Enzymes

Naphthol AS-BR is a substrate for the histochemical demonstration of acid and alkaline phosphatase.

EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells).

SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 ?M.

7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with an IC50 of ~1-3 μM.

SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM.

NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).

Andecaliximab is a recombinant IgG4 monoclonal antibody that targets matrix metalloproteinase 9 (MMP9). Andecaliximab has demonstrated anti-fibrotic efficacy in a mouse model of idiopathic pulmonary fibrosis. Andecaliximab can be used for research on gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF).

cyclo(RLsKDK) (TFA) (BK-1361 (TFA)) is a specific inhibitor of the metalloproteinase ADAM8, with an IC50 value of 182 nM. It has potential applications in inflammatory diseases and cancer.

EWP 815 is a disulfide analogue and an effective inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. It also participates in inhibiting the activity of dopamine beta-hydroxylase in vivo.

HKB99 is a conformational inhibitor of phosphoglycerate mutase 1 (PGAM1), which is a glycolytic enzyme. HKB99 inhibits the formation of invasive pseudopodia and increases the level of plasminogen activator inhibitor-2 (PAI-2). It also increases oxidative stress, activates JNK/c-Jun, and inhibits AKT and ERK. HKB99 can be used for research on non-small cell lung cancer (NSCLC).

JMS-053 is an effective, selective, and reversible inhibitor of PTP4A. It inhibits PTP4A1, PTP4A2, PTP4A3, CDC25B and DUSP3 with IC50 values of 29.1 nM, 48.0 nM, 34.7 nM, 92.6 nM and 207.6 nM respectively. JMS-053 can inhibit cancer cell migration and spheroid growth while reducing the growth of ovarian tumors in vivo.

JUN-1111 is an irreversible selective inhibitor of Cdc25 phosphatase, with IC50 values of 0.38, 1.8, 0.66, 28 and 37 μM for Cdc25A, Cdc25B, Cdc25C, VHR and PTP1B respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases and reduces the expression of phosphoCdk1.

MMP2-IN-1 is a moderately effective inhibitor of MMP2, with an IC50 of 6.8 μM. MMP2-IN-1 exhibits significant anti-proliferative activity in certain cancer cells by blocking the cell cycle and inducing apoptosis.

MMP-7-IN-1 is an effective and selective inhibitor of MMP-7 (IC50=10 nM), with IC50>11 mM for MMP-1, -2, -3, -8, -9, and -13. MMP-7 is a potential target for diseases such as cancer and fibrosis.

MY33-3 is an effective and selective inhibitor of protein tyrosine phosphatase RPTPβ/ζ, with an IC50 value of ~0.1 μM. MY33-3 also inhibits PTP-1B (IC50 ~0.7 μM). MY33-3 can reduce ethanol consumption and alleviate neuroinflammation and cognitive dysfunction caused by Sevoflurane.

NFF-3 TFA peptide is a selective MMP substrate. NFF-3 TFA selectively binds to MMP-3 and MMP-10 and is hydrolyzed by them. NFF-3 TFA is also cleaved by trypsin, hepatocyte growth factor activator, and factor Xa. By labeling NFF-3 TFA with CyDye Cy3/Cy5Q, fluorescence can be generated in cell experiments to detect cellular activity.

PRL-3 Inhibitor 2 (compound 2) is an effective inhibitor of PRL-3, with an IC50 value of 28.1 μM.

SPAA-52 is a low molecular weight protein tyrosine phosphatase (LMW-PTP) inhibitor with oral activity, competitive and reversible properties (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used for research on diabetes.

Uralenol is a natural PTP1B inhibitor (IC50=21.5 μM) derived from Broussonetia papyrifera. In many cellular and biochemical studies, PTP1B has been shown to play a major role in the dephosphorylation of insulin receptors.

FN-439 TFA is a selective collagenase-1 inhibitor.

ML 400 is a potent and selective LMPTP inhibitor with an IC50 value of 1680 nM.

KLH45b is an inhibitor of DDHD2 (DDHD domain containing 2).