Esterases (Phosphomono-)
The family of phosphoprotein phosphatases includes enzymes that dephosphorylate serine, threonine (EC 3.1.3.16) and tyrosine (EC 3.1.3.48) residues within their substrates. Analogous to kinases, some show certain specificity towards Ser/Thr or Tyr residues, like PPM1D (EC 3.1.3.16). Phosphatases that do not show this selectivity are classified as dual-specificity phosphatases (DUSP).
DUSPs have been implicated as major modulators of critical signaling pathways that are dysregulated in various diseases. DUSPs can be divided into six subgroups on the basis of sequence similarity. Of these subgroups, a great deal of research has focused on the characterization of the mitogen-activated protein kinase phosphatases (MKPs)[1]. While DUSP1 has been identified as a prototypic MAPK phosphatase, an essential endogenous regulator of the inflammatory response to lipopolysaccharide (LPS)[2], the DUSP6 functions as a feedback regulator of fibroblast growth factor (FGF) signaling to limit the activity of extracellular signal–regulated kinases (ERKs) 1 and 2[3].
[1] Dual-specificity phosphatases: critical regulators with diverse cellular targets. K.I. Patterson et al. Biochem. J. 2009, , 418, 475-489.
[2] Dual specificity phosphatase 1 (DUSP1) regulates a subset of LPS-induced genes and protects mice from lethal endotoxin shock. M. Hammer et al. J. Exp. Med. 2006, 203, 15-20.
[3] Dusp6(Mkp3) is a negative feedback regulator of FGF stimulated ERK signaling during mouse development. Chaoying Li. Development. 2007, 134, 167-176.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3729 | ABBV-CLS-484 hydrochloride | Inhibitor of phosphatase PTPN1/N2 (Protein Tyrosine Phosphatase Non-Receptor Type 1 and 2), | Inquire | |
| 2178 | BCI | Allosteric inhibitor of dual-specificity phosphatases (DUSP) | €75.00 | |
| 2852 | BCI hydrochloride | Allosteric inhibitor of dual-specificity phosphatases (DUSP) | €75.00 | |
| 1821 | CCT 007093 | Protein phosphatase 1D (PPM1D) inhibitor | €95.00 | |
| 3018 | DJ001 | Selective, non-competitive, allosteric inhibitor of PTPσ | €125.00 | |
| 3439 | FBPase-1 inhibitor | Allosteric inhibitor of fructose-1,6-bisphosphatase (FBPase-1) | €110.00 | |
| 3767 | GDC-1971 | Orally available, potent, and selective inhibitor of the protein tyrosine phosphatase SHP2 | Inquire | |
| 3721 | JAB-3068 | SHP2 inhibitor | Inquire | |
| 2820 | LB-100 | Specific, competitive inhibitor of PP2A | €110.00 | |
| 3680 | LockdownPro | Prodrug of Lockdown; PPM1F inhibitor | €90.00 | |
| 2480 | LW6 | Inhibitor of HIF-1α stability via MDH2 inhibition and/or binding with CHP1 | €85.00 | |
| 3559 | Myricetin | RNase L inhibitor | €70.00 | |
| 3080 | NCGC00249987 | Specific, allosteric EYA2 phosphatase inhibitor | €130.00 | |
| 3267 | NCGC00378430 | SIX1/EYA2 complex inhibitor | €140.00 | |
| 2702 | NQ301 | Selective allosteric inhibitor of CD45 | €90.00 | |
| 3086 | NSC 95397 | Potent and selective Cdc25 dual specificity phosphatase (DUSP) inhibitor | €70.00 | |
| 3436 | PRL-3 inhibitor | Selective inhibitor of PRL-3 | €90.00 | |
| 3004 | Raphin1 | Selective, brain-penetrant, and orally bioavailable inhibitor of PPP1R15B (R15B) | €105.00 | |
| 2983 | Raphin1 acetate | Selective, brain-penetrant, and orally bioavailable inhibitor of PPP1R15B (R15B) | €110.00 | |
| 3868 | RMC-4550 hydrochloride | Potent, selective and orally available small molecule allosteric inhibitor of SHP2 | Recently added | Inquire |
| 2963 | SBI-425 | Potent, selective and orally bioavailable TNAP inhibitor | €125.00 | |
| 2524 | Sephin 1 | Selective PPP1R15A inhibitor devoid of PPP1R15B and α2-adrenergic activity | €55.00 | |
| 2186 | SF 1670 | Inhibitor of PTEN with significant inhibitory effect on PTPRC and GALK | €120.00 | |
| 2633 | SHP099 | Highly potent, selective and orally bioavailable SHP2 inhibitor | €80.00 | |
| 2263 | Tacrolimus | Potent Calcineurin (Ca2+ dependent protein phosphatase 2B) inhibitor | €100.00 | |
| 3865 | TNO155 | Selective and orally bioavailable allosteric inhibitor of SHP2 | Recently added | Inquire |
| 2723 | TPI-1 | Selective SHP1 inhibitor | €95.00 | |
| 3400 | Tubulin inhibitor 6 | Tubulin polymerization inhibitor; iHAP | €90.00 | |