerguastat ((E/Z)-Sephin1) is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). (E/Z)-Icerguastat can be used for protein misfolding diseases research[1].
h-NTPDase-IN-4 (compound 4c) is a pan-inhibitor of NTPDase with IC50s of 3.58 μM (h-NTPDase1), 10.21 μM (h-NTPDase2), 0.13 μM (h-NTPDase3), 13.57 μM (h- NTPDase8).
Rosiptor is an activator of SH2-containing inositol-5'-phosphatase 1 (SHIP1).
L-690488 is a prodrug of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330[1][2].
1-(4-Hydroxy-2-methoxyphenyl)-3-(4-hydroxy-3-prenylphenyl), isolated from Broussonetia kazinoki, shows in vitro inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 13.00 μM. PTP1B is a negative regulator of insulin action and an important mediator in the pathogenesis of insulinresistance and non-insulin dependent diabetes mellitus. PTP1B is regarded as a significant target for type 2 diabetes[1].
AS1949490 is a potent and selective SHIP-2 (SH2 domain-containing inositol 5′ phosphatase 2) inhibitor, with an IC50 of 620 nM. AS1949490 activated glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[1][2].
SHP099 is a potent, selective, orally available SHP2 inhibitor with an IC50 of 70 nM.
PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.
Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
Cyclosporin A-d3 is the d3-labeled Cyclosporin A (HY-B0579)[1].
h-NTPDase-IN-2 (compound 3l) is a pan-inhibitor of h-NTPDase, with IC50s of 0.35 μM (h-NTPDase1), 4.81 μM (h-NTPDase2), 37.73 μM (h-NTPDase3), 10.32 μM (h-NTPDase8), respectively[1].
CPDA is a novel potent SH2 domain-containing inositol phosphatase 2 (SHIP2) inhibitor that can effectively ameliorate insulin resistance in 3T3-L1 adipocytes.Target: SHIP2in vitro: CPDA was found to enhance insulin signaling.in vivo: CPDA greatly improves abnormal glucose metabolism in diabetic animals. CPDA was also found to improve the abnormal glucose metabolism in db/db mice.
MY33-3 is a small-molecule inhibitor of RPTPβ/ζ (PTPRZ1) with IC50 of 0.1 uM, significantly increases the phosphorylation of key tyrosine residues of RPTPβ/ζ substrates involved in neuronal survival and differentiation; blocks ethanol conditioned place preference, shows limited effects on ethanol-induced ataxia, and potentiates the sedative effects of ethanol in mice; increases levels of phosphorylated ALK and TrkA in neuroblastoma cells, modulates signaling pathways activated by alcohol.
BCI-215 (BCI215) is a potent, tumor cell-selective dual specificity MAPK phosphatase (DUSP-MKP) inhibitor; restores defective MAPK activity caused by overexpression of DUSP1 and DUSP6 in mammalian cells; inhibits cell motility, causes apoptosis but not primary necrosis, and sensitizes cells to lymphokine-activated killer cell activity in MDA-MB-231 human breast cancer cells; induces rapid and sustained phosphorylation of ERK, p38 and JNK, also hyperactivates MKK4/SEK1; causes selective cancer cell cytotoxicity in part through non-redox-mediated activation of MAPK signaling.
AQX-435 is a potent SHIP1 activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth[1].