A potent, selective, reversible Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively.

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

A selective protein phosphatase PHLPP inhibitor with IC50 of 4 uM for PP2C domain of PHLPP2.

BCI is A small-molecule, allosteric inhibitor of DUSP6 (dual-specificity phosphatase 6) with IC50 of 12.3 uM; also inhibits human DUSP1 with IC50 of 11.5 uM; suppresses the ERK-induced activation of Dusp6 and regulates heart size in zebrafish.

Benzbromarone is a highly effective and well tolerated non-competitive inhibitor of xanthine oxidase, used as an uricosuric agent, used in the treatment of gout.

CDC25 Phosphatase Inhibitor I, BN82002, is a cell-permeable ortho-hydroxybenzylamino compound that has been reported to display antitumor properties.

JTT-551 (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR.

JTT-551 sodium (JTT551, JTT 551) is a novel potent, selective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with Ki of 0.22 uM, displays >45-fold and >136-fold selectivity over TCPTP, CD45 and LAR.

LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

LMPTP inhibitor 1 is a potent molecule for diabetes which can increase liver IR phosphorylation in vivo and reverses high-fat diet-induced diabetes by inhibiting the IR phosphatase LMPTP.

NQ301 is a selective CD45 inhibitor (IC50 = 200 nM). Exhibits >200-fold selectivity for CD45 over six related protein tyrosine phosphatases.

Raphin1 is an orally available selective phosphatase inhibitor improves proteostasis and diminishes deficits in a mouse model of Huntington’s disease.

Razuprotafib is a potent protein tyrosine phosphatase β (HPTPβ) inhibitor..

Razuprotafib sodium is a potent protein tyrosine phosphatase β(HPTPβ) inhibitor..

RMC-4550 (RMC4550) is a potent, selective, allosteric inhibitor of SHP2 with IC50 of 0.58 nM (full-length SHP2 enzyme), suppresses pERK signaling in Calu-1 cells with IC50 of 7 nM.

SHP099 is a selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM.

SHP099 is a selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM.

TPI-1 is a potent and selective SHP-1 inhibitor effective at low nanomolar levels.

KY-226 (KY226) is a potent, allosteric, orally active inhibitor of protein tyrosine phosphatase 1B (PTP1B) with IC50 of 0.28 uM (human PTP1B), does not exhibit PPARγ agonist activity.

(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.

DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration.

Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.

SC-43, a sorafenib derivative, is an agonist of Src-homology protein tyrosine phosphatase-1 (SHP-1/PTPN6) and reduces liver fibrosis. SC-43 reduces p-STAT3 and induces apoptosis with anti-tumor activity.

C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.

ARL67156 trisodium salt hydrate is an inhibitor of ecto-ATPase. ARL67156 trisodium salt hydrate is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively. ARL67156 trisodium salt hydrate prevents in vivo the development of calcific aortic valve disease.

1-Naphthyl phosphate potassium salt is a non-specific phosphatase inhibitor. 1-Naphthyl phosphate potassium salt decreases the splice-correcting effect.

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

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.

AQX-435 is a potent SHIP1 phosphatase activator. AQX-435 reduces PI3K activation downstream of the B-cell receptor (BCR) and induces apoptosis of malignant B cells, and reduces lymphoma growth.

3,5-Difluoro-L-tyrosine is a functional, tyrosinase-resistant mimetic of tyrosine. 3,5-Difluoro-L-tyrosine can be used to analyze the substrate specificity of protein tyrosine phosphatases (PTPs).

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).

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.

Calcineurin autoinhibitory peptide is a selective inhibitor of Ca2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide could protect neurons from excitatory neuronal death.

Calcineurin autoinhibitory peptide TFA is a selective inhibitor of Ca2+/calmodulin-dependent protein phosphatase (calcineurin), with an IC50 of ~10 μM. Calcineurin autoinhibitory peptide TFA could protect neurons from excitatory neuronal death.

[pTyr5] EGFR (988-993) TFA is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) TFA is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).

2-Bromo-4'-hydroxyacetophenone a PTP1B inhibitor, with a Ki of 42 μM.

L-690330 hydrate is a competitive 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. L-690330 hydrate exhibits 10-fold more sensitive than mouse and rat IMPase.

SHIP2-IN-1 is a potent SHIP2, inhibits SHIP2 activity, with an IC50 of 2 µM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease.

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 bind

DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property.

Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes.

Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist...

SHP2 IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC50 of 3 nM.

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. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders.

CDC25B-IN-2 is a potent cdc25B inhibitor.

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 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.

PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent.

PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.

PTP1B-IN-14 is a selective PTP1B inhibitor (IC50 = 0.72 μM) targeting the allosteric site.

Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter.

Cytostatin is a potent and selective inhibitor of PP2A with promising antitumor activity. Cytostatin belongs to the fostriecin family of natural products.

SHP2 protein degrader-1 is a potent allosteric inhibitor of SHP2. SHP2 protein degrader-1 induces SHP2 degradation and cell apoptosis. SHP2 protein degrader-1 has the potential for the treatment of SHP2 related diseases.

Dibefurin is a fungal metabolite that acts as an inhibitor of calcineurin phosphatase.

PTP1B-IN-15 is a potent and selective inhibitor of protein tyrosine phosphatase 1B (PTP1B). PTP1B-IN-15 has the potential for the research of type II diabetes and obesity.

Calcium glycerophosphate is an inhibitor of intestinal alkaline phosphatase F3. Calcium glycerophosphate is a source of calcium and phosphorus in total parenteral nutrition solutions.

Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy.

Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.

Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts.

SHP2 inhibitor is an effective SHP2 allosteric inhibitors (IC50≤50 nM), blocking the activation of SHP2 by targeting the auto-inhibited conformation of SHP2 (WO2019183367A1, compound 118).

GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.

(S)-ABBV-CLS-484 is a potent PTPN1 or PTPN2 inhibitor.

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo.

NSC45586 free base (NCS 45586, NCI45586) is a potent, specific PHLPP2 inhibitor with IC50 of 4 uM, targets the PHLPP2 PP2C domain, suppresses MYC and triggers cell death.

CNBDA is a novel selective Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitor with IC50 of 5 uM, 25-fold selectivity over SHP1.Treatment HER2-positive BC cells with CNBDA suppressed cell proliferation in 2D culture, anchorage-independent growth in soft agar, and mammosphere (tumorisphere) formation in suspension cultures in a concentration-dependent manner.CNBDA inhibited EGF-induced signaling and expression of HER2 by inhibiting the PTPase activity of SHP2 in BC cells.

IACS-15414 (IACS 15414) is a potent, selective, orally bioavailable SHP2 inhibitor with IC50 of 122 nM; IACS-15414 potently suppressed the mitogen-activated protein kinase (MAPK) pathway signaling and tumor growth in RTK-activated and KRASmut xenograft models in vivo. IACS-15414 potently suppressed the mitogen-activated protein kinase (MAPK) pathway signaling and tumor growth. IACS-15414 had excellent PK properties across species but a narrow hERG window.

Lockdown Ester Prodrug (Lockdown Pro) is the ester-modified Lockdown with increased membrane permeability and prodrug-like properties, a selective small-molecule inhibitor of the integrin phosphatase PPM1F, blocks cancer cell invasion.Lockdown Ester Prodrug (Lockdown Pro) effectively block PPM1F-mediated effects on integrin β1 and PAK in cells, Lockdown Pro suppresses tissue invasion by PPM1F-overexpressing human cancer cells.

Lockdown is a selective, reversible and non-competitive inhibitor of the integrin phosphatase PPM1F (IC50=16.37 uM), blocks cancer cell invasion.Lockdown acts in a dose-dependent, allosteric manner with high selectivity for PPM1F.Lockdown does not inhibit other protein phosphatases (PTP1P, PTPRJ, PP5) in vitro and does not induce additional phenotypes in PPM1F knockout cells.Lockdown fully re-capitulated the phenotype of PPM1F-deficient cells, increased phosphorylation of PPM1F substrates and corruption of integrin-dependent cellular processes in Lockdown treated glioblastoma cells.Phosphatase PPM1F is a regulator of cell adhesion by fine-tuning integrin activity and actin cytoskeleton structures. Elevated expression of this enzyme in human tumors is associated with high invasiveness, enhanced metastasis, and poor prognosis.

NHB1109 is a potent, selective, orally active PTPRD phosphatase inhibitor with IC50 of 0.6 uM, displays selectivity over PTPRS, PTPRF, PTPRJ or PTPN1/PTP1B phosphatases.NHB1109 exhibited no substantial potency at other protein tyrosine phosphatases screened, no significant potency at any of the targets of clinically-useful drugs identified in EUROFINS screens.NHB1109 (200 mg/kg) is well tolerated by mice.NHB1109 is a good candidate to advance to in vivo studies in addiction paradigms and toward human use to reduce reward from addictive substances.

NRT-870-59 is a potent, reversible PTP4A3 inhibitor (IC50=86 nM) with inhibitory specificity for PTP4A3 versus both PTP4A3 A111S mutant and CDC25B.NRT-870-59 does not inhibit CDC25B and PTP4A3 A111S mutant at 1 uM, and 5- to 6-fold less potent aginst DUSP3.NRT-870-59 inhibits PTP4A1, PTP4A2, PTP4A3 mutants C49S, K144I and A106V with IC50 of 133.2, 264.4, 86.0, 332.2, 180.2 and 57.7 nM, respectively.NRT-870-59 inhibits cancer cell colony formation, which is required PTP4A3 expression.The PTP4A (phosphatase of regenerating liver/PRL) phosphatases are a unique subfamily of protein tyrosine phosphatases (PTPs) comprising three highly homologous members (PTP4A1, PTP4A2, and PTP4A3) with 80% amino acid sequence identity.PTP4A3, and to a lesser extent PTP4A1 and PTP4A2, are overexpressed in many types of cancer, promote tumor invasion and dissemination, and contribute to poor patient prognosis.

PF-07284892 (PF 07284892) is a small molecule inhibitor of SHP2 that may block MAPK signaling and lead to tumor growth inhibition.

RMC-4630 is a potent and selective inhibitor of SHP2, a central node in the RAS signaling pathway.

SBI-2130 (SBI 2130) is a novel furanylbenzamide molecule as inhibitor of both WT and oncogenic SHP2 with IC50 of 0.22/5.0 uM for Wt SHP2/SHP2-E76K.

SBI-4668 (SBI 4668) is a novel furanylbenzamide molecule as inhibitor of both WT and oncogenic SHP2 with IC50 of 0.73/1.8 uM for Wt SHP2/SHP2-E76K, 13-fold selective over PTP1B and 73-fold selective over STEP; SBI-4668 exhibited cell viability inhibitory effect on cell growth in both Kasumi-1 cells (IC50=8.5 uM) and KYSE-520 cells (IC50=5.4 uM), SBI-4668 on cell viability was also determined in additional AML cell lines, including MOLM-13 (IC50 = 12 μM) and MV4-11 (IC50 = 8.2 μM). SBI-4668 inhibited U-937 cell (harbor a G60R oncogenic mutation in SHP2) growth with IC50 of 6.3 uM, which is comparable to the potency found in AML cells expressing WT SHP2, while RMC4550 showed a very weak effect on this G60R mutation cell.

SCP1 inhibitor T-62 (T-62) is a specific, small molecule covalent inhibitor of small CTD phosphatase 1 (SCP1), reduces transcription factor REST protein level HEK293 cells.

SCP1 inhibitor T-65 (T-65) is a specific, small molecule covalent inhibitor of small CTD phosphatase 1 (SCP1), reduces transcription factor REST protein level HEK293 cells with EC50 of 1.5 uM.T-65 showed no detectable inhibition against a panel of eight mammalian cysteine-based phosphatases, including SHP2, TCPTP, CD45, DUSP3 and and lymphoid protein tyrosine phosphatase (LYP) at 25 uM.T-65 promotes REST degradation, increases expression of REST-suppressed genes DYRK1a, ELAVL1, USP37, CELSR3, and SCN2 in HEK293 cells.

SMIP-30 is a potent and selective inhibitor of PPM1A with IC50 of 1 uM, selectively inhibits the phosphatase activity of PPM1A.SMIP-30 shows poor inhibitory activity against closest homolog PPM1B (IC50>30 uM).SMIP-30 is an uncompetitive inhibitor for PPM1A (Ki=0.84 uM), does not exhibit any cytotoxic effects up to 30 uM in THP-1 macrophages.SMIP-30 dose-dependently reduces the Mtb burden in infected macrophages, and is well tolerated in vivo and combined with rifampicin reduces Mtb burden in the lungs of infected mice.SMIP-30 induces LC3B-II expression, activates autophagy in Mtb-infected macrophages in a PPM1A-dependent manner.SMIP-30 induces a dose-dependent increase in phosphorylation of S403-p62 in WT macrophages.

TK-453 (TK453) is a potent, selective SHP2 allosteric inhibitor with IC50 of 18.76 and 179 nM for SHP2-WT and SHP2-E76K, respectively.TK-453 has strong inhibitory effect on the enzyme activity of the SHP2-WT, and does not inhibit the activity of the SHP2-PTP catalytic domain, and homologues (SHP1 and PTP1B).TK-453 binds SHP2-WT (KD=150 nM) and SHP2-E76K, higher affinity with SHP2 than SHP099.TK-453 binds in the allosteric binding pocket at the junction of three domains and stabilizes the autoinhibition conformation of SHP2.TK-453 alleviates imiquimod (IMQ)-induced inflammation in macrophages, inhibits the phosphorylation levels of p-IKKα/β and p-p65.TK-453 significantly ameliorates imiquimod-triggered skin-like inflammation in mice via inhibition of IL-23/Th17 axis.

ARL67156 (FPL 67156) triethylamine is a selective ecto-ATPase inhibitor. ARL67156 triethylamine is a competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively. ARL67156 triethylamine can be used in the research of disease like calcific aortic valve disease, asthma.

Pimecrolimus hydrate (SDZ-ASM 981 hydrate) is a potent, nonsteroid and orally active calcineurin inhibitor. Pimecrolimus hydrate shows anti-inflammatory activity. Pimecrolimus hydrate has the potential for the research of atopic dermatitis and oral erosive lichen planus.

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.

EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity.

SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research.

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

HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1). HKB99 inhibits the formation of invasive pseudopodia and increases the level of PAI-2 in vitro. HKB99 increases the oxidative stress, activates JNK/c-Jun and suppresses AKT and ERK. HKB99 can be used for the research of non-small-cell lung cancer (NSCLC).

ATUX-1215 is a direct, orally active small molecule activator of protein phosphatase 2A (PP2A), suppresses bleomycin-induced fibrosis in vivo.

ATUX-792 is a small molecule activator of protein phosphatase 2A (PP2A), decreases survival, proliferation, and motility of neuroblastoma in vitro and tumor growth in vivo.

CNBCA is a selective, competitive inhibitor of Src homology phosphotyrosyl phosphatase 2 (SHP2) with IC50 of 0.87 uM, effectively suppresses breast cancer cell phenotypes.

DS-1211 (DS1211) is a potent, selecitve inhibitor of tissue-nonspecific alkaline phosphatase (TNAP) with IC50 of 3.4 nM.

HN252 is a potent protein phosphatase 1B (PPM1B) inhibitor with Ki of 0.52 uM and IC50 of 0.76 uM, shows no inhibition against topoisomerases in vitro.

JAB-3068 (JAB3068) is a potent, selective and orally bioavailable allosteric inhibitor of SHP2.

K161 is a potent, pan-SHIP1/2 inhibitor with IC50 of 1.5- 6 uM and 6.5-13 uM, respectively.

K306 is a specific, small molecule agonist of SH2-containing 5' inositol phosphatase 1 (SHIP1) with EC50 of 119 nM, 10-fold higher selectivity over SHIP2.

NGD61181 is a pyrazole-based SHIP2 inhibitor, has micromolar binding affinity and inhibitory activity, does not contain a phosphatase “warhead,” binds the active site of SHIP2.

NSC49L (NSC30049) is a small molecule agonist (activator) of protein phosphatase 2A (PP2A), specifically stimulates PP2A-Cα activity with Kact of 14 nM, downregulates the AKT1/mTOR/4EBP1-axis, and inhibits p21 translation.

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

SBI-221 is a small molecule inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM and 7.4 uM for SHP2-E76K and SHP2-WT in isothermal CETSA assays, respectively.

SBI-668 is a selective inhihitor of SHP2-E76K mutant with IC50 of 2.1 uM in isothermal CETSA assays, 7-fold selectivity over SHP2-WT (IC50=15 uM).