Phosphatase

SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.

L-690330 hydrate is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively.

PHPS1 sodium is a potent and selective Shp2 inhibitor with Kis of 0.73, 5.8, 10.7, 5.8, and 0.47 μM for Shp2, Shp2-R362K, Shp1, PTP1B, and PTP1B-Q, respectively.

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

TD52, an Erlotinib derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity.

NCGC00378430 is a potent inhibitor of the SIX1/EYA2 protein-protein interaction.

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.

SHP2-IN-6 hydrochloride is a potent SHP2 inhibitor with an IC50 of 25.8 nM. SHP2-IN-6 hydrochloride is extracted from patent WO2017211303A1, compound 7.

Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A).

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.

CDC25B-IN-2 is a potent cdc25B inhibitor.

CPT-157633, a difluoro-phosphonomethyl phenylalanine derivative, and is a PTP1B inhibitor.

DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM.

SHP389 is an allosteric SHP2 inhibitor, with an IC50 of 36 nM for both SHP2 and p-ERK.

RMC-4630 (SHP2-IN-7) is an SHP2 inhibitor extracted from patent WO2018013597.

PTP1B-IN-3 diammonium is a potent and orally active PTP1B inhibitor with IC50s of 120 nM for both PTP1B and TCPTP.

BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 ?M, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.

ABBV-CLS-484 is a potent PTPN1 or PTPN2 inhibitor with a sub-nanomolar activity.

MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor.

MP07-66, a FTY720 analogue, is devoid of immunosuppressive effects and shows promising antitumor effects in chronic lymphocytic leukemia by disruption of the SET-PP2A complex leading to PP2A reactivation.

Calcium glycerophosphate is an inhibitor of intestinal alkaline phosphatase F3.

LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively.

GDC-1971 (compound 199) is a SHP2 inhibitor.